PFIZER CANADA INC., v. WARNER-LAMBERT COMPANY LLC, 2013 FC 120

Date: 20130204 Docket: T-556-11 Citation: 2013 FC 120 Toronto , Ontario , February 4, 2013 PRESENT: The Honourable Mr. Justice Hughes BETWEEN: PFIZER CANADA INC., AND WARNER-LAMBERT COMPANY LLC Applicants and PHARMASCIENCE INC.

AND THE MINISTER OF HEALTH Respondents REASONS FOR JUDGMENT AND JUDGMENT [ 1 ] This is an application brought under the provisions of the Patented Medicines (Notice of Compliance) Regulations SOR/93- 133, as amended ( NOC Regulations ) to prohibit the Minister of Health from issuing a Notice of Compliance to Pharmascience Inc. in respect of its PMS-Pregabalin capsules of 25 mg, 50 mg, 75 mg, 150 mg, and 300 mg dosage strengths until the expiry of Canadian Letters Patent No. 2,255,652 ('652 patent).

The original Notice of Application was filed April 1, 2011, which means that this matter must be determined by April 1, 2013. [ 2 ] For the reasons that follow, I find that the Application is dismissed, with costs. INDEX [ 3 ] The following is an Index to these Reasons by paragraph numbers: THE PARTIES Paras 4 to 8 THE '652 PATENT GENERALLY Paras 9 to 15 THE EVIDENCE Paras 16 to 20 ISSUES Paras 21 to 23 BURDEN Paras 24 to 27

PERSON SKILLED IN THE ART Paras 28 to 35 THE '652 PATENT IN DETAIL

a) The Specification Paras 36 to 58 Paras 36 to 58 CLAIM 3 Paras 59 - 62 CONSTRUCTION OF CLAIM 3 – PAIN Paras 63 to 82 CLAIMS BROADER THAN THE INVENTION MADE OR DISCLOSED Paras 83 to 95 SOUND PREDICTION – UTILITY DISCLOSURE Pharmaceutical Claims Invention History of the Jurisprudence Where does all this leave us? In the present case: Paras 96 to 163 Paras 102 to 105 Paras 106 to 111 Paras 112 to 158 Para 159 Paras 160 to 163 UTILITY – SOUND PREDICTION – CLAIM 3 1 . Pregabalin does not treat all types of pain 2 .

The patent fails to disclose any utility of the racemate or any basis for a sound prediction that the racemate would treat all or even some types of pain: Paras 164 to 185 Paras 168 to 178 Paras 179 to 185 OBVIOUSNESS Paras 186 to 205 REISSUE APPLICATION Paras 206 to 215 CONCLUSIONS AND COSTS Paras 216 to 218 THE PARTIES [ 4 ] The Applicant Pfizer Canada Inc. (Pfizer) is a “first person” as so described in the NOC Regulations . It has listed the '652 patent in accordance with those Regulations .

Pfizer has obtained from the Minister of Health a Notice of Compliance to sell tablets containing pregabalin in 25, 50, 75, 150, and 300 mg. strengths, which it does under the brand name LYRICA. [ 5 ] The Applicant Warner-Lambert Company LLC (Warner-Lambert) claims to be the owner of the '652 patent. This claim is not contested in these proceedings. [ 6 ] The Respondent Pharmascience Inc. (Pharmascience) is a “second person” as so described in the NOC Regulations . It seeks to sell a generic version of Pfizer’s LYRICA drug. To do so, it must receive a Notice of Compliance from the Minister of Health.

In accordance with the NOC Regulations , Pharmascience has served Pfizer with a Notice of Allegation dated February 11, 2011. [ 7 ] In that Notice of Allegation, Pharmascience alleged that claims 4, 6-12, 14 and 15 of the ‘652 patent would not be infringed, and that the patent is invalid on the grounds of anticipation, obviousness, inutility, lack of sound prediction, ambiguity and claims broader than the invention made or disclosed; all as more particularly set out in the enclosed Detailed Statement. [ 8 ] 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 Pharmascience in appropriate circumstances.

