Date:
20130319
Dockets: T-1420-11
T-288-12
Citation:
2013 FC 283
Toronto, Ontario, March 19,
2013
PRESENT: The
Honourable Mr. Justice Hughes
Docket:
T-1420-11
BETWEEN:
|
NOVARTIS PHARMACEUTICALS CANADA
INC.
|
|
|
Applicant
|
and
|
|
TEVA CANADA LIMITED and
THE MINISTER OF HEALTH
|
|
|
Respondents
|
|
and
|
|
|
NOVARTIS AG and
BOEHRINGER MANNHEIM GmbH
|
|
|
|
Respondent Patentees
|
Docket: T-288-12
AND BETWEEN:
|
|
|
|
NOVARTIS PHARMACEUTICALS
CANADA INC.
|
|
|
|
Applicant
|
|
and
|
|
|
TEVA CANADA LIMITED and
THE MINISTER OF HEALTH
|
|
|
|
Respondents
|
|
and
|
|
|
NOVARTIS AG and
ROCHE DIAGNOSTICS GmbH
|
|
|
|
Respondent Patentees
|
REASONS FOR JUDGMENT AND JUDGMENT
HUGHES
J.
[1]
These
reasons are common to two applications each brought by Novartis Pharmaceuticals
Canada Inc. under the provisions of the Patented Medicines (Notice of
Compliance) Regulations SOR/93-133 as amended (NOC Regulations). In
each application, Novartis seeks to restrain the Minister of Health from
issuing a Notice of Compliance to Teva Canada Limited; in one application it is
in respect of 4 mg/5 ml strength of zoledronic acid IV infusion (T-1420-11) and
in the other it is in respect of 5 mg/100 ml strength of zoledronic acid IV
infusion (T-288-12) until the expiry of each of Canadian Letters Patent No.
1,338,895 and 1,338,937. The issues in each application are those of validity
of those two patents. Infringement is not an issue in either application. Thus,
the two applications proceeded on common evidence and argument and were heard
together.
[2]
For
the reasons that follow, I find that Teva’s allegations with respect to
invalidity, on the basis of inutility and lack of sufficiency of the ‘895
patent, claim 14 to be justified thus the application is dismissed with respect
to that patent. I find that Teva’s allegations with respect to invalidity of
the ‘937 patent are not justified thus the application will be allowed in
respect of that patent. The Applicant is entitled to half of its costs at the
middle of Column IV.
[3]
The
following is an Index to these Reasons by paragraph number:
THE
PARTIES
|
Paras
4 to 7
|
THE
'895 PATENT GENERALLY
|
Paras
8 to 12
|
THE
'937 PATENT GENERALLY
|
Paras
13 to 17
|
THE
EVIDENCE
|
Paras
18 to 23
|
ISSUES
|
Paras
24 to 27
|
BURDEN
OF PROOF
|
Para 28
|
PERSON
SKILLED IN THE ART
|
Paras
29 to 34
|
THE
'895 PATENT IN DETAIL
|
Paras
35 to 55
|
THE
'895 PATENT – CLAIM 14
|
Paras
56 to 64
|
THE
'937 PATENT IN DETAIL
|
Paras
65 to 78
|
THE
'937 PATENT – CLAIMS 1 & 2
|
Paras
79 to 83
|
BISPHOSPHONATES – TECHNICAL BACKGROUND
|
Paras
84 to 95
|
ZOLEDRONATE
|
Paras
96 to 99
|
TESTING
FOR POTENCY
|
Para 100
|
WHAT
DID THE '895 INVENTORS DO?
|
Paras
101 to 103
|
WHAT
DID THE '937 INVENTORS DO?
|
Paras
104 to 107
|
THE CONFLICT – AND RESULTING CLAIMS
|
Paras
108 to 113
|
OBVIOUSNESS
|
Paras
114 to 116
|
THE '895 PATENT - THE INVENTIVE CONCEPT
|
Paras
117 to 119
|
THE '937 PATENT - THE INVENTIVE CONCEPT
|
Paras
120 to 138
|
DATE OF THE INVENTION - '895 PATENT
|
Paras
139 to 142
|
DATE OF THE INVENTION - '937 PATENT
|
Paras
143 to 145
|
WHAT WAS THE “COMMON GENERAL KNOWLEDGE” AND “STATE OF THE ART”
|
Paras
146 to 162
|
LACK OF UTILITY – PLEADING
|
Para 163
|
UTILITY – CLAIM 14 OF THE '895 PATENT
|
Paras
164 to 170
|
LACK OF UTILITY – CLAIMS 1 & 2 OF THE '937 PATENT
|
Paras
171 to 172
|
SUFFICIENCY – PLEADING
|
Para 173
|
SUFFICIENCY – LEGAL PRINCIPLES
|
Paras
174 to 175
|
SUFFICIENCY – DATE FOR DETERMINATION
|
Paras
176 to 189
|
CONCLUSIONS AND COSTS
|
Paras
190 to 193
|
THE PARTIES
[4]
The
Applicant Novartis Pharmaceuticals Canada Inc. (Novartis) is the same in each
application. It has listed each of the two patents at issue in accordance with
the NOC Regulations and has itself obtained Notices of Compliance from
the Minister of Health to sell a bone mechanism regulator product in Canada containing zoledronate as an active ingredient. Novartis is a “first person” as
described in the NOC Regulations.
[5]
The
Respondent Teva Canada Limited (Teva) is a “second person” as so described in
the NOC Regulations. It seeks to sell generic versions of Novartis’
drug. Application T-1420-11 deals with Teva’s intent to seek a Notice of Compliance
to sell such a drug for administration by IV infusion in a 4 mg/5 ml dose and
has served upon Novartis a Notice of Allegation dated July 20, 2011 in
accordance with the NOC Regulations. Application T-288-12 deals with
Teva’s intent to seek a Notice of Compliance to sell such a drug for
administration by IV infusion in a 5 mg/100 ml dose and has served upon
Novartis a Notice of Allegation dated December 23, 2011 in accordance with the NOC
Regulations.
[6]
The
Respondent Minister of Health is charged with various duties under the NOC
Regulations, including the issuance of a Notice of Compliance to a “second
person”, such as Teva, in appropriate circumstances. The Minister took no
active role in these proceedings.
[7]
Novartis
asserts, and Teva does not challenge, that Canadian Patent 1,338,895 is owned
by the Respondent Boehringer Mannheim GmbH and that Canadian Patent 1,338,937
is owned by the Respondent Novartis AG. Neither of these entities took any
active role in these proceedings.
THE '895 PATENT
GENERALLY
[8]
Canadian
Letters Patent No. 1,338,895 (the '895 patent) resulted from an application
filed with the Canadian Patent Office on July 29, 1987. Therefore, that patent
is governed by the provisions of the “old” Patent Act, RSC 1985, c. P-4,
applicable to patents, the application for which was filed in the Canadian
Patent Office prior to October 1, 1989.
[9]
The
'895 patent claims priority from an application filed in the Federal Republic
of Germany on August 1, 1986. This is the presumed “date of invention” upon
which the issue of obviousness is to be determined provided that the priority
document is in the evidence and supports the claimed invention. A different
date of invention can also be proved by evidence as to what the inventors did.
[10]
The
'895 patent was issued and granted to Boehringer Mannheim GmbH on February 4,
1987. The patent is to be construed as of that date. The term of the patent is
to be calculated as being seventeen (17) years from the date of grant; thus
this patent’s term will expire February 4, 2014.
[11]
The
'895 patent names Elmar Bosies and Rudi Gall, both of the Federal Republic of
Germany, as inventors. The record shows that Bosies is deceased and Gall is
“fearful of death”; therefore, we have no evidence from the inventors in these
proceedings.
[12]
Only
claim 14 of the ‘895 patent is at issue in these proceedings.
THE '937 PATENT
GENERALLY
[13]
Canadian
Letters Patent No. 1,338,937 (the '937 patent) resulted from an application
filed with the Canadian Patent Office on October 19, 1987. Therefore, that
patent, like the '895 patent, is governed by the provisions of the “old” Patent
Act, applicable to patents applied for in Canada before October 1, 1989.
[14]
The
'937 patent claims priority from an application filed with the Swiss Patent
Office on November 21, 1986. This is the presumed “date of invention” upon
which the issue of obviousness is to be determined based on the evidence as
discussed with respect to the ‘895 patent.
[15]
The
'937 patent was issued and granted to Ciba-Geigy AG of Switzerland on February 25, 1997. The patent is to be construed as of that date. The term
of the patent is to be calculated as being seventeen (17) years from that date;
thus, this patent’s term will expire February 25, 2014.
[16]
The
'937 patent names Knut A. Jaeggi and Leo Widler, both of Switzerland, as inventors. One of them, Leo Widler, provided evidence in these proceedings.
[17]
The
'937 patent contains two (2) claims, claims 1 and 2, both of which are at issue
in these proceedings.
THE
EVIDENCE
[18]
As
is usual in these proceedings, the evidence took the form of affidavits,
exhibits to affidavits, transcripts of cross-examination, and exhibits to
cross-examination. The Court had no opportunity to see or hear the witnesses, or
to observe their demeanour.
[19]
The
Applicants have filed the affidavits, with exhibits, of the following persons:
•
Dr.
Leo Widler: He
is one of the named inventors of the '937 patent. He is a Senior Investigator,
Global Discovery chemistry at the Novartis Research Institutes for Biomedical
Research in Basel, Switzerland. He provided some history as to bisphosphonates
generally, and particular history leading up to the '937 patent. He was
cross-examined.
•
Dr.
Martin Knauer: of Bensheim Germany He is a Patent Attorney
employed by Roche Diagnostics GmbH as Director and Senior Patent Counsel for
patent conflicts. He filed two affidavits attaching as exhibits documents of
Boehringer Mannheim (acquired by Roche) relating to developments leading to the
'895 patent. He was cross-examined.
•
Dr.
Frank H. (Hal) Ebetino (expert): of Blackrock, Ireland. He is a consultant in drug discovery and development with specific expertise in the
bisphosphonate (BP) field. He is a Visiting Scholar at the University of Southern California, and a Visiting Research Professor at Queen’s University, Belfast. He worked with Proctor & Gamble in the early development of BPs. He provided
a history of the development of generations of BPs. He dealt with arguments and
evidence of Teva as to obviousness and sufficiency of the ''937 patent. He was
cross-examined.
•
Dr.
Mark Lundy (expert): of West Chester, Ohio. He is President
of Osteoresearch LLC, a consulting firm for the pharmaceutical industry. He
received a PhD I Biomedical Sciences from Albany Medical College and started
his courses in the bone field as a post-doctoral fellow in the Department of
Medicine and Anatomy at Loma Linda University in California. He joined Proctor
& Gamble and did much of the early research into BPs there. He provided a
history of the development of BPs and specific opinions respecting the '895 and
'937 patents. He reviewed the documents provided by Dr. Knauer as to
developments leading to the '895 patent. He addresses in particular statements as
to utility made in Dr. Grynpas’ affidavit. He was cross-examined.
•
Dr.
James J. Benedict (expert): of Aveda, Colorado, Vice-President of
Research and Development at Cerapedics, Inc. He received a doctorate from the University of Wisconsin in Transition Metal Organometallic Chemistry. He began his career
at Proctor & Gamble dealing with phosphonates and moved on to other
organizations engaged in bone metabolism and bisphosphonate research. He gave a
history of bisphosphonates and opinions as to inventiveness of the '895 patent
and its sufficiency. He rebutted the evidence of some of Teva’s witnesses. He
was cross-examined.
•
Ejvind
Johannes-Christiansen (expert): of Hellerup, Denmark, a European patent attorney. He gave evidence as to when a Danish patent application, 1985 0
5996 was published and actually obtainable by the public. He was not
cross-examined. At the hearing, Counsel for Teva advised the Court that Teva
was not relying on the Danish application for any purpose in these proceedings.
•
Eric
McIntomny:
a law clerk employed in the offices of the Applicants’ Counsel. He provided, as
exhibits, certain correspondence between the firms of Counsel representing
Teva. He was not cross-examined.
[20]
The
Respondent Teva filed the affidavits, with exhibits, of the following persons:
•
Dr.
Stanley Michael Roberts (expert): of Devon, United Kingdom. He received a doctorate from the University of Salford, and did post-doctorates at
the University of Zurich and Harvard University. He was a professor at various English Universities and Head of Chemical Research at Glaxo Group in Greenford, UK. He has received various honours and consults in a variety of areas, including medicinal
chemistry, agrochemistry, biotechnology and combinatorial chemistry. He provides
opinions as to obviousness respecting the '895 and '937 patents. He was
cross-examined.
•
Dr.
Jouko Vepsalainen (expert): of Kuopio, Finland. He received a
doctorate from the University of Joensuu, Finland; his thesis focused on
halomethylene bisphosphonation. He worked exclusively in the area of bisphosphonates.
He teaches and has written many scientific papers in that area. He submitted an
affidavit and rebuttal affidavit directed to the obviousness of the '895 and
'937 patents. He was cross-examined.
•
Dr.
Marc Grynpas (expert): of Toronto, Ontario. He is a Senior
Scientist at the Samuel Lunenfeld Research Institute at Mount Sinai Hospital, Toronto; and a Professor in the Department of Laboratory Medicine & Pathobiology
at the University of Toronto. He deals principally with utility in respect of
the '895 and '937 patents. He was cross-examined.
•
Christine
Slattery:
of Oakville, Ontario. She is fluent in English, French and German and is a
freelance translator. She compared a European Patent Application in German, No.
0 170 228, with a United States patent in English 4,687,767. She found them to
be almost identical. She was not cross-examined. Her evidence is not contested.
•
John
Coakley:
of Hamilton, Ontario. He is a freelance translator fluent, among other things,
in Danish and English. He compared Danish Patent Application No. 168754 with
European Patent Application No. 0186405, in English, and found them to be
mostly identical. He was not cross-examined. As previously stated, the Danish
application is no longer at issue.