The Minister took no active role in these proceedings.

THE '652 PATENT GENERALLY [ 9 ] Canadian Letters Patent No. 2,255,652 (the '652 patent) was applied for by an application deemed to be filed with the Canadian Patent Office on July 16, 1997. Therefore, that patent is governed by the provisions of the “new” Patent Act , RSC 1985, c. P-4, applicable to patents applied for after October 1, 1989. [ 10 ] The application was filed under the provisions of the Patent Cooperation Treaty (PCT) and claims priority from a first application filed in the United States Patent Office on July 24, 1996.

This is the date upon which issues of obviousness and anticipation will be determined. [ 11 ] Under the provisions of the PCT the application for the patent was deemed to be filed in the Canadian Patent Office on July 16, 1997. This is the date from which the term of the patent is to be calculated and upon which the issue of sound prediction is to be considered. [ 12 ] The application was laid open for public inspection under the provisions of the Patent Cooperation Treaty on January 29, 1998.

This is the date that is to be used for purposes of construing the patent and its claims. [ 13 ] The '652 patent names Lakhbir Singh of Great Britain as inventor. He filed an affidavit in these proceedings and was cross- examined. [ 14 ] The '652 patent was issued and granted to Warner-Lambert Company of the United States on July 13, 2004.

The term of the patent, unless the patent is declared to be invalid in an appropriate action, will expire twenty (20) years from the date that the application was filed in Canada; that is, on July 16, 2017. [ 15 ] It is agreed that only one claim, claim 3, of the '652 patent is at issue in this proceeding. The construction of that claim and the patent will be considered later in these Reasons. THE EVIDENCE [ 16 ] 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. [ 17 ] The Applicants have filed the affidavits, with exhibits, of the following persons: • Dr. Kenneth E. McCarson : Associate Professor of Pharmacology at the University of Kansas Medical Centre, Kansas City, Kansas. He claims expertise in respect of the formalin test, carrageenin test, and post-surgical model all as reported in the '652 patent. He submitted an affidavit in chief and a reply affidavit, and was cross-examined. • Dr.

Stephen McMahon : Professor of Physiology at King’s College London, and Director of the London Pain Consortium. He claims expertise in the fields of neuroscience, somatosensory neurobiology, and particularly, pain. Dr. McMahon submitted an affidavit in chief and a reply affidavit, and was cross-examined. • Dr. Roman Jovey : A medical doctor trained as a general practitioner and is the Medical Director at CPM Centres for Pain Management in Mississauga, Ontario, and Physician-Director of the Addictions & Concurrent Disorders Centre at the Credit Valley Hospital in Mississauga.

He claims expertise, as a medical doctor, in the areas of chronic pain management and substance abuse. Dr. Jovey filed an affidavit and was cross-examined. • Dr. Lakhbir Singh : He is the person named as inventor in the '652 patent. Dr. Singh filed an affidavit and was cross- examined.

• Dr. Ann G. Hayes : A pharmacologist acting as an independent pharmaceutical consultant to the pharmaceutical industry, particularly in the area of central nervous system diseases. Her affidavit was filed in reply to the affidavit of Dr. Jamali (which I will note later). She was cross-examined. • Dianne Zimmerman : A law clerk in the offices of the Applicants’ solicitors. Her affidavit served to place a large number of documents in the record. She was not cross-examined. [ 18 ] Pharmascience raised challenges as to the extent of the expertise as claimed by Drs. McCarson, McMahon, and Jovey.