•
Melissa
Marie Dimilta: of Toronto, Ontario. An articling student in
Teva’s Counsel’s office. She located and provided a copy of what is called the
Schenck article.
•
Louise
McLean:
of Toronto, Ontario. A law clerk in Teva’s Counsel’s office. She provided an
affidavit and a reply affidavit. She was cross-examined. Her evidence served to
make of record certain documents referred to in the Notices of Allegation and
correspondence between the Counsel for the Applicants and Teva.
[21]
In
addition, certified copies of certain patents, including the '895 and '937
patents, as well as others, were filed.
[22]
Each
of the parties, at the hearing and in their memorandum, tried to marginalize
the evidence of the experts of the other. Dr. Roberts, one of Teva’s experts, was
said to be too much of a generalist and had not been involved in research
respecting bone treatment. He made a search of the prior art, but did not keep
his notes, which he described as “hieroglyphics”. Novartis’ experts were said
to be “too expert” in that they worked too close to the field at the time and
were unable to see the matters clearly as would a “disinterested” scientist.
[23]
I
am unable to come to any conclusion that would cause me to reject, or give
minimal weight, to the evidence of any expert for either party. Dr. Roberts
spoke as a generalist; he conducted, in my opinion, a proper prior art search.
Novartis’ experts were close to the subject but gave what I find to be fair and
disinterested opinions. All of the witnesses for both parties gave useful
evidence. I find no reason to reject or be sceptical about any of it.
ISSUES
[24]
The
main issue is whether or not these applications for prohibition should be
granted. That issue depends on whether the Court has been satisfied, or not,
that Teva’s allegations as to invalidity of the '895 and '937 patents are
justified.
[25]
In
respect of the '895 patent, Teva’s allegations as to invalidity are based on:
•
obviousness
•
lack
of utility
•
insufficiency
[26]
With
respect to the '937 patent, the allegations as to invalidity are based on:
•
obviousness
•
lack
of utility
•
insufficiency
•
overbreadth
[27]
In
its Notice of Allegation, Teva also raised an issue as to double patenting. At
a pre-trial conference, Teva’s Counsel advised the Court that this issue would
not be pursued.
BURDEN
OF PROOF
[28]
The
issues relate only to Teva’s allegations as to invalidity of the two patents at
issue. I recently wrote on that subject in Pfizer Canada Inc v Pharmascience
Inc, 2013 FC 120, and I repeat and adopt what I wrote at paragraphs 25 and
26:
[25] There have been many decisions addressing
the question of burden when the issue in NOC proceedings is that of patent
validity. I refer for instance to Pfizer Canada Inc v Apotex Inc, 2007 FC 26 at
paras 9 and 12, and 2007 FCA 195, leave to appeal to Supreme Court refused;
Pfizer Canada Inc v Canada (Minister of Health), 2012 FC 767 at para 42,
affirmed in the result 2012 FCA 308.
[26] To put the matter briefly, the Patent Act,
subsection 43(2) affords a patent a presumption of validity. In NOC proceedings
the “second person” must lead some evidence to rebut that presumption. Once
such evidence has been led the Court must determine the issue of validity on
the usual civil burden of proof having regard to all the relevant evidence.
PERSON
SKILLED IN THE ART
[29]
The
person skilled in the art (PSIA) or person of ordinary skill in the art
(POSITA) is the person to whom a patent is directed and through whose eyes many
issues respecting a patent are to be considered.
[30]
The
Applicants, in their Memorandum of Argument, propose the following definition
of such a person:
77. Novartis’ position is that a PSIA would be
part of a discovery team at a pharmaceutical company looking for a new BP. The
PSIA would have a Ph.D. degree with some experience in the BP field or,
alternatively, a Master’s or Bachelor’s degree but with more experience investigating
BPs. The discovery team would be composed of medicinal chemists, biologists,
and sometimes other subspecialists such as physical chemists. However, the
medicinal chemist would be the scientist determining which compounds to make
and test. Further, the chemist would also have to have specific experience in
BP chemistry.
[31]
Teva
in its Memorandum of Argument proposes the following definition for such a
person:
33. The skilled person is a skilled technician
who has a mind willing to understand a specification addressed to him, who is
“not a dullard, but lacking in imagination” and who is permitted to experiment
when assessing obviousness, provided that the testing is routine and does not
involve intense investigation. The skilled person “keeps up with the literature
and is skilled in reading a patent, not only within the context of its subject
matter, but also as a legal document. He reads patents in this and other
jurisdictions as if he read them the day they were first made public, casting
aside all he has learned since then”.
34. The parties agree that the skilled person
for the 895 Patent and the 937 Patent would have had a few years of experience
working in the area of drug design or a few years of education at the Ph.D.
level in the pharmaceutical area. The skilled person was part of a project
team, such as the team tasked with developing a new BP. It included a medicinal
chemist who would determine which compounds to make and test. Biologists
conducted tests in models to assess activity and completed the team.
[32]
The
differences between the two are narrow. The Applicants state these differences
as follows in their Memorandum:
78. Novartis’ position is, for the most part,
consistent with Teva’s position with the exception of two important clarifications.
First, the PSIA must have actual experience developing new BPs. Second, to the
extent the PSIA includes a researcher from academia, such persons would only
fall within the definition of a PSIA if the focus of their research was on drug
discovery and if they had experience working with a drug discovery team at a
pharmaceutical company in the BP field.
[33]
Teva
argues at paragraphs 35 through 37 of its Memorandum that the Applicants’
definition is too narrow and would have the effect of eliminating persons other
than those who were employed by one of the five brand companies working on
bisphosphonates at the time; it would include the elimination of Dr. Widler,
one of the inventors named in the '937 patent and a witness for the Applicants.
[34]
I
accept Teva’s definition as the most appropriate and find that the differences
with their definition and that of the Applicants’ are few, and that the
Applicants’ differences create a PSITA that is too narrowly defined.
THE
'895 PATENT IN DETAIL
[35]
The
'895 patent is titled:
Diphosphonic Acid
Derivatives, Processes for the Preparation Thereof and Pharmaceutical
Composition Containing Them
[36]
It
begins at page 1 by stating that the invention concerns “new diphosphonic acid
derivatives; how to prepare them, and pharmaceutical compositions containing
those derivatives:
The present invention is
concerned with new diphosphonic acid derivatives, processes for the preparation
thereof and pharmaceutical compositions containing them.
[37]
At
page 1 from lines 5 to 19, a number of patent applications, all German except
for one European, are identified as disclosing certain diphosphonic acid
derivatives. At page 23, some of these applications are more particularly
identified as issued patents, although there is no particular correlation with those
listed at page 1 and at page 23. Counsel for the Applicants could not explain
why.
[38]
Returning
to page 1, commencing at line 20, the '895 patent identifies a particular
feature of its diphosphonic acid derivatives that differs from the previously
described derivatives; namely, that:
…there is only one carbon atom between this
diphosphonate residue and the heterocyclic radical and the heterocyclic radical
is not a pyrazole ring…
[39]
I
digress from the '895 patent for a moment to point out that this feature can be
illustrated using the examples found at paragraph 25 of Novartis’ Memorandum of
Argument. That example is specific to one of the many compounds embraced by the
'895 patent, Zoledronate, but it serves to illustrate what the patent says is
the inventive concept:
[40]
Returning
to the '895 patent, the description at page 1, starting at line 20 and over to
page 2, describes the features of this particular composition; namely, that
these derivatives are suitable for the wider treatment of calcium metabolism
disturbances:
We have now found that analogous
derivatives of these compounds in which there is only one carbon atom between
the diphosphonate residue and the heterocyclic radical and heterocycle is not a
pyrazole ring also display these actions and , in addition, as good calcium
complex formers, are suitable for the wider treatment of calcium metabolism
disturbances. In particular, they can be very well used in cases in which the
bone formation and breakdown is disturbed, i.e. they are suitable for the
treatment of diseases of the skeletal system, for example osteoporosis,
Bechterew’s disease and the like.
Moreover on the basis of these
properties, they can also be used in therapy of bone matastases or urolithiasis
and for the prevention of heterotopic ossifications. Furthermore, due to their
influencing of the calcium metabolism, they form a basis for the treatment of
rheumatoic arthritis, osteoarthritis and degenerative arthrosis.
[41]
From
the middle of page 2 to page 3, line 18, there is a description of several of
the components of the compound.
[42]
Commencing
at line 24 of page 3 to the end of page 9, several processes for the
preparation of the compounds are described.
[43]
From
the top of page 10 to line 8 of page 11, there is a discussion as to pharmaceutically
acceptable salts.
[44]
At
page 11, lines 9 to 18, there is a discussion as to various forms in which the
pharmaceutical may be administered, liquid or solid.
[45]
From
line 19, page 11, to line 7, page 12, there is a description as to additives,
sometimes called excipients.
[46]
From
lines 8 to 13 of page 12, a general description as to dosages which “can depend
on various factors” is given.
[47]
At
page 13, a test of one of the compounds (not zoledronate) is described with
results tabulated on Table 1 appearing on page 14.
[48]
At
pages 15 through to the middle of page 18, a large number of compounds are
particularly identified as being “Preferred in the sense of the present
invention”. None of them is zoledronate.
[49]
From
the middle of page 18 to the end of page 22, a number of examples are provided,
which are said to “show some of the process variants which can be used in
synthesising the compounds according to the present invention”. Zoledronate is
not specifically identified as a compound which can be produced. However,
Example 1 is said to produce a compound that would fall within the scope of
claim 14 however, that compound is not zoledronate.
[50]
Page
23 has already been discussed.
[51]
The
'895 patent ends with 25 claims. Claim 1 is a very broad claim encompassing a vast
number of compounds. Claim 2 claims a narrower range of compounds, as does
Claim 3. Claims 4 and 5, 15, 16, 17, and 18 are directed to specific compounds;
none of them being zoledronate. Claims 6 and 7 are pharmaceutical composition
claims dependent on one or more of claims 1 through 5. Claims 8 to 12 are
claims directed to the use of the compounds claimed in one or more of claims 1
through 5. Claims 13 and 20 are directed to a process for making the compounds.
[52]
Claim
14 is the claim at issue, which I will subsequently discuss in more detail.
[53]
Claim
19 claims the composition of claim 14, as well as claims 15, 16, 17 or 18, with
a compatible salt.
[54]
Claim
21 claims the composition of claim 14, as well as claims 15, 16, 17 or 18, with
a salt and carrier.
[55]
Claims
22, 23, 24 and 25 are directed to the use of the composition of claim 14, as
well as claims 15, 16, 17 or 18, for various medical purposes such as calcium
metabolism disturbances, arthritis, diseases of the skeletal system, rheumatic
arthritis, osteoarthritis, degenerative arthrosis therapy of bone metastases,
and urolithiasis, and prevention of heterotropic ossification.
THE '895
PATENT – CLAIM 14
[56]
Claim
14 of the '895 patent is the only claim that is at issue in these proceedings.
That claim is an independent claim; that is, it does not incorporate by
reference any other claim; it stands on its own. Claim 14 reads:
14. A heteroarylalkane diphosphonic acid of
formula I
Wherein R1 is a 5-membered heteroaryl
radical selected from imidazolyl, thiazolyl, oxazolyl, isoxazolyl, triazolyl,
thiadiazolyl and oxadiazolyl, which is unsubstituted or substituted one or more
times by lower alkyl, lower alkoxy, phenyl or halogen; R2 is a
hydrogen atom, hydroxyl group or an amino group or a salt thereof.
[57]
Claim
14 is directed to a class of compounds called heteroarylalkane diphosphonic
acids, having the general formula depicted as Formula I, with a number of
choices of atoms or combinations of atoms that can be placed at the R1
and R2 positions. The evidence is that a conservative estimate of
the number of individual compounds that would be embraced by this claim is 1.2
million.
[58]
Any
one of a number of chemical structures may be placed at the R1 position,
each of which may be generally described as a five-membered heteroaryl radical,
with the group within that general description restricted to the following:
…selected from imidazolyl, thiazolyl, oxazolyl,
isoxazolyl, triazolyl, thiadiazolyl and oxadiazolyl, which is unsubstituted or
substituted one or more times by lower alkyl, lower alkoxy, phenyl or halogen;…
[59]
At
the R2 position, there may be a hydrogen atom, or a group of
molecules selected from the hydroxyl group of molecules, or a group of
molecules selected from the amino group of molecules.
[60]
In
the descriptive portion of the '895 patent, R1 is part of
a broader class referred to as Het and R2 as X.
[61]
Thus,
in claim 14, there are a finite number of choices for R1 and
a finite number of choices for R2. The total number of choices is
calculated as being about 1.2 million.
[62]
Among
the resulting choices is that where R1 is an imidazole ring joined
to the Formula I structure at one of the nitrogen positions in the ring and
where R2 is a hydroxyl (OH). The resulting compound may be
chemically depicted as follows:
[63]
This
compound is referred to in the evidence as zoledronate or zoledronic acid. It
is the active ingredient in Novartis’ commercial products. Teva wants to
receive a Notice of Compliance to sell a generic version of those products,
also containing zoledronic acid as the active ingredient.
[64]
Thus
to construe claim 14 it claims a class of some 1.2 million compounds all
sharing a selection of molecules at the R1 and R2 positions
placed on a biphosphonic backbone; zoledronate is but one of such compounds.
THE
'937 PATENT IN DETAIL
[65]
The
'937 patent is titled:
Process for the
Manufacture of Novel Substituted Alkanediphosphonic Acids
[66]
The
patent begins at page 1 by stating that it relates to certain novel acids
depicted as Formula I:
Novel substituted
alkanediphosphonic acids
The present invention
relates to novel substituted alkanediphosphonic acids, in particular to
heteroarylalkanediphosphonic acids of formula
Wherein R1 is a 5-membered heteroaryl
radical which contains, as hetero atoms, 2 to 4 N-atoms or 1 or 2 N-atoms as
well as 1 0- or s-atom, and which is unsubstituted or C-substituted by lower
alkyl, phenyl or phenyl which is substituted by lower alkyl, lower alkoxy
and/or halogen, or by lower alkoxy, hydroxy, di-lower alkylamino, lower
alkylthio and/or halogen, and/or is N-substituted at a N-atom which is capable
of substitution by lower alkyl, lower alkoxy and/or halogen, and R2 is
hydrogen, hydroxy, amino, lower alkylthio or halogen, and to the salts thereof,
to the preparation of said compounds, to pharmaceutical compositions containing
them, and to the use thereof as medicaments.