I find that they have extensive expertise sufficient to be of assistance here. [ 19 ] The Respondent Pharmascience filed the affidavits, with exhibits, of the following persons: • Dr. Alan Cowan : A Professor of Pharmacology and Anaesthesiology at Temple University, Pennsylvania. He claims expertise in the treatment of pain and use of various animal models of pain. He filed an affidavit in chief and a sur-reply affidavit. He was cross-examined. • Dr. C. Peter Watson : An Assistant Professor of Medicine, Division of Neurology, at the University of Toronto.

He is a medical doctor and claims expertise in the treatment and diagnosis of neuropathic pain. Dr. Watson submitted an affidavit and was cross- examined. • Dr. Fakhreddin Jamali : Professor in the Faculty of Pharmacy and Pharmaceutical Services, University of Alberta. He claims expertise in the field of pharmacokinetics and pharmacodynamics, onset of analgesia and inflammation. He filed an affidavit in chief and another in sur-reply. He was cross-examined. • Rebecca Hayley : A law clerk in the offices of Pharmascience’s solicitors. Her affidavit served to place certain documents in the record.

She was not cross-examined. [ 20 ] The Applicant challenges the expertise as claimed by Dr.Watson to the extent that he is a medical doctor and not expert in animal models. I reject that challenge as I will find that the patent is directed to persons skilled in the art including medical doctors experienced in the treatment of pain such as Dr Watson. ISSUES [ 21 ] The principal issue for determination by the Court is whether or not to grant an Order prohibiting the Minister from granting a Notice of Compliance to Pharmascience for its generic pregabalin tablets until the expiry of the '652 patent.

The basis for doing so is whether the various allegations raised by Pharmascience as to invalidity of the '652 patent, are justified. Those allegations, though many were raised in the Notice of Allegation, have been reduced in the written and oral arguments made by Pharmascience, to the following: • Claims Broader than the Invention Made or Disclosed • Sound Prediction • Actual Inutility • Obviousness [ 22 ] It must be noted that while Pharmascience raised the issues of anticipation and ambiguity in its Notice of Allegation these issues were not pursued in its written argument submitted to the Court.

The Notice of Allegation did raise the point that Pfizer had applied to reissue the ‘652 patent so as to include a number of very specific claims but ultimately abandoned that application. This point was not included in Pharmascience’s written argument but was addressed in its oral argument. Pharmascience raised a question of sufficiency in Dr Cowan’s affidavit (paragraphs 105-107) however sufficiency was not raised in the Notice of Allegation.

[ 23 ] In order to address the active issues, the Court must address the following issues first: • Burden • Person Skilled in the Art • Claim Construction BURDEN [ 24 ] The main issue is whether Pharmascience’s allegations as to invalidity of the ‘652 patent are justified. Infringement is not an issue. [ 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. [ 27 ] In this case Pharmascience has led evidence as to validity as has Pfizer. The matter will be considered on the usual civil burden which rests upon Pharmascience. PERSON SKILLED IN THE ART [ 28 ] The person skilled in the art, or as sometimes described, the person of ordinary skill in the art (POSITA) is the notional person, which may include a team of persons, through whose eyes a patent is to be construed, the prior art is to be considered.

This notional person may be pertinent to other issues that arise in respect of a patent under consideration by the Court. [ 29 ] In the present case the parties are agreed, to a certain extent, as to the qualifications as to the person skilled in the art. They are agreed that such a person includes a scientist with advanced education and experience in pharmaceuticals used in the treatment of pain. Pharmascience urges that such a person should be in addition should be a physician who treats patients suffering from pain. [ 30 ] Assistance can be derived from the wording of the ‘652 patent.

The opening paragraph states: The present invention is the use of analogs of glutamic acid and gamma-aminobutyric acid (GABA) in pain therapy, as the compounds exhibit analgesic/antihyperalgesic action.

Advantages of the use of the compounds includes the finding that repeated use does not lead to tolerance nor is there a cross-tolerance between morphine and the compounds. [ 31 ] The ‘652 patent acknowledges, at page 1, lines 9 to 15 that the compounds themselves are known and have been previously used to treat certain disorders of the central nervous system. [ 32 ] Much of the description of the patent deals with tests administered to rats in order to determine or predict the ability of the compounds to alleviate pain. [ 33 ] I note that the named inventor, Dr.