[67]
There
follows at page 1 over to the upper third of page 3 a description of some of
the constituents that may be used in creating the compound. This is followed at
page 2 over to the first three lines of page 4 by a discussion of the salts
that can be formed from the compound.
[68]
From
the first full paragraph on page 4 to the first three lines of page 5, there is
a description of the “valuable properties” of the compounds embraced by Formula
I:
The compounds of formula I and salts thereof have
valuable pharmacological properties. In particular, they have a pronounced
regulatory action on the calcium metabolism of warm-blooded animals. Most
particularly, they effect a marked inhibition of bone resorption in rats, as
can be demonstrated in the experimental procedure described in Acta Endrocinol.
78, 613-24 (1975), by means of the PTH-induced increase in the serum
calcium level after subcutaneous administration of doses in the range from
about 0.01 to 1.0 mg/kg, as well as in the TPTX (thyroparathyroidectomised) rat
model by means of hypercalcaemia induced by vitamin D3 after
subcutaneous administration of a dose of about 0.0003 to 1.0 mg. Tumor
calcaemia induced by Walker 256 tumors is likewise inhibited after peroral
administration of about 1.0 to 100 mg/kg. In addition, when administered
subcutaneously in a dosage of about 0.001 to 1.0 mg/kg in the experimental
procedure according to Newbould, Brit. J. Pharmacology 21, 127 (1963),
and according to Kaibara et al., J. Exp. Med. 159 1388-96 (1984), the
compounds of formula I and salts thereof effect a marked inhibition of the
progression of arthritic conditions in rats with adjuvant arthritis. They are
therefore eminently suitable for use as medicaments for the treatment of
diseases which are associated with impairment of calcium metabolism, for
example inflammatory conditions in joints, degenerative processes in articular
cartilage, of osteoporosis, periodontitis, hyperparathyroidism, and of calcium
deposits in blood vessels or prothetic implants. Favourable results are also
achieved in the treatment of diseases in which an abnormal deposit of poorly
soluble calcium salts is observed, as in arthritic diseases, e.g. ancylosing spondilitis,
neuritis, bursitis, periodontitis and tendinitis, fibrodysplasia,
osteoarthrosis or arteriosclerosis, as well as those in which an abnormal
decomposition of hard body tissue is the principal symptom, e.g. hereditary
hypophosphatasia, degenerative states of articular cartilage, osteoporosis of
different provenance, Paget’s disease and osteodystrophia fibrosa, and also
osteolytic conditions induced by tumors.
[69]
From
the first full paragraph at page 5 through to the middle of page 7, a large
number of compounds are identified specifically as being to which the invention
“relates” or “relates more particularly” or “preferably relates” or “relates
firsts and foremost”. Zoledronate is not specifically named, but does fall
within the broad range of the compounds so identified.
[70]
At
the middle of page 7, this paragraph appears:
The invention relates specifically to the compounds
of formula I and the salts thereof, especially the inner salts and
pharmaceutically acceptable salts thereof with bases mentioned in the Examples.
[71]
There
are about thirty two compounds specifically named in Examples 1 to 20 which are
the Examples for the preparation of compounds, omitting repetitions.
Zoledronate, written as:
2-(imidazol-1-yl)-1-hydroxyethane-1,
1 diphosphonic acid
is one of them. It appears in two of the examples;
Example 11 and Example 13:
Example 11: The procedure of
Example 1 is repeated, starting from 1-imidazoleacetic acid hydrochloride,
1-(1H-1,2,4-triazole) acetic acid hydrochloride, 1-pyrazoleacetic acid
hydrochloride, and 3-pyrazoleacetic acid hydrochloride, to give the following
compounds:
2-(imidazol-1-yl)-1-hydroxyethane-1,
1-diphosphonic acid, m.p. 239°C (dec.),
2-(1H-1,2,4-triazol-1-yl)-1-hydroxeyethane-1,
1-disphosphonic acid, m.p. 255°C (dec.),
2-(pyrazol-1-yl)-1-hydroxyethane-1, 1-diphosphonic
acid, m.p. 234°C (dec.), and
2-(pyrazol-3-yl)-1-hydroxyethane-1, 1-disposphonic
acid, m.p.
(Emphasis added)
. . .
Example 13: With stirring and
under reflux, 8.6 g (0.053 mole) of imidazol-1-ylacetic acid hydrochloride, 7.1
ml of 85% phosphoric acid and 25 ml of chlorobenzene are heated to 100°C. Then
13.9 ml of phosphorus trichloride are added dropwise at 100°C, whereupon
evolution of gas occurs. Over the course of 30 minutes a dense mass precipitates
from the reaction mixture. The batch is heated for 3 hours to 100°C and the
supernatant chlorobenzene is removed by decantation. The residual viscous mass
is heated for 3 hours to the boil, with stirring and under reflux, with 40 ml
of 9N hydrochloric acid. The batch is then filtered hot with the addition of
carbon and the filtrate is diluted with acetone, whereupon the crude 2-(imidazol-1-yl)-1-hydroxyethane-1,
1-diphosphonic acid precipitates. This product is recrystallised from
water. Melting point: 239°C (dec.). Yield: 41% of theory.
(Emphasis added)
[72]
Returning
to page 7 and through to the top of page 14, there is a discussion of the
various processes by which the compounds may be produced.
[73]
From
the second paragraph at page 14 to the first paragraph of page 16, there is a
description of the various forms and formulations that a pharmaceutical,
including the compound, may take.
[74]
The
second paragraph at page 16 speaks to the use of the compound:
The present invention also relates to the use of the
compounds of formula I and salts thereof preferably for the treatment of
inflammatory conditions, primarily to diseases associated with impairment of
calcium metabolism, e.g. rheumatic diseases and, in particular, osteoporoses.
[75]
From
the middle of page 16 over to the top of page 17, dosage regimens are
described.
[76]
From
the top third of page 17 to the top of page 24, there are twenty Examples
directed to the preparation of the various compounds, including, as previously
discussed, Examples 11 and 13, which describe the preparation of several
specific compounds, one of which is zoledronate.
[77]
From
pages 24 to 27, Examples 21 to 25 are provided, in which various tablets,
lozenges, capsules and injection liquids are discussed. None of them mention
zoledronate specifically.
[78]
Two
claims follow: claims 1 and 2.
THE
'937 PATENT – CLAIMS 1 & 2
[79]
The
'937 patent contains only two claims – claims 1 and 2 – both of which are at
issue in these proceedings. Those claims read:
a. 2-(imidazol-1-yl)-1-hydroxyethane-1,
1-diphosphonic acid, or a pharmaceutically acceptable salt thereof.
b. A pharmaceutical
composition containing a compound as claimed in claim 1 together with
conventional pharmaceutical excipients.
[80]
Claim
1 relates to a single specific compound:
2-(imidazol-1-yl)-1-hydroxyethane-1, 1-diphosphonic
acid
or a pharmaceutically
acceptable salt of that compound.
[81]
This
formula is yet another way that claimants could write the formula for zoledronate
or zoledronic acid, which was one of the 1.2 million or so compounds falling
within the number of compounds encompassed by claim 14 of the '895 patent as
previously discussed.
[82]
Claim
2 simply claims that this chemical compound is made into a pharmaceutical
composition by mixing it with “conventional pharmaceutical excipients”.
[83]
No
complex construction of claims 1 and 2 is needed. Claim 1 claims a single
compound-zoledronate. Claim 2 is a mixture of zoledronate and pharmaceutical
excipients.
BISPHOSPHONATES
– TECHINICAL BACKGROUND
[84]
Both
Novartis and Teva have provided, through their expert witnesses, as well as the
assistance of Counsel at the hearing, considerable information as to the
technical background respecting bisphosphonates and their use in treating
certain bone diseases.
[85]
Bones
in the human body, as well as in other mammals, are comprised of various
materials; including collagen, calcium, andphosphates. Some of this material
is, in a continuing process, released into the body – a process called bone
resorption – and new material is retrieved from the body. This process
continues during a person’s lifetime and provides for bone growth as well as
repair to cracked and damaged bone material. Due to aging and some diseases,
this process may become unbalanced. In particular, more bone resorption than is
desirable may occur, resulting in conditions such as osteoporosis.
[86]
In
the late 1960’s, researchers, particularly Dr. Fleisch, determined that a class
of compounds known generally as bisphosphonates were useful in controlling the
level of bone resorption. The general structure of a bisphosphonate can be
depicted as follows:
[87]
The
PO3 H2 molecules are the phosphonates; the C in the
middle is sometimes referred to as the geminal carbon a name derived from the
term Gemini (the astrological twins) since there are twin phosphonates
attached. At the positions noted as R1 and R2 a number of
different atoms or molecules may be attached by a “linker” molecule or
molecules.
[88]
One
of the earliest bisphosphonates (or BPs, as they are called in these
proceedings), is one known as etidronate, which had some commercial success. It
can be depicted chemically as:
[89]
Etidronate
had been in existence since the late 1800’s and was used, for instance, to
prevent mineral build-up inside pipes. Its use as a bone resorption inhibitor
was a new use that came about in the late 1960’s and early 1970’s when it was
determined that it would bind to bone mineral surfaces and inhibit bone
resorption.
[90]
Another
early bisphosphonate used to control bone resorption was clodronate. It can be
depicted as :
where each of R1 and R2
is chlorine (Cl).
[91]
Development
of what is known as second generation bisphosphonates followed. Work was done
with respect to the “linkers” between the geminal carbon and the R1
molecule. Up to nine (9) linkers being carbon containing molecules (CH2)
were investigated. In paragraph 67 of his affidavit, Dr. Benedict provides
illustration of such linkers.
[92]
Work
also continued in the selection of suitable candidates for the atoms or
molecules to be placed in the R1 and R2 position. Among
the leading candidates for the R1 position were molecules containing
nitrogen (N), including ring-structured molecules having five or six sides.
[93]
Examples
of rings having five sides (heterocycles), and those that are not, are
illustrated at paragraph 98 of Dr. Benedict’s affidavit.
[94]
Within
the many types of five-sided rings containing nitrogen are those illustrated at
paragraph 44 of Dr. Vepsalainen’s affidavit.
[95]
There
are also a number of corners on the five-sided ring where that ring may be
chemically attached to a “linker” such as CH2. These corners are
given numbers according to chemical convention and where a structure is
identical to another except for the corner at which the five-sided ring
structure is attached to a linker, each structure is called an “isomer” of the
other.
ZOLEDRONATE
[96]
Zoledronate
can be depicted chemically as follows:
[97]
There
is a “geminal” carbon (C) to which are attached two phosphonates (PO3H2).
At the R2 position there is a hydroxyl (OH) attached directly to the
geminal carbon. The heterocylic ring at the R1 position is attached through
a nitrogen atom (N) through one carbon-containing “linker”, CH2. The
heterocyclic ring is of the type known to chemists as an imidazole.
[98]
Zoledronate
has proven to be a very potent bone resorption inhibitor. A dose injected just once
a year has, in many cases, proven to be effective.
[99]
It
is useful, to distinguish between a drug that is “effective” and one that is
“potent”. An “effective” drug is one that produces a desired result. A “potent”
drug is one that is “effective” even at low doses. A determination of “Lowest
Effective Dosage (LED)” of a drug is made by testing. The less of a drug that
is required to achieve a desired effect, the more potent it is.
TESTING
FOR POTENCY
[100]
Scientists
have determined that rats are a good model for determining the effectiveness
and potency of a candidate drug in humans. A common test is that known as TPTX.
In such a test, a group of laboratory rats are selected, their thyroid is
removed, and they are fed various dosages of candidate drugs over a period of
time. At the end, the rats are “sacrificed” and their bones examined. The
results are tabulated. Those candidates requiring the lowest dosages in order
to preserve the bones in a reasonable state are said to be the most potent.
WHAT
DID THE '895 INVENTORS DO?
[101]
Neither
of the two persons named as inventors of the '895 patent gave evidence. One is
dead and the other is, presumably, nearly dead. However, a patent agent
knowledgeable about the files and records kept by the inventors, Dr. Knauer,
did give evidence, including provision of the records made by or under the
direction of, the inventors.
[102] It
appears that, prior to the filing date of the application for the patent in Canada, July 29, 1987, the inventors made the compound that we now call zoledronate. The
compound was made on April 3, 1987. The compound was tested in July 1987, prior
to the Canadian filing date. Further testing was made after that date and,
because of its potency, the drug was selected for further evaluation.
[103] The priority
application was filed in Germany on August 1, 1986. A draft of that
application, dated June 23, 1986, was provided in Dr. Knauer’s second
affidavit. At this time, only one compound that would fall within the scope of
claim 14 had been made and subjected to biological testing. It was not zoledronate.
WHAT DID THE '937
INVENTORS DO?
[104] Dr.
Widler, one of the inventors named in the '937 patent, provided an affidavit
and was cross-examined.
[105] He
testified that, in 1986, he and the other named inventor, Dr. Jaeggi, were
assigned to a project to come up with new bisphosphonates. In
cross-examination, he admitted that he was familiar with patent applications of
others shortly after they became public.
[106] Prior
to the date upon which the application was filed in Canada, November 19, 1987, they
had made zoledronate and tested it using the TPTX model.