Singh, in cross-examination in reply to questions 79 to 82 said that he was not a chemist but that his contribution was as a pharmacologist. [ 34 ] I am satisfied that a person skilled in the art is a team including a scientist such as a pharmacologist with experience in animal modeling with compounds of interest and a physician with experience in the selection and use of compounds likely or believed to be

likely to be effective in the alleviation of pain. [ 35 ] I am able, in varying degrees, to receive assistance from all the expert witnesses whose evidence has been provided in these proceedings. THE '652 PATENT IN DETAIL

a) The Specification [ 36 ] The specification or descriptive portion of the patent begins at page 1 with a general statement of the invention; namely, the use of certain compounds in pain therapy, because they exhibit certain action. The advantage is stated to be that they do not lead to tolerance or cross-tolerance with morphine. The present invention is the use of analogs of glutamic acid and gamma-aminobutyric acid (GABA) in pain therapy, as the compounds exhibit analgesic/antihyperalgesic action.

Advantages of the use of the compounds includes the finding that repeated use does not lead to tolerance nor is there a cross-tolerance between morphine and the compounds. [ 37 ] The next paragraph at page 1 acknowledges that these are known compounds previously used to treat certain central nervous system disorders; a number of patents disclosing the compounds and such uses are cited; the WP 93/23383 patent should be noted as it is referred to by some of the expert witnesses: The compounds of the invention are known agents useful in antiseizure therapy for central nervous system disorders such as epilepsy, Huntington’s chorea, cerebral ischemia, Parkinson’s disease, tardive dyskinesia, and spasticity.

It has also been suggested that the compounds can be used as antidepressants, anxiolytics, and antipsychotics. See WO 92/09560 (United States Serial Number 618,692 filed November 27, 1990) and WP 93/23383 (United States Serial Number 886,080 filed May 20, 1992). [ 38 ] There follows at page 1 a

summary of the invention; namely, the use of a certain compound in the treatment of pain “especially for chronic pain”, including “but not limited to” a long list of particular types of pain, including a type of “acute” pain:

SUMMARY OF THE INVENTION The instant invention is a method of using a compound of Formula I below in the treatment of pain, especially for treatment of chronic pain disorders.

Such disorders include, but are not limited to, inflammatory pain, postoperative pain, osteoarthritis pain associated with metastatic cancer, trigeminal neuralgia, acute herpetic and postherpetic neuralgia, diabetic neuropathy, causalgia, brachial plexus avulsion, occipital neuralgia, reflex sympathetic dystrophy, fibromyalgia, gout, phantom limb pain, burn pain, and other forms of neuralgic, neuropathic, and idiopathic pain syndromes. [ 39 ] At the top of page 2, the compound is described by a general formula called Formula I, which is later claimed in claim 1; a set of preferred compounds are set out, which are claimed in claim 2, and more preferred compounds – two of them – are set out; these two compounds are claimed in claim 3, which is the claim at issue.

[ 40 ] I digress at this point to deal with the concept of racemates, as the above description deals with diastereomers and enantiomers. A brief discussion of racemates and enantiomers can be found in the affidavits of Dr. Hayes and the reply affidavit of Dr. Jamali. I repeat what I wrote in Janssen-Ortho Inc v Novopharm Limited , 2006 FC 1234 (aff’d 2007 FCA 217 ) at paragraphs 28 to 31: 28 Molecular compounds although often written out as a series of letters, number and symbols or depicted on a flat sheet of paper, do not exist that way in reality. They are three dimensional structures.