[107] The
priority patent application was filed in Switzerland on November 19, 1986. That
application contained claims to the genus of the compounds as well as several
specific compounds. Zoledronate was made and tested in July 1987, which is after
the priority application was filed; but before the Canadian application was
filed. There is a change from the data contained in the priority application to
that found at page 4 of the Canadian patent. This change apparently reflects
testing done respecting certain compounds (not specifically identified) between
the two dates. We do not know if the testing done on zoledronate reflects or
was modified by the results of the testing as reported in the patent, since the
test results on zoledronate are not specifically identified or set out in the '937
patent.
THE CONFLICT - AND
RESULTING CLAIMS
[108] Under
the provisions of the “old” Patent Act, if two or more patent
applications filed before October 1, 1989 in the Canadian Patent Office
appeared to the examiners to claim, or could possibly claim, the same invention,
the Commissioner of Patents could declare that a conflict existed between them.
Section 43 of the “old” Patent Act required that the Commissioner of
Patents request that the parties file affidavit evidence as to the date of
invention. The Commissioner would review that evidence and award claims to one
or other of the parties based on the Commissioner’s determination as to which
inventor was the “first to invent” the particular subject matter of a
particular claim. Often, certain claims were awarded to one party and other
claims to another. The process often took years to resolve. A re-examination by
the Federal Court could follow.
[109] In
the present case, the evidence of Dr. Widler indicates that Ciba-Geigy (now
Novartis) became aware that its application had been placed in conflict with
that of Boehringer. The parties resolved the matter between themselves so that
Boehringer obtained the '895 patent with broad genus claims; the narrowest of
which is the claim at issue, claim 14; while Ciby-Geigy obtained claims
specific to only one compound, zoledronate, in the '937 patent.
[110] Thus,
while in the beginning both applications contained claims to many compounds, by
agreement, the '895 patent retained the broad genus claims, and the '937 patent
retained the claims specific only to zoledronate. In the present case some nine
years passed between the time the patent applications were filed in Canada and the two patents were granted. By that time it would have become apparent that
zoledronate was the compound of commercial interest.
[111] Thus
the parties, together, had the benefit of the '895 patent with its broad
“cascading” claims which, at a minimum, in claim 14, “cascaded” to 1.2 million
compounds while having another patent – the '937 patent – with two claims
directed only to zoledronate, the commercially favoured compound.
[112] Dr.
Robert’s affidavit, paragraph 43, illustrates the benefits of a patent which
“stakes out the ground” to a broad genus of compounds. It may discourage others
from investigation into the genus:
43.
The
medicinal chemist would have been particularly interested in reviewing patents
for molecules in the relevant area for several reasons. First, the patents
would claim compounds thought to be valuable enough to protect. Second, the
patents would identify compounds the medicinal chemist should avoid where the
goal was to find a drug for development. Third, the patents would allow
identification of unpatented molecules that would be expected to have the
requisite activity. The medicinal chemist would have looked for trends or
recurring features to signpost the pathway forward wherever possible.(emphasis
added)
[113] In
the present situation, we have the discouraging patent '895, and the patent
directed to the specific compound, the '937 patent; all as a result of
protracted conflict proceedings.
OBVIOUSNESS
[114]
I
have recently reviewed the law in Canada as to obviousness and set out my views
in Pfizer Canada Inc v Pharmascience Inc, 2013 FC 120. I repeat what I
wrote at paragraphs 186 to 190:
186 The jurisprudence respecting obviousness has
recently been established by the Supreme Court of Canada in Apotex Inc v
Sanofi-Synthelabo Canada Inc, [2008] 3 S.C.R. 265, 2008 SCC 61. Rothstein J wrote
the unanimous reasons of the Court and, in particular, wrote at paragraphs 67
to 71:
67 It will be useful in an obviousness inquiry to
follow the four-step approach first outlined by Oliver L.J. in Windsurfing
International Inc. v. Tabur Marine (Great Britain) Ltd., [1985] R.P.C. 59
(C.A.). This approach should bring better structure to the obviousness inquiry
and more objectivity and clarity to the analysis. The Windsurfing approach was
recently updated by Jacob L.J. in Pozzoli SPA v. BDMO SA, [2007] F.S.R. 37 (p.
872), [2007] EWCA Civ 588, at para. 23:
In the result I would restate the Windsurfing
questions thus:
(1) (a) Identify the notional "person skilled
in the art";
(b) Identify the relevant common general knowledge
of that person;
(2) Identify the inventive concept of the claim in
question or if that cannot readily be done, construe it;
(3) Identify what, if any, differences exist between
the matter cited as forming part of the "state of the art" and the
inventive concept of the claim or the claim as construed;
(4) Viewed without any knowledge of the alleged
invention as claimed, do those differences constitute steps which would have
been obvious to the person skilled in the art or do they require any degree of
invention' [Emphasis added.]
It will be at the fourth step of the
Windsurfing/Pozzoli approach to obviousness that the issue of "obvious to
try" will arise.
i. When Is the "Obvious to Try" Test
Appropriate'
68 In areas of endeavour where advances are often
won by experimentation, an "obvious to try" test might be
appropriate. In such areas, there may be numerous interrelated variables with
which to experiment. For example, some inventions in the pharmaceutical
industry might warrant an "obvious [page294] to try" test since there
may be many chemically similar structures that can elicit different biological
responses and offer the potential for significant therapeutic advances.
ii. "Obvious to Try" Considerations
69 If an "obvious to try" test is
warranted, the following factors should be taken into consideration at the
fourth step of the obviousness inquiry. As with anticipation, this list is not
exhaustive. The factors will apply in accordance with the evidence in each case.
1. Is it more or less self-evident that what is
being tried ought to work' Are there a finite number of identified predictable
solutions known to persons skilled in the art'
2. What is the extent, nature and amount of effort
required to achieve the invention' Are routine trials carried out or is the
experimentation prolonged and arduous, such that the trials would not be
considered routine'
3. Is there a motive provided in the prior art to
find the solution the patent addresses'
70 Another important factor may arise from
considering the actual course of conduct which culminated in the making of the
invention. It is true that obviousness is largely concerned with how a skilled
worker would have acted in the light of the prior art. But this is no reason to
exclude evidence of the history of the invention, particularly where the
knowledge of those involved in finding the invention is no lower than what
would be expected of the skilled person.
71 For example, if the inventor and his or her team
reached the invention quickly, easily, directly and relatively inexpensively,
in light of the prior art and common general knowledge, that may be evidence
supporting a finding of obviousness, unless [page295] the level at which they
worked and their knowledge base was above what should be attributed to the
skilled person. Their course of conduct would suggest that a skilled person,
using his/her common general knowledge and the prior art, would have acted
similarly and come up with the same result. On the other hand, if time, money
and effort was expended in research looking for the result the invention
ultimately provided before the inventor turned or was instructed to turn to
search for the invention, including what turned out to be fruitless "wild
goose chases", that evidence may support a finding of non-obviousness. It
would suggest that the skilled person, using his/her common general knowledge
and the prior art, would have done no better. Indeed, where those involved
including the inventor and his or her team were highly skilled in the
particular technology involved, the evidence may suggest that the skilled
person would have done a lot worse and would not likely have managed to find
the invention. It would not have been obvious to him/her to try the course that
led to the invention.
187 This test was amplified by the Federal Court
of Appeal in Apotex Inc v Pfizer Canada Inc, 2009 FCA 8, where Noel JA, for the
Court, distinguished between mere possibilities and speculation, which is not
the test; and more or less self-evident, which is the test. He wrote at
paragraphs 28 to 30:
28 I take it from this that the test adopted by the
Supreme Court is not the test loosely referred to as [page235] "worth a
try". After having noted Apotex' argument that the "worth a try"
test should be accepted (at paragraph 55), Rothstein J. never again uses the
expression "worth a try" and the error which he identifies in the
matter before him is the failure to apply the "obvious to try" test
(at paragraph 82).
29 The test recognized is "obvious to try"
where the word "obvious" means "very plain". According to
this test, an invention is not made obvious because the prior art would have
alerted the person skilled in the art to the possibility that something might be
worth trying. The invention must be more or less self-evident. The issue which
must be decided in this appeal is whether the Federal Court Judge failed to
apply this test.
30 In my respectful view, he did not. While the
Federal Court Judge does not use the phrase "obvious to try", his
reasons show that he conducted his analysis along the dividing line drawn in
Sanofi-Synthelabo. Specifically, he rejected the contention that the invention
was obvious based on mere possibilities or speculation and looked for evidence
that the invention was more or less self-evident.
188 The test adopted by the Supreme Court of Canada is based on two United Kingdom decisions and is often referred to as the Windsurfing/Pozzoli
test. This test was recently considered by the United Kingdom Court of Appeal
(Civil Division) in MedImmune Limited v Novartis Pharmaceuticals UK Limited,
[2012] EWCA Civ 1234. Lord Justice Kitchin wrote at paragraphs 85 to 90:
[85] It is often convenient, but by no means
essential, to consider an allegation of obviousness using the structured
approach explained by this court in Pozzoli v BDMO SA [2007] EWCA Civ 588,
[2007] Bus LR D117, [2007] FSR 37 at 23:
‘(1) (a) Identify the notional 'person skilled
in the art';
(b) Identify the relevant common general
knowledge of that person;
(2) Identify the inventive concept of the claim in
question or if that cannot readily be done, construe it;
(3) Identify what, if any, differences exist between
the matter cited as forming part of the 'state of the art' and the inventive
concept of the claim or the claim as construed;
(4) Viewed without any knowledge of the alleged
invention as claimed, do those differences constitute steps which would have
been obvious to the person skilled in the art or do they require any degree of
invention''
[86] Step (2) may pose some problems. In some cases,
as in this one, the parties agree what the inventive concept is. This has the
advantage of limiting the obviousness analysis to the essence of the invention.
But often the parties do not agree and in such cases it will usually be a
futile exercise for the court to seek to resolve their disagreement, for
ultimately all that matters is what the patentee has claimed. As Lord Hoffmann
said in Conor v Angiotech [2008] UKHL 49, [2008] 4 All ER 621, [2008] RPC 716
at 19 '... the patentee is entitled to have the question of obviousness
determined by reference to the claim and not to some vague paraphrase based
upon the extent of his disclosure in the description'.
[87] I would add, so too is the Defendant. The
patentee may have drawn his claim so broadly that it includes products or
processes that owe nothing to the inventive contribution he has made, rendering
the claim particularly vulnerable to an allegation of obviousness.
[88] Step (3) presents little conceptual difficulty.
It simply requires the court to identify the differences between the prior art
and the claim.
[89] It is step (4) which is key and requires the
court to consider whether the claimed invention was obvious to the skilled but
unimaginative addressee at the priority date. He is equipped with the common
general knowledge; he is deemed to have read or listened to the prior
disclosure properly and in that sense with interest; he has the prejudices,
preferences and attitudes of those in the field; and he has no knowledge of the
invention.
[90] One of the matters which it may be appropriate
to take into account is whether it was obvious to try a particular route to an
improved product or process. There may be no certainty of success but the skilled
person might nevertheless assess the prospects of success as being sufficient
to warrant a trial. In some circumstances this may be sufficient to render an
invention obvious. On the other hand, there are areas of technology such as
pharmaceuticals and biotechnology which are heavily dependent on research, and
where workers are faced with many possible avenues to explore but have little
idea if any one of them will prove fruitful. Nevertheless they do pursue them
in the hope that they will find new and useful products. They plainly would not
carry out this work if the prospects of success were so low as not to make them
worthwhile. But denial of patent protection in all such cases would act as a
significant deterrent to research.
189 Lord Justice Lewiston agreed and added at
paragraph 184:
[184] In many 'obvious to try' cases, it is the idea
of trying that constitutes the inventive step. It was no doubt this that led
Sir Donald Nicholls V-C to say in Molnlycke AB v Procter & Gamble Ltd
[1994] RPC 49 that '... obviousness connotes something which would at once
occur to a person skilled in the art who was desirous of accomplishing the
end'. (Emphasis added)
190 Lord Justice Moore-Bick agreed with both.
[115] I
have already identified the notional person skilled in the art, which is step
1(a) in the Sanofi test. Step 1(b) requires that the relevant common
general knowledge be identified; however, that must be identified as of the
date of the invention. Given that both patents at issue are “old” Patent Act
patents, the common general knowledge must be ascertained as of the “date of
the invention”. In turn, such an inquiry must begin with “what is the
invention”. Step 2 of the Sanofi test requires identification of the “inventive
concept” of the claim in question. Thus, I will begin with the “inventive
concept” of claim 14 of the '895 patent.
[116] Justice
Near (as he then was) summarized the law in this respect quite well in his
decision AstraZeneca Canada Inc v Teva Canada Limited, 2013 FC 245, at
paragraph 13:
[13] Despite AstraZeneca’s protestations, this
is not always the end of the analysis (see Apotex Inc v Sanofi-Synthelabo
Canada Inc, 2008 SCC 61, [2008] SCJ No 63 [Sanofi] at para 77). Where, as in
this case, the inventive concept of the claims is not discernible from the
claims themselves because they present a bare chemical formula, the Court is
directed to read the specification in the patent to determine the inventive
concept of the claims (Sanofi, above, at para 77; Servier, above, at para 58; Teva
Canada Ltd v Pfizer Canada Inc, 2012 SCC 60, [2012] SCJ No 60 [Teva v Pfizer]
at para 50). The Supreme Court and the Federal Court of Appeal both recently
reiterated the principle that “the entire specification, including the claims,
must be considered in determining the nature of the invention” (Teva v Pfizer,
above, at para 50; Allergan Inc v Canada (Minister of Health), 2012 FCA 308,
[2012] FCJ No 1467 at para 73). However, this does not give the Court free
rein to construe the claims as broadly or as narrowly as it wishes. The
patentee is “entitled to have the question of obviousness determined by
reference to his claim and not to some vague paraphrase based upon the extent
of his disclosure in the description” (Servier, above, at para 69; Angiotech
Pharmaceuticals Inc v Conor Medsystems Inc, [2008] UKHL 49 at para 19).
THE '895 PATENT
- THE INVENTIVE CONCEPT
[117] Claim
14 of the '895 patent claims some 1.2 million compounds, all having a
bisphosphonate backbone; with several choices for one group of compounds
directly linked to the geminal carbon, and with several choices for another
group of compounds, all linked with a single carbon-containing linker such as
CH2 to the geminal carbon.
[118] The
invention is described at pages 1 and 2 of the '895 patent, which I repeat in
part:
The present invention is
concerned with new diphosphonic acid derivatives, processes for the preparation
thereof and pharmaceutical compositions containing them.
.
. .
We have found that analogue
derivatives of these compounds in which there is only one carbon atom between
the diphosphonate residue and the heterocyclic radical and the heterocycle is
not a pyrazole ring also display these actions and, in addition, as good
calcium complex formers, are suitable for the wider treatment of calcium
metabolism disturbances. In particular, they can be very well used in cases in
which the bone formation and breakdown is disturbed.
[119] I
accept, with one caveat, the description of the inventive concept articulated
by the Applicant at paragraph 143 of its Memorandum; that caveat is that the
“family” of compounds is about 1.2 million members:
182. The inventive concept of claim 14 is a family
of (about 1.2 million members) novel compounds containing a 5-membered ring,
which is connected to the geminal BP carbon by a one-carbon linker (―CH2―).
These BP’s have biological activity as calcium complex formers and inhibit bone
resorption.
THE '937 PATENT – THE INVENTIVE
CONCEPT
[120] Claims
1 and 2 of the '937 patent are directed to one compound only, zoledronate, or
zoledronate mixed with pharmaceutical excipients.
[121] The
invention is diffusely described in the patent. I repeat part of page 1:
The present invention relates to novel substituted
alkanediphosphonic acids, in particular to heteroarylalkanediphosphonic acids
of formula
Wherein R1(a number of compounds) and R2
is (a number of atoms or compounds)
[122]
At
page 4, the description states, in part:
The compounds of
formula I and salts thereof have valuable pharmacological properties. In
particular, they have a pronounced regulatory action on the calcium metabolism
of warm-blooded animals. Most particularly, they effect a marked inhibition of
bone resorption in rats, as can be demonstrated…
[123] The
description continues by describing a number of compounds as being preferred,
most preferred, and first and foremost and concluding with a statement at page
7 that the invention relates specifically to some 32 compounds found in the
Examples. Zoledronate is one of them, but is not specifically mentioned in this
description:
The invention relates specifically to the compounds
of formula I and the salts thereof, especially the inner salts and
pharmaceutically acceptable salts thereof with bases mentioned in the Examples.
[124] The
patent ends with two claims. Claim 1 is specific to zoledronate; claim 2 is
directed to zoledronate, plus pharmaceutical excipients.
[125] I
disagree with the description of the inventive concept as set out at paragraph
87 of the Applicant’s Memorandum:
87. The inventive concept of the claims of the
'937 Patent is that zoledronate is a novel compound that is an exceptionally
potent inhibitor of bone resorption in rats.
[126] My
disagreement is that there is nothing in the claims, or in the description, to
indicate that zoledronate is an “exceptionally potent inhibitor”. It can be
deduced from what is set out at page 4 of the patent that zoledronate is among
the many compounds described that has certain potency. We do not know if it is
the greatest or least or somewhere in between those encompassed by the
description.
[127] At
this point, the decision of the Supreme Court of Canada in Teva Canada
Limited v Pfizer Canada Inc, 2012 SCC 60, must be considered. That decision
was concerned with whether the patent met the disclosure requirements of the Patent
Act. The Supreme Court began by reaffirming the “bargain” theory of the
patent system. LeBel J, for the Court, wrote at paragraph 32:
32 The patent system is based on a
"bargain", or quid pro quo: the inventor is granted exclusive rights
in a new and useful invention for a limited period in exchange for disclosure
of the invention so that society can benefit from this knowledge. This is the
basic policy rationale underlying the Act. The patent bargain encourages
innovation and advances science and technology. Binnie J. explained the quid
pro quo as follows in AZT, at para. 37:
A patent, as has been said many times, is not
intended as an accolade or civic award for ingenuity. It is a method by which
inventive solutions to practical problems are coaxed into the public domain by
the promise of a limited monopoly for a limited time. Disclosure is the quid
pro quo for valuable proprietary rights to exclusivity which are entirely the
statutory creature of the Patent Act.
[128] Respecting
adequate disclosure, he wrote at paragraph 34:
34 Therefore, adequate disclosure in the
specification is a precondition for the granting of a patent. As Hughes J.
stated in Eli Lilly Canada Inc. v. Apotex Inc., 2008 FC 142, 63 C.P.R. (4th)
406, at para. 74:
Thus, one must both advance the state of the
art and disclose that advance in order to gain the patent monopoly. Failing to
do so, thus invalidating the monopoly, can be in the form of one or more of
several matters such as, the "invention" was not new, or the
so-called invention was "obvious" or the disclosure was
"insufficient" or "what you disclosed doesn't support the
monopoly that you claim".
[129] Concerning
disclosure, the Court reviewed prior jurisprudence and concluded by affirming
its previous decisions in Consolboard ([1981] 1 S.C.R. 504) and Pioneer
Hi-Bred ([1989] 1 S.C.R. 1623) at paragraphs 51 and 52:
51 In Pioneer Hi-Bred, the Court referred to
Consolboard in discussing the Act's disclosure requirements once again. Lamer
J. (as he then was), writing for the Court, described those requirements as
follows:
In summary, the Patent Act requires that the
applicant file a specification including disclosure and claims (Consolboard
Inc., supra, at p. 520). Canadian courts have stated in a number of cases the
test to be applied in determining whether disclosure is complete. The applicant
must disclose everything that is essential for the invention to function
properly. To be complete, it must meet two conditions: it must describe the
invention and define the way it is produced or built ... . The applicant must
define the nature of the invention and describe how it is put into operation. A
failure to meet the first condition would invalidate the application for
ambiguity, while a failure to meet the second invalidates it for insufficiency.
The description must be such as to enable a person skilled in the art or the
field of the invention to produce it using only the instructions contained in
the disclosure ... and once the monopoly period is over, to use the invention
as successfully as the inventor could at the time of his application (Minerals
Separation, supra, at p. 316). [Emphasis added; citations omitted; pp.
1637-38.]
52 In Consolboard and in Pioneer Hi-Bred, the
Court correctly analysed the disclosure requirements set out in s. 27(3) of the
Act. The reasoning in those cases should be reaffirmed and applied in the case
at bar.
[130] The
Court then addressed the particular patent at issue by defining the nature of
the invention. This is the same exercise that I am doing now. LeBel J wrote at
paragraph 53:
53 In determining whether the disclosure
requirements have been met in this case, the first step is to define the nature
of the invention in Patent '446. This must be done in order to comply with s.
27(3) of the Act, which requires, among other things, that the specification
"correctly and fully describe the invention". Therefore, we must ask:
What is the invention in Patent '446?
[131] The
patent under consideration by the Supreme Court contained a number of claims in
what that Court described at paragraph 80 as “cascading” claims. It began with
Claim 1, which at paragraph 73 the Court said involved over 260 quintillion
claims, with claims 2 to 5 directed to progressively smaller groups. Claims 6
and 7 each related to only one compound. The Court held, at paragraph 75, that
a “minor research project” would have to be conducted to determine whether
claim 6 or claim 7 contained the correct (i.e. commercial) compound. In fact,
claim 7 was directed to the compound known as sildenafil, the active ingredient
in the drug sold under the name Viagra.
[132] As
discussed by LeBel J at paragraph 56, it was argued by the patentee Pfizer that,
so long as there was one claim specific to the compound at interest, there was
adequate disclosure of the invention; regardless as to whether there were other
specific or other general claims. At paragraphs 57 to 63 of LeBel J’s Reasons,
he reviewed previous jurisprudence and rejected any broad conclusion that could
have been drawn from the previous jurisprudence as might have supported
Pfizer’s submissions.
[133] At
paragraph 64, LeBel J adopted a “case-by-case basis” for considering the
disclosure of a patent, and the invention was so disclosed:
64 It is possible, as in Boehringer, for each
claim in a patent to disclose a separate invention. Where this issue is raised,
however, individual patents must be considered on a case-by-case basis. In my
view, the approach Teva advocates for at para. 119 of its factum is useful in
this case: "... the specification as a whole must be examined to determine
whether sildenafil and the other compounds claimed in the patent are linked so
as to form a single general inventive concept". This is consistent with
this Court's comment in Consolboard, at p. 520: "We must look to the whole
of the disclosure and the claims to ascertain the nature of the invention and
methods of its performance ... ."
[134] At
paragraphs 66 and 67, the patent under consideration by the Supreme Court is
seen to be very similar to the '937 patent:
66 In this case, if we consider the
specification as a whole, there is nothing to support the view that the use of
sildenafil for the treatment of ED is a separate invention from the use of any
of the other claimed compounds for that same purpose. No specific attributes or
characteristics are ascribed to sildenafil that would set it apart from the
other compounds. Even if we take into consideration the fact that sildenafil is
an "especially preferred compound", there is still nothing that
distinguishes it from the other eight "especially preferred
compounds". The use of sildenafil and the other compounds for the
treatment of ED comprises one inventive concept.
67 In fact, the patent itself suggests that the
entire class of claimed compounds will be effective in treating ED. The first
sentence of the specification states: "This invention relates to the use
of a series of [compounds] for the treatment of impotence" (A.R. vol. X,
at p. 164 (emphasis added)). The following appears on the second page of the
specification: "Unexpectedly, it has now been found that these disclosed
compounds are useful in the treatment of erectile dysfunction." And page
11 of the specification contains this statement:
Thus the invention includes a pharmaceutical
composition for the curative or prophylactic treatment of erectile dysfunction
in a male animal, including man, comprising a compound of formula (I), or a
pharmaceutically acceptable salt thereof, together with a pharmaceutically
acceptable diluents, or carrier. [Emphasis added; A.R., vol. X, at p. 174.]
The plural word "inventions" does not
appear in Patent '446.
[135] Then
the Supreme Court considers a situation, apparently put to it by Counsel, that
a “divisional” patent could have been filed wherein the description would have
been the same, but the claims restricted to one compound only; presumably
sildenafil. At paragraph 68, LeBel J wrote:
68 There is no evidence on the record to suggest
that Pfizer filed a divisional application under s. 36(2.1). It would be
disingenuous for Pfizer to imply that there is one invention in the patent
application for the purpose of complying with s. 36(1) and then to submit that
each claim concerns a distinct invention for the purposes of this appeal. If
Patent '446 is viewed as a whole, there is only one invention: the use of the
compound or compounds that are effective in treating ED.
[136] The
problem with the patent before the Court, as stated in paragraph 80 of LeBel
J’s Reasons, was not that there were cascading claims - presumably overly broad
- but that the patent claimed in two separate claims two compounds without
making it clear which compound was the truly useful one.
80 I would not make too much of the fact that
Claim 1 included over 260 quintillion compounds. The practice of cascading
claims -- although it may, as in this case, result in claims that are overly
broad -- is a common one that does not necessarily interfere in every case with
the public's right to disclosure. The skilled reader knows that, when a patent
contains cascading claims, the useful claim will usually be the one at the end
concerning an individual compound. The compounds that do not work are simply
deemed invalid. In accordance with s. 58, any valid claim -- in this case,
Claim 7 -- survives despite the existence of invalid claims. However, the
public's right to proper disclosure was denied in this case, since the claims
ended with two individually claimed compounds, thereby obscuring the true
invention. The disclosure failed to state in clear terms what the invention
was. Pfizer gained a benefit from the Act -- exclusive monopoly rights -- while
withholding disclosure in spite of its disclosure obligations under the Act. As
a matter of policy and sound statutory interpretation, patentees cannot be
allowed to "game" the system in this way. This, in my view, is the
key issue in this appeal. It must be resolved against Pfizer.
[137] In
the present case, the '937 patent contains only two claims directed to one
compound only, zoledronate. In effect, it is a “divisional” in that claims to any
other compound have been removed.
[138] I
find that, unlike the '895 patent, the '937 patent, because it claims only one
compound, zoledronate, is, on a case-by-case basis, distinguishable from that
considered by the Supreme Court in Teva. I find that the inventive
concept of the '937 patent is that zoledronate is a useful inhibitor of bone
resorption in rats and that, as such, is suitable for use as a medicament in
the treatment of diseases in humans associated with impairment of calcium
metabolism.
DATE OF THE INVENTION
- '895 PATENT
[139] As I
have found, the inventive concept of the '895 patent, as expressed in claim 14,
is that there is a family of about 1.2 million members of compounds that have
biological activity as calcium complex formers, and without bone resorption.
[140] As
discussed under the caption “What did the '895 inventors do?” those inventors
made and tested two compounds, only one of which falls within the parameters of
claim 14 (and is not zoledronate) before the filing of the priority German
application on August 1, 1986. A draft application dated June 23, 1986 is the
first document to postulate that a “class”, however broad, of compounds may be
useful in testing bone disease. There is no support for leaping from one or two
compounds to a class of 1.2 million compounds.
[141] In
this regard, I note the evidence of the Applicant’s expert, Dr. Ebetino who, in
the summary of his opinions, states at paragraphs 23 and 24:
23. By 1987, there was an appreciation that
BPs had a physical chemical and a biochemical or cellular effect that
contributed to their ability to inhibit bone resorption. However, the
biochemical/cellular mechanism of action was unknown. Therefore, there was no
ability to predict the potency of a BP based on structure activity relationships.
24. As taught to skilled persons by the
pioneering researcher in the BP field (Dr. Fleisch) in 1985, it was dangerous
to make assumptions about the activity of any new BPs based upon what was known
about previous BPs. Each BP needed to be assessed on its own and had to be
synthesized and tested in a biological model in order to assess its potency.
[142] Therefore,
the “date of invention” can be no earlier than the date of the draft of the
priority application, June 23, 1986, wherein a “class” was articulated. I do
not, at this point, go into whether such articulation was sound or sufficient.
DATE
OF INVENTION – THE '937 PATENT
[143]
As
I have found, the inventive concept of the '937 patent is that zoledronate is a
useful inhibitor of bone resorption in rats and that, as such, is suitable for
use as a medicament in the treatment of diseases in humans associated with
impairment of calcium metabolism.
[144] As
discussed under the caption “What did the '937 inventors do?” the inventors
made and tested zoledronate in rats in July 1987, which is after the filing of
the priority application, but before the filing of the Canadian application. I
find that the date of invention of the inventive concept of the '937 patent is
July 1987.
[145] I
have not chosen the priority filing date of the '937 patent, which is the
filing date of the Swiss application, November 21, 1986, since there is no
evidence that the inventors had made or tested zoledronate as of that date; nor
is there any evidence that they could have, as of the priority date, soundly
predicted that zoledronate would be the compound of choice.
WHAT WAS THE
“COMMON GENERAL KNOWLEDGE” AND “STATE OF THE ART”
[146] The
Supreme Court of Canada in Sanofi, at paragraph 67, adopted the approach
of the United Kingdom Courts in Windsurfing, as restated in Pozzoli.
I have set out this paragraph earlier in these Reasons. In step 1(b), the Court
is asked to identify the relevant “common general knowledge” and in step 3, the
Court is asked to identify the differences between the inventive concept and the
“state of the art”. Presumably, the state of the art may include knowledge that
is not common or generally known.
[147] In
the present case, we are to consider the common general knowledge or state of
the art as of two different dates; for the '895 patent, it is June 23, 1986;
whereas, for the '937 patent, it is July 1987. Fortunately, the evidence in the
record provides only one significant event between those dates – the
publication of what is referred to as the '057 patent application published on
November 12, 1986.
[148] Dr.
Roberts, an expert witness for Teva, summarized his conclusions as to trends in
the art as of July 1986 at paragraphs 151 to 156 of his affidavit:
CONCLUSIONS/TRENDS AS OF JULY 1986
151.
Based
on the prior art, the skilled person would have known that bisphosphonate
compounds inhibited bone resorption and were known to be effective in treating
bone disorders.
152.
The
known bisphosphonate compounds all shared the same bisphosphonate structure
with substituents attached to the geminal carbon at the R and R1
positions.
153.
The
substituent at the R-position that maintained or often improved activity was
the hydroxyl group.
154.
Compounds
whole R1 substituent contained at least one nitrogen atom tended to
have greater activity that compounds that did not.
155.
The
state of the art revealed that hydroxybisphosphonates containing 5-and
6-membered heterocyclic substituents at the R1 position, connected
by an alkyl chain (1 to 8 carbons in the case of 6-membered heterocyclic rings,
2 to 8 in the case of 5-membered nitrogen heterocyclic rings excluding
substituted pyrazoles; and 1 to 8 in the case of substituted pyrazoles and
5-membered heterocyclic rings more generally) resulted in molecules active in
inhibiting bone resorption.
156.
One
5-membered, nitrogen-containing heterocycle in particular, imidazole, was known
to have an effect on bone resorption when substituted at the 1-position. A
suggested mechanism of action ws through thromboxane synthetase inhibition.
Imidazole had been used as a substituent at the R1 position in a
bisphosphonate compound for use in treating a variety of disorders relating to
calcium metabolism or abnormal bone resorption including diseases of the
skeletal system such as osteoporosis, Paget’s disease, Bechterew’s disease and
also treatment of bone metastases, urolithiasis, prevention of heterotopic
ossification, rheumatoid arthritis and osteoarthritis.
[149] Dr.
Roberts offered his opinion as to the '057 patent application published in
November 1986. I set out paragraphs 172 to 175 of his affidavit, which gives
the flavour as to how he tests that application. He acknowledges that the '057
application offers many choices, but he is of the opinion that, given those
choices, a person skilled in the art, at every juncture where a choice is to be
made, makes a choice that he considers to be obvious. I am sceptical about such
logic; it depends rather much on hindsight, knowing the result to be achieved.
He says:
172.
The
skilled person would have applied the well known bisphosphonate chemistry to
furnish the product with imidazole attached to the bisphosphonate moiety
through a single carbon atom. The methyl bisphosphonate could, theoretically be
attached at 1 of 3 possible positions on the imidazole ring. The chemistry to
make all three compounds was well-established and extremely simple.
Accordingly, the skilled medicinal chemist would likely have made all three of
these obvious variations.
173.
If
the skilled person were to select one, however, in my view, it would have been
the one with the imidazole attached at the 1 position (through the nitrogen).
This is because the literature indicated that an imidazole substituted at the
1-position (at the nitrogen) inhibited bone resorption.
174.
Following
the 057 Application literally, the skilled person is taught to react imidazole
with EHDP as opposed to applying the well-known bisphosphonate synthesis. The
skilled person was well aware that these two compounds do not naturally react
with each other to form a covalent bond, as was the concept of the 057
Application, but can easily be made to do so. In this case, the skilled person
would have made the compound linking imidazole to EHDP at the 1 position first,
if not exclusively.
175.
The
easiest reaction is (and would have been) to activate the methyl group of
etidronate and react it with the imidazole using the nitrogen atom of the
imidazole. This would have resulted in an attachment at the 1-position (in
other words, at the nitrogen atom). The attachment at position 1 is the
molecule now known as zoledronic acid.
[150] Dr.
Roberts concludes, at paragraphs 249 to 252 of his affidavit, that the
inventive concepts of each of the '895 patent and '937 patent would have been
immediately apparent:
J. WERE
THE INVENTIVE CONCEPTS OF THE PATENTS IMMEDIATELY APPARENT?
(a) 895
Patent
249.
To
the skilled person, it would have been obvious that a hydroxybisphosphonate
attached to a 5-membered heterocycle, particularly one containing nitrogen,
by a one- carbon link would have bone resorption inhibition
activity. The alleged invention of the one carbon bridge between the geminal
carbon and the heterocyclic substituent is uninventive and obvious.
250.
Accordingly,
in my opinion, the asserted claims of the 895 Patent were immediately
apparent and obvious by the invention date (even assuming it found
by the Court to be as early as April 1986) based on the prior art as
described above.
(b) 937 Patent
251.
In
y opinion, claims 1 and 2 of the 937 Patent were obvious as at November 1986,
based on the prior art as described above.
252.
All
of the teachings leading to the 895 Patent had advanced even further by
November of 1986. In particular, the 057 Application specifically
and expressly taught that combining known bisphosphonates, such as what is
now known as EHDP with an imidazole (the simplest one of which is imidazole
itself) would result in a compound useful for treating diseases of bone
metabolism. Since imidazole was the simplest compound, this would be the
imidazole compound to have been used first. Linking EHDP with imidazole
in the manner set out in the 057 Application, using the simplest and
most obvious chemistry, would have yielded zoledronic acid, and nothing
else.
[151] Dr.
Vepsalainen, another of Teva’s experts, reaches similar conclusions at
paragraphs 15 to 17 of his affidavit:
IV. SUMMARY OF MY OPINION
895 Patent
15. For the reasons set out below, in my
opinion, claims 1-3, 6-8, 10, 12, 14, 19 and 21-25 of the 895 Patent claim
subject matter that would have been obvious to the skilled person. The
hydroxybisphonate compounds with nitrogen-containing heteroaromatic ring
attachments claimed in the 895 Patent were, in material respects, almost
identical to many of the prior art compounds. By July 29, 1986, and even
earlier, the prior art had claimed that virtually all hydroxybisphosphonate,
with aromatic and heteroaromatic rings substituents in the R1
position, were active in treating calcium metabolism disturbances and other
bone disease, whether the rings were attached to the central carbon by a
1-carbon or an 8-carbon bridge. The prior art made clear that a nitrogen in the
R1 position conferred additional activity.
16. Even the narrowest claim of the 895 Patent
claimed hydroxybisphosphonates with heteroaromatic nitrogen-containing rings
attached to the central carbon by a 1-carbon bridge. There was nothing new or
surprising about the fact that these compounds were said to have activity in
treating calcium metabolism disturbances and other bone disease.
937 Patent
17. Likewise, for the reasons I set out below,
in my opinion, claims 1 and 2 of the 937 patent, claiming zoledronic acid, a
hydroxybisphosphonate with an imidazole substituent attached to a 1-carbon
bridge at the 1-position, would have been obvious to the skilled person. By
November 21, 1986, and even earlier, there was substantial prior art teaching
that hydroxybisphonates with nitrogen-containing heteroaromatic rings,
including imidazole, had activity in treating calcium metabolism disturbances
and other bone disease.
[152] Not
surprisingly, the Applicant’s experts are of a different opinion. Dr. Ebetino
summarizes his opinions at paragraphs 22 to 26 of his affidavit:
D. SUMMARY OF
OPINIONS
22. The prior
art and common general knowledge available to the uninventive but nonetheless
skilled person in the BP field as of mid 1987 provided no clear trends or any
logical guidance in the design of potent BPs. The prior art was contradictory
and pointed in different research starting points and directions.
23. By 1987, there was an appreciation that
BPs had a physical chemical and a biochemical or cellular effect that
contributed to their ability to inhibit bone resorption. However, the
biochemical/cellular mechanism of action was unknown. Therefore, there was no
ability to predict the potency of a BP based on structure activity relationships.
24. As taught to skilled persons by the
pioneering researcher in the BP field (Dr. Fleisch) in 1985, it was dangerous
to make assumptions about the activity of any new BPs based upon what was known
about previous BPs. Each BP needed to be assessed on its own and had to be
synthesized and tested in a biological model in order to assess its potency.
25. The amount of time and effort required to
synthesize and test new BPs was extensive. It is not the case that BP chemistry
was routine or easy. The researchers developing new BPs were often faced with
challenges not faced by researchers in other fields of medicinal chemistry.
26. It would not have been self-evident or
plain to the skilled person to attempt to make a compound possessing the
structure of zoledronate based on the prior art and common general knowledge.
Even if an attempt to make zoledronate was worth a try, there was nothing in
the art or common general knowledge which made it self-evident or very plain to
the skilled person that it would be more potent than earlier disclosed BPs.
Potency could only be learned upon making and testing the compound.
[153] Dr.
Benedict was asked for his opinions only as to the '895 patent. He states at
paragraphs 126 to 131 of his affidavit:
The Inventive Concept of Claim 14 Was Not More or
Less Self-Evident
126. The differences that exist between the
state of the art compounds and the class of inventive compounds disclosed in
claim 14 are significant since one could not predict the activity of this class
of compounds based on the activity of the prior art compounds until a member of
the class of claim 14 had been synthesized and tested. As I described above,
there could be profound differences in the potency of bisphosphonates that
resulted from seemingly small changes to their structures. Estimating the
activity of bisphosphonates based upon their structure was simply not possible
before the synthesis and biological testing of the compound.
127. Further, there was very little data
available in the published literature and patents regarding the antiresorptive
activity of different bisphosphonates. This was especially the case for bisphosphonates
containing rings linked to the geminal carbon. As I will discuss below in my
comments regarding the affidavit of Dr. Vepsalainen, the only document (U.S. Patent 4,416,877) that he cites that discloses any antiresorptive activity data for
bisphosphonates bearing rings shows that these compounds were marginally active
at best. Further, Dr. Roberts apparently did not locate this document in his
search and did not consider it to be a part of the relevant prior art.
128. The lack of data regarding the antiresorptive
activity of bisphosphonates was further complicated by the fact that there are
two different mechanisms at play that influence bisphosphonates’ effects on
bone metabolism: the physical-chemical effect and the cellular or biological
effect. As I discussed above (beginning at paragraph 58), researchers were
considering two main routes to increase the therapeutic index of bisphosphonates:
(1) reducing their binding affinity to hydroxyapatite by modifying R1
and (2) increasing the antiresorptive potency by modifying R2.
129. However, the skilled person did not know
the reason why the bisphosphonates inhibited bone resorption. While a
biological (as opposed to a physical-chemical) mechanism had been postulated,
the specific target (e.g. an enzyme) was not identified until the 1990’s. Thus,
one could not propose changes to the structure of the bisphosphonates based on
characteristics of the target. In addition, unlike today, where the medicinal
chemist has access to sophisticated computational molecular modelling programs,
we did not have that type of technology to assist us in our development of
novel bisphosphonates.
130. As I describe in Part V of my affidavit
(“Scientific Background”), there were many possible directions that a person
skilled in the art could take in trying to develop novel bisphosphonates.
Further, even once a particular direction was chosen, due to the very limited
knowledge of structure-activity relationships, there was very little guidance
at that point. An expression that we used at Procter & Gamble was that we
had to “kiss a lot of frogs” before potent new bisphosphonate was found.
131. Thus, in my opinion, it was not more or
less self-evident that the inventive concept of claim 14 ought to work. As I
mentioned above, one could not predict the activity of a particular class of
bisphosphonates before synthesizing and testing a member of the class.
[154] Having
read the evidence of all the expert witnesses, both in their affidavits and in
cross-examination, I am left with the view that, even given a broad number of
choices for atoms or molecules or compounds that could be attached, even using
one carbon linker, to the geminal carbon backbone of a bisphosphonate, there is
still too much uncertainty as to whether any particular combination will be
useful. As an example, I quote paragraph 109 of Dr. Grynpas’ (Teva’s expert)
affidavit:
109. The Boehringer Patent claims a wide range
of compounds for a broad range of uses. The Boehringer Patent’s specification
only provides data for two of the claimed compounds. These data show that these
two similar compounds have at least a 10-fold difference in potency. Again,
with only two compounds tested, the skilled person would not have known if the
range covered by these two tested compounds represented the whole range, or the
top or bottom of the range. It is therefore not possible for the skilled person
to evaluate the potency of any of the other claimed compounds. Furthermore,
based on the information in the specification, that person would not be able to
draw any conclusions with respect to the potential utility of each of these
claimed compounds for the treatment of the claimed uses.
[155] Dr.
Benedict (one of the Applicant’s experts) gave this answer to question 760
during his cross-examination
760.
I
am asking whether a compound that has a two-carbon chain linker would make it
self-evident that a compound with a one-carbon chain linker ought to have the
same activity.
THE WITNESS: I am willing to answer the question.
MR. RENAUD: You can answer the question.
THE WITNESS: Based on my experience in
the bisphosphonate world, if I was told that the molecule had a two-carbon atom
linker and it had activity, and we will define that activity as being able to
inhibit bone resorption, then to me it would be interesting to make the
one-carbon atom molecule and test it. It would be interesting to me to do that.
I would, just based on my experience, be
hesitant to predict if it would be better than or less good than the molecule
with the two-carbon atom chain based on what I knew about bisphosphonates in
1986 and earlier.
[156] Dr.
Benedict, in his affidavit, addressed the dangers involved in leaping to
conclusions as to a general class from a single compound. At paragraph 162 of
his affidavit, he wrote:
162. Second, I note that one would have no idea
what the effect of shortening the chain length would be until a member of the
class had been synthesized and tested. While the '524 and '228 Applications
disclose a broad class of compounds, including the compounds referred to as (a)
and (b) in Dr. Roberts’ depiction, these Applications do not disclose any data
such that a person skilled in the art could identify a structure-activity
relationship between the length of the chain and the anti-resorptive activity
of the bisphosphonate.
[157] Dr.
Roberts (one of Teva’s experts) said much the same in answer to question 532
and 533 of his cross-examination:
532. Q. In paragraph 253 of your
affidavit, you state:
“…In my view, the claims of the '895
patent, even the narrowest asserted claim, were obvious. If, however, the court
finds otherwise, in my view, the skilled person would have found it obvious to
make an test the claimed compounds or any one of the hydroxylated claimed
compounds, expecting that the tested compounds would be useful for inhibiting
bone resorption to treat bone metabolic disorders, as the predecessor compounds
had been…”
That is your opinion, correct?
A.
Yes.
533. Q. In your opinion, once any one of
the hydroxylated claimed compounds claimed in the
'895 patent were made and shown to have activity in
inhibiting bone resorption, the skilled person
would equally expect that the compounds would be
useful for inhibiting bone resorption and to
treat bone metabolic disorders, as the
predecessor compounds had been; correct?
A. I think testing one compound would not be
enough to support the whole patent.
[158] At
paragraph 104 of his affidavit, Dr. Ebetino (one of the Applicant’s experts)
referred to a scientific paper written by Dr. Russell, whom he described as a
current leader in the field in 2011, and quoted the following passage from that
paper, Exhibit M:
It should be remembered that
despite the intensive efforts of medicinal chemists throughout the 1980s the
identification of promising BPs was largely an empirical exercise. Any new BP
had to be treated to determine its biological activity, which could not be
predicted from its structure alone. Even quite close structural analogues could
show striking differences in biological activity. It is only in the past decade
or so, after the molecular mechanisms of action have become much clearer, has
it been possible to relate structure to activity on a more scientific basis.
[159] I
conclude that it would not be “more or less self evident” that the class of
compounds claimed in claim 14 of the '895 patent or zoledronate as claimed in
the '937 patent ought to work as of their respective dates of invention.
[160] I
agree that researchers working in the area may have perceived a “hole”, as
Teva’s Counsel put it, in the state of the art in that the “one carbon linker”
had not been explored. However, given the numerous choices for what are described
as the R1 and R2 positions, even if some are more
apparent than others, and given that there was no real predictability as to
what might work. This would be the same whether one considers common general
knowledge or state of the art. I cannot conclude that it was “self evident”
that what is claimed in either patent ought to work.
[161] I
conclude, as did Kitchin LJ of the United Kingdom Court of Appeal in MedImmune
Limited v Novartis Pharmaceuticals UK, [2012] EWCA Civ 1234, that one
cannot raise the bar too high in respect of obviousness. Research ought to be rewarded,
not discouraged:
[90] One of the matters which it may be appropriate
to take into account is whether it was obvious to try a particular route to an
improved product or process. There may be no certainty of success but the
skilled person might nevertheless assess the prospects of success as being
sufficient to warrant a trial. In some circumstances this may be sufficient to
render an invention obvious. On the other hand, there are areas of technology
such as pharmaceuticals and biotechnology which are heavily dependent on
research, and where workers are faced with many possible avenues to explore but
have little idea if any one of them will prove fruitful. Nevertheless they do
pursue them in the hope that they will find new and useful products. They
plainly would not carry out this work if the prospects of success were so low
as not to make them worthwhile. But denial of patent protection in all such
cases would act as a significant deterrent to research.
[162] I
find, therefore, that neither claim 14 of the '895 patent, nor claims 1 and 2
of the '937 patent, are invalid for obviousness. Teva’s allegations in this
respect are not justified.
LACK
OF UTILITY - PLEADING
[163]
Teva
has alleged that each of claims 14 of the '895 patent, and claims 1 and 2 of
the '937 patent, are invalid for lack of utility. Applicant’s Counsel argues
that Teva did not set out in its Notice of Allegations, sufficient in respect
of the arguments that it now makes. I disagree. Sections 1.4.2 and 2.2.2 of
that Notice, which spans some three pages each, provide sufficient basis for
the arguments made before me.
UTILITY – CLAIM
14 OF THE '895 PATENT
[164] The
evidence shows that the inventors named in the '895 patent tested two
compounds, neither of which was zoledronate, and only one of which falls within
the scope of claim 14 of the '895 patent, before filing the priority
application in Germany. In the following year, before the Canadian application
was filed, they had also made and tested zoledronate. However, the question is
not with respect to these specific compounds, but to the class of 1.2 million
compounds embraced by claim 14. I repeat what Dr. Grynpas (one of Teva’s
experts) wrote at paragraph 109 of his affidavit:
109. The Boehringer Patent claims a wide range
of compounds for a broad range of uses. The Boehringer Patent’s specification
only provides data for two of the claimed compounds. These data show that these
two similar compounds have at least a 10-fold difference in potency. Again,
with only two compounds tested, the skilled person would not have known if the
range covered by these two tested compounds represented the whole range, or the
top or bottom of the range. It is therefore not possible for the skilled person
to evaluate the potency of any of the other claimed compounds. Furthermore,
based on the information in the specification, that person would not be able to
draw any conclusions with respect to the potential utility of each of these
claimed compounds for the treatment of the claimed uses.
[165] Dr.
Lundy, whom the Applicant put forward to rebut Dr. Grynpas, took a rather
measured and cautious approach in considering the matter. At paragraphs 98 to
100, he very carefully attempts to define and distinguish the wording that he
uses and that of the patent:
98. At page 2, lines 5 to 11, the
inventors state:
Moreover on the basis of these properties,
they can also be used in the therapy of bone metastases or of urolithiasis and
for the prevention of heterotopic ossifications. Furthermore, due to their
influencing of the calcium metabolism, they form a basis for the treatment of
rheumatoic arthritis, osteoarthritis and degenerative arthrosis.
99. In the underlined passages
above, the inventors are telling the skilled reader that, based upon the
ability of the compounds to be good calcium complex formers (“these
properties”), they can be used to influence calcium metabolism, which is at the
core of the identified calcium metabolic disorders. The compounds therefore
“form a basis” for the treatment of certain identified medical conditions.
100. Again, the statements
underlined above would not, in my opinion, teach the skilled reader that the
inventors were stating that the new compounds would be immediately useful in
the treatment of any medial condition. I reach this opinion on the basis of the
qualifying language used in the patent and the fact that a skilled person
would, upon reading the patent as a whole, readily understand that these new
compounds would have to undergo rigorous safety and efficacy studies before
these compounds could be considered to be a therapeutic solution in the
treatment of identified diseases of the skeletal system.
[166] Dr.
Lundy reviews the inventors’ notebooks and comes to the conclusion at paragraph
121 of his affidavit, without stating why, that “the compounds of claim 14 were
useful”. At paragraph 122, he declined to comment on sound prediction:
121. Thus, based upon the information in the
'895 Patent as confirmed by the testing in the Knauer affidavit, I am of the
opinion that the inventors had, before July 29, 1987, demonstrated that the
compounds in claim 14 were useful as calcium complex formers and inhibitors of
bone resorption in rats, and therefore had the potential to be used in the
treatment of calcium metabolism disturbances.
122. Given this demonstration of the utility, I
understand that it is unnecessary for me to consider the issue of sound
prediction. However, I have considered the issue of sound prediction below in
relation to my comments upon the affidavit of Dr. Grynpas.
[167] Given
Dr. Lundy’s answers on cross-examination as exemplified by the answer to
question 760 set out earlier in these Reasons that he would have to test before
knowing utility, I find that the inventors named in the '859 patent did not, as
of the Canadian filing date, establish that the class of 1.2 million compounds
embraced by claim 14 had utility.
[168] Further,
there is nothing in the description of the '859 patent that any witness said
would establish a basis for sound prediction that all members of that class
would have utility. In brief, the state of the art was at the empirical stage
where compounds would have to be assessed individually. There was no consensus
in the state of the art at the time that there was a basis for drawing
conclusions as to a class.
[169] Lord
MacDermott put the situation well in May & Baker Limited v Boots Pure
Drug Company (1950), 67 RPC 23 (HL) at page 50:
Before proceeding to consider the original
specification and the nature of the invention it claims it will be appropriate
to mention two matters which, while this particular art remains in an empirical
state, appear to me to be necessary consequences of that characteristic. In the
first place an invention in this chemo-therapeutic field must be in respect of
a substance which has actually been produced. There cannot be an empirical
discovery in respect of a bare formula. And secondly, the discovery of each new
compound having a therapeutic value is a separate invention. If the inventor is
bound to say – “I have made” a new substance which I find has therapeutic
value, but I cannot be certain that any “other substance, no matter how similar
its molecular structure, will have such a value “until I made and test it”
then, as it seems to me, the inventive step he has taken must attach to the
single substance he has made and to it alone. And if he has made and proved
several such substances the position must, I think, remain the same for, while
the art retains its empirical nature, the worth of each new substance is a new
discovery. But when the inventor can say that his inventive step is such that
each of the various new products which manifest it must have therapeutic value,
and that although some of them have never been made, then, as I see the matter,
the state of the art will have changed. It will have lost its empirical nature,
at least to some extent, and the chemist will have found some law or principle
by which he may predicate therapeutic effect in advance.
[170] I
find that Teva’s allegations as to lack of utility of claim 14 of the ‘895
patent are justified.
LACK OF UTILITY
– CLAIMS 1 & 2 OF THE '937 PATENT
[171] Unlike
the '895 patent, the claims of the '937 patent are directed to one compound
only, zoledronate. The inventors made and tested that compound before the
Canadian application was filed and found it to be useful for the stated purpose
namely, a pronounced regulatory action on the calcium metabolism of
warm-blooded animals.
[172] I
find that Teva’s allegations as to lack of utility in respect of claims 1 and 2
of the '937 patent not to be justified.
SUFFICIENCY -
PLEADING
[173] Teva
has alleged that each of the '859 and '937 patents lack sufficiency and do not
show how to make and use the compounds claimed in the claims at issue.
Applicant’s Counsel argues that Teva did not set out in its Notice of
Allegations sufficient allegations in respect of the arguments that it now
makes. I disagree. Sections 1.4.3 and 2.2.3 of that Notice provide a sufficient
basis for the arguments made before me.
SUFFICIENCY – LEGAL
PRINCIPLES
[174] As
discussed earlier in Teva, supra, the Supreme Court of Canada reaffirmed
its earlier decisions in Consolboard and Pioneer Hi-Bred in
establishing that, for a disclosure be sufficient, it must enable a person
skilled in the art, having only the disclosure, to put the invention into
practice. LeBel J wrote at paragraphs 51 and 52:
51 In Pioneer Hi-Bred, the Court referred to
Consolboard in discussing the Act's disclosure requirements once again. Lamer
J. (as he then was), writing for the Court, described those requirements as
follows:
In summary, the Patent Act requires that the
applicant file a specification including disclosure and claims (Consolboard
Inc., supra, at p. 520). Canadian courts have stated in a number of cases the
test to be applied in determining whether disclosure is complete. The applicant
must disclose everything that is essential for the invention to function
properly. To be complete, it must meet two conditions: it must describe the
invention and define the way it is produced or built ... . The applicant must
define the nature of the invention and describe how it is put into operation. A
failure to meet the first condition would invalidate the application for
ambiguity, while a failure to meet the second invalidates it for insufficiency.
The description must be such as to enable a person skilled in the art or the
field of the invention to produce it using only the instructions contained in
the disclosure ... and once the monopoly period is over, to use the invention
as successfully as the inventor could at the time of his application (Minerals
Separation, supra, at p. 316). [Emphasis added; citations omitted; pp.
1637-38.]
52 In Consolboard and in Pioneer Hi-Bred, the
Court correctly analysed the disclosure requirements set out in s. 27(3) of the
Act. The reasoning in those cases should be reaffirmed and applied in the case
at bar.
[175] As
the Supreme Court in Consolboard affirmed, the specification does not
have to set out all the advantages, nor all the reasons why the invention
works. Dickson J, for the Court, wrote at page 526:
As Thorson P. stated in R. v.
American Optical Company et al. at p. 85:
Nor is it any objection to the
sufficiency of the disclosures that the advantages of the invention as
enumerated by Professor Price were not set out in the specification…If an
inventor has adequately defined his invention he is entitled to its benefit
even if he does not fully appreciate or realize the advantages that flow from
it or cannot give the scientific reasons for them. It is sufficient if the
specification correctly and fully describes the invention and its operation or
use as contemplated by the Inventor, so that the public, meaning thereby
persons skilled in the art, may be able, with only the specification, to use
the invention as successfully as the Inventor could himself.
SUFFICIENCY – DATE FOR
DETERMINATION
[176] The
date upon which sufficiency is to be determined becomes important in this case.
Teva asserts that the date for determination is the date of filing the
application in Canada. The Applicant asserts that it is the date of publication
which, in this case, is the dates upon which the patents were issued and
granted.
[177] For
the same reasons as discussed with respect to utility, I find that the '895
patent, claim 14, is insufficient, even at the date that the patent was issued
and granted. No further discussion is required in respect of that patent.
[178] The
matter is different with respect to the '937 patent, claims 1 and 2. The patent
was issued and granted with only two claims – both specific to zoledronate. For
the same reasons as previously set out, I have distinguished this patent from
that considered by the Supreme Court in Teva on the basis that the
claims were specific to zoledronate, only. However, when the application was
filed in Canada, the application contained claims to many compounds, including
genus claims and claims to specific compounds; including, but not restricted
to, zoledronate. If I were to consider sufficiency as of the date of filing the
application, I would find that the application was no different than that
considered by the Supreme Court in Teva, and thus was invalid for lack
of sufficient disclosure.
[179] Canadian
law has not been clear as to what is the date for considering sufficiency.
Under the “old” Patent Act, an application was filed and never available
to the public until it was issued and granted. There was no time limit as to
how long an application could remain in the Patent Office, provided that timely
responses to examiner’s office actions were made. Where a patent application
was in conflict with another, years could elapse, as is the case here, before a
patent was issued and granted. While an application was pending, claims could
be added, removed or changed. The disclosure, subject to correction of clerical
and editing errors, a specification could not be amended to describe or add matter
not “reasonably inferred” from the specification as originally filed (Patent
Rules SOR/96-423, Rule 181).
[180] Under
the “new” Patent Act, applicable to applications filed after October 1,
1989, a patent application is available to the public eighteen months after its
Canadian or priority filing date, if applicable. Thus, eighteen months or less
after an application was filed, it was published. Amendments to the claims and
description could still be made before the patent was issued and granted, on
the same basis as an “old” Patent Act application but at least the
public could see what was going on.
[181] Thus,
for “old” Patent Act patents, there is a choice of two dates to consider;
the application date, and the date of publication, which was the date the
patent was issued and granted. For a “new” Patent Act patent, there is a
choice of three dates; the application date, the publication date (18 months
after the Canadian, or if applicable, priority application), and the date that
the patent was issued and granted.
[182] Binnie
J for the Supreme Court in Free World Trust v Électro Santé Inc, [2000]
2 SCR 1024, established that the critical date for claim construction was the
date of publication (i.e. for “new” Act patents, 18 months after first
filing an application; for “old” Act patents, the date the patent was
issued and granted). He expressly left open whether the same date would apply
in respect of consideration of sufficient disclosure. It is to be noted that he
relied on decisions of the United Kingdom Courts in that regard when he wrote
at paragraph 53:
53 The date of publication continues to be the
critical date in England: Terrell, supra, at p. 106, although Lord Hoffmann (as
he now is) has observed that "there is an important difference between the
1949 [Patent Act] and the 1977 [Patent Act]" which requires the date of
application (or priority date) to become the critical date for certain purposes:
Biogen Inc. v. Medeva PLC, [1997] R.P.C. 1 (H.L.), at p. 54. In that case the
court was dealing with the sufficiency of disclosure, but some English judges
have taken the cue to construe claims as of the date of application as well,
e.g., Dyson Appliances Ltd. v. Hoover Ltd., [2000] E.W.J. No. 4994 (QL)(Pat. Ct.), at para. 48(k). In Canada, Reed J. advocated a similar position in [page1055] AT
& T Technologies, Inc. v. Mitel Corp. (1989), 26 C.P.R. (3d) 238
(F.C.T.D.), at p. 260, even in the absence of these statutory changes. While
there may be some advantages to the establishment of a single critical date for
multiple purposes including obviousness, sufficiency and claims construction,
my view is that Canadian law does not support the date of application as the
critical date for claims construction.
[183] The
only other decision of the Supreme Court of Canada that touches on the matter
is that of Pioneer Hi-Bred Limited v Commissioner of Patents, [1989] 1
SCR 1623. It must be noted, however, that the Court was dealing there only with
a patent application; no patent had been granted. The issue of sufficiency
arose in the context as to whether a patent application directed to hybrid corn
was sufficient in describing how the hybrid was developed. Lamer J, for the
Court, wrote at pages 1637 and 1638:
It appears to me that the duty of disclosing the
steps followed in arriving at an invention is a general principle of patent law
recognized by the domestic legislation of many countries (in the United
Kingdom, see Patents Act 1977 (U.K.), 1977, c. 37, s. 14(3); in the U.S., see
35 U.S.C. § 112 (1982); see also the West German legislation, in s. 35(2) and
international treaties (Patent Cooperation Treaty, June 19, 1970, 28 U.S.T.
7647, Art. 5; European Convention, October 5, 1973, Art. 83).
In summary, the Patent Act required that the
applicant file a specification including disclosure and claims (Consolboard
Inc., supra, at p. 520). Canadian courts have stated in a number of cases the
test to be applied in determining whether disclosure is complete. The applicant
must disclose everything that is essential for the invention to function
properly. To be complete, it must meet two conditions: it must describe the
invention and define the way it is produced or built (Thorson P. in Minerals
Separation North American Corp. v. Noranda Mines Ltd., [1947] Ex. C.R. 306, at
p. 316). The applicant must define the nature of the invention and describe how
it is put into operation. A failure to meet the first condition would invalidate
the application for ambiguity, while a failure to meet the second invalidates
it for insufficiency. The description must be such as to enable a person
skilled in the art or the filed of the invention to produce it using only the
instructions contained in the disclosure (Pigeon J. in Burton Parsons Chemicals
Inc. v. Hewlett-Packard (Canada) Ltd., [1976] 1 S.C.R. 555, at p. 563; Monsanto
Co. v. Commissioner of Patents, [1979] 2 S.C.R. 1108, at p. 1113) and once the
monopoly period is over, to use the invention as successfully as the inventor
could at the time of his application (Minerals Separation, supra, at p. 316).
[184] Turning
to the United Kingdom jurisprudence, I start with the brief summary provided by
the authors of Terrell on the Law of Patents (16th ed), Sweet
& Maxwell, London, 2006 at paragraph 7 – 93:
On what date is the sufficiency of a specification
to be judged?
The House of Lords in Biogen Inc v
Medeva Plc held that the correct date for assessing sufficiency for the
purposes of the 1977 Act was the date of application, because matter may not be
added and an insufficient application should not become sufficient because of
general developments in the state of the art after the filing date. It had
previously been considered that the relevant date was the date of publication,
but that is no longer good law.
[185] The
House of Lords in Biogen Inc v Medeva Plc, [1997] RPC 1 was required to
address the date upon which sufficiency was to be considered because of changes
to the United Kingdom Patent Act in 1977. Prior to those changes, a
Court could invalidate a patent if a claim lacked a “fair basis” in the
description. After 1977, the Court or the Comptroller (like our Commissioner of
Patents) could revoke a patent if it did not disclose the invention clearly and
completely enough (section 72(1)(c), Patent Act 1977, 1977, c. 37). Lord
Hoffman, whose opinion the other members of the House adopted, considered the
question at length. I will repeat all of what he said; however, in brief, he
held that the relevant date for considering sufficiency was the date of
application. This was done essentially on a policy consideration. An
application, once it was filed, could not be amended. An applicant should not
be able to take advantage of intervening advances in the state of the art so as
to render sufficient an insufficient application as filed. He said, as reported
at pages 53 and 54:
14. Sufficiency
If your Lordships are agreed that,
lacking the support of an earlier priority dated, the patent is valid for
obviousness, it is unnecessary to consider whether it was also invalid for
insufficiency and therefore liable to be revoked under section 72(1)(c). But
the reasoning by which I have come to the conclusion that the patent was not
entitled to the earlier priority also, in my view, leads to the conclusion that
it was insufficient. I should however mention one point of some general
importance concerning the construction of this provision which arose in the
course of argument. This is the question of the date on which the specification
must “disclose the invention clearly enough and completely enough for it to be
performed by a person skilled in the art”. The Court of Appeal thought it was
the date of filing of the application, which in this case was 21 December 1979.
Aldous J. said it was the date upon which the application was published, which
was 28 May 1986. On the latter view, a specification may be insufficient when
the application is filed but satisfy section 72(1)(c) because of advances in
the art made between then and the date of publication. I do not think that the
point arises in this case, because, whatever date one chooses, the patent did
not disclose any method for making the antigens other than the disclosed in
Biogen 1. It therefore remained insufficient for the purposes of sustaining a
claim to every recombinant DNA method. Nevertheless, since the point was argued
and there was a difference of view in the courts below, I shall shortly express
my own opinion.
Aldous J. followed a number of
authorities which held that the date of publication was the date for deciding
the question of sufficiency under the Patents Act 1949. The reasoning was that
the purpose of requiring a specification was to allow the public to work the
invention after the expiry of the monopoly. This in itself might suggest that
it was enough if the disclosure was sufficient when the patent expired. But, as
Buckley L.J. said in Standard Brands Inc.’s Patent (No. 2) ‘1981] R.P.C. 499,
529, the public was also entitled to know as soon as the patent is published
whether it was valid or not. This pointed to the date of publication. He also
drew attention to the fact that the specification might have been amended after
filing. Such amendments would be treated as relating back to the date of filing
and it would therefore be inappropriate to test sufficiency by reference to the
specification originally filed.
In my view, however, there is an
important difference between the 1949 and 1977 Acts which make decisions on the
earlier Act an unsafe guide. Section l72(1)(c) of the 1977 is not only intended
to ensure that the public can work the invention after expiration of the
monopoly. It is also intended to give the court in revocation proceedings a
jurisdiction which mirrors that of the Patent Office under section 14(3) or the
E.P.O. under article 83 of the EPC, namely, to hold a patent invalid on the
substantive ground that, as the E.P.O. said in Exxon/Fuel Oils (T 409/91)
[1994] O,J. E.P.O. 653, paragraph 3.3, the extent of the monopoly claimed exceeds
the technical contribution to the art made by the invention as described in the
specification. In the 1949 Act, this function was performed by another ground
for revocation, namely that the claim was not “fairly based on the matter
disclosed in the specification” (section 32(1)(i)). The requirement of
sufficiency was therefore regarded as serving a narrower purpose. But the
disappearance of “lack of fair basis” as an express ground for revocation does
not in my view mean that general principle which it expressed has been
abandoned. The jurisprudence of the E.P.O. shows that it is still in full
vigour and embodied in articles 83 and 84 of the EPC, of which the equivalents
in the 1977 Act are section 14(3) and (5) and section 72(1)(c).
Section 72(1)(c) can only give effect to
this principle if the relevant date for compliance is the date of application.
It would be illogical if a patent which ought to have been rejected under
section 14(3) is rendered immune from revocation under section 72(1)(c) by advances
in the art between the date of application and the publication of the
specification. The provisions for amendment, so far from detracting from this
view, seem to me to support it. Section 76(2) says that the amended application
shall not disclose matter which extends beyond that previously disclosed. In
other words, the application may not add new matter to make an insufficient
application sufficient. It seems to me in accordance with this scheme that an
insufficient application should also not become sufficient because of general
developments in the state of the art after the filing date. I therefore agree
on this point with the Court of Appeal.
[186] That
decision would make sense in Canada under the scheme of either the “old” or
“new” Patent Act, were it not for the recent decision of the
Supreme Court of Canada in Teva.
[187] The
Teva decision has caused me to distinguish the '937 patent at issue here
from that considered by the Supreme Court on the basis that in the '937 patent,
the claims were limited to a single compound. Claims can be added, removed or
amended at any time during the application process, whether one is dealing with
the “old” or “new” Patent Act. Even after a patent has been issued and
granted it may, within a limited period, be reissued with fewer or more or
different claims; claims may be reduced by disclaimer and possibly even by
dedication. The patentee is not seeking advantages because of advances in the
scientific state of the art; but rather, is seeking to keep up with the state
of the jurisprudence.
[188] I
find that the most appropriate date for consideration of sufficiency of a
Canadian patent is, as found by Buckley LJ in Standard Brands, as
referred to by Lord Hoffman in Biogen, that of the date of publication.
That is the date that the public is seized with the application. That is the
date that the person applying for the patent has committed to claims for the
invention in a manner available to the public. In the case of an “old” Act
patent, this would be the day that the patent was issued and granted. In the
case of a “new” Act patent, it would be the date of publication.
[189] Using
this date, since as of the date the '937 patent - an “old” Act patent -
was issued and granted, the patent claims were restricted to zoledronate, and
thus the patent is distinguishable from that considered by the Supreme Court of
Canada in Teva. Accordingly, I find, in this case, that Teva’s
allegations as to insufficiency of the '937 patent are not justified.
CONCLUSIONS
AND COSTS
[190]
In
conclusion, I have found that Teva’s allegations as to invalidity of the '895
patent, claim 14, on the grounds of invalidity and insufficiency, are
justified. The application in respect of that patent must be dismissed.
[191] I
have found Teva’s allegations as to invalidity of the '937 patent, claims 1 and
2, not to be justified. The application in respect of that patent will be
allowed.
[192] The
Applicant has been successful in part. While I appreciate that, in the result,
the Applicant will secure an Order for prohibition for the longer term of the
two patents at issue; costs are intended to defray, in part, the expenses of
the litigation. In this case, using a rough measure, I allocate half the
expenses to each patent.
[193] Costs
are awarded at the middle of Column IV, which is usual in these cases. Costs of
a senior and junior Counsel at the hearing are awarded. Experts fees are
awarded provided that they are reasonable and do not exceed the fees of senior
Counsel for like time involvement. Disbursements related to travel for conducting
or defending a cross-examination of a witness, but not otherwise, are awarded.
I consider business class travel to be reasonable when traveling to Europe. All costs, expert fees, disbursements and applicable taxes, are to be reduced by
one-half.