Some compounds only assume one three dimensional shape, others such as those that are racemic, do not. 29 Racemic compounds, also called racemates, exist as comprising the same atoms in the same sequence, but bent at joints called chiral centres so as to assume what has been called left handed (levo) or right handed (dextro) configurations. Levo is sometimes simply depicted as (-) and dextro as (+). The left handed configuration is the mirror image of the right. 30 A racemate is said to contain an equal number of left and right handed configurations of the molecule.

This concept is sometimes depicted (+/-) although that is unnecessary when a competent chemist would be able to detect a chiral centre. 31 Knowing that a compound is racemic is to know that, if there is only one chiral centre as there is in this case of Ofloxacin, there is a left hand and a right hand version of the molecule. Each version can be detected optically by a device such as a polarimeter. That device will detect which of the two configurations turns light to the left (levo or -) and which turns light to the right (dextro or +).

Depending on the prevailing conditions different researchers may detect the molecules differently. [ 41 ] To this I would add that sometimes, instead of using (+) or (-), or dextro or levo, to identify one or other of the enantiomers, the letters R and S are used. [ 42 ] In the language of the '652 patent, the two compounds that are said to be “more preferred’, the racemate (having equal parts of the S and R enantiomers) is written as “3-aminomethyl-5-methyl-hexanoic acid” and the enantiomer of interest is the “S” enantiomer, which is written as “(S)-3-(aminomethyl)-5-methylhexanoic acid”.

This “S” enantiomer is also identified in the patent as “CI-1008 (S)”. In the evidence and argument in this case, and in general scientific parlance, the S enantiomer is referred to as pregabalin.

Thus, the two “more preferred” compounds, as set out in the description and in claim 3, can more easily be referred to as pregabalin and its racemate. [ 43 ] I further note that in some of the scientific literature in evidence the R enantiomer is referred to as R-Isobutyl gaba. [ 44 ] To return to the text of the ‘652 patent and commencing at the lower portion of page 2 and continuing to the top portion of page 5 of the '652 patent, six tests conducted using rats are described, together with reference to the drawings attached to the back of the patent.

While the description refers to 3-aminomethyl-5-methyl-hexanoic acid (the racemate) as one of the compounds tested it is agreed by Counsel for the parties that what in fact was tested and being reported is a compound which is the R enantiomer and not the racemate.

[ 45 ] The first test, Figure 1, compares gabapentin, pregabalin (CI-1008) and the R enantiomer administered to rats in what has been described as a formalin test. The second and third tests, Figures 2 and 3, compares gabapentin and pregabalin administered to rats in what has been described as a carrageenin test; in one pressure is applied to a rat’s paw in the other heat is applied. In the fourth test, Figure 4, morphine, gabapentin and pregabalin are administered to rats before surgery is conducted.

The fifth test, Figure 5, is similar but it measures allodynia, a painful response to a mild stimulus such as brushing. The sixth and final test reported, Figure 6 tests only pregabalin administered to rats in respect of thermal hyperalgesia, an increased response to a painful stimulus, and allodynia. It must be noted that no tests in respect of the racemate are reported in the ‘652 patent. [ 46 ] At page 5, a “Detailed Description” of the invention is provided. It reiterates that the invention is a method of using a compound of Formula I as an analgesic in the treatment of pain.

A variety of types of pain are listed. This list is not co-extensive with the list at page 1; for instance, the two types of “acute” pain are not listed. The pain is limited to neuropathic pain. A list of such pain is provided; however, it is stated that the pain is “not limited to” the pain as listed. A one sentence paragraph follows which also includes fibromyalgia pain. A paragraph follows stating that currently-marketed analgesics (not named) treat such pain poorly due to insufficient efficacy or limiting side effects.

No statement is provided saying that the compounds of the invention are better than existing compounds; nor are test results provided to support a claim of superiority. DETAILED DESCRIPTION The instant invention is a method of using a compound of Formula I above as an analgesic in the treatment of pain as listed above. Pain such as inflammatory pain, neuropathic pain, cancer pain, postoperative pain, and idiopathic pain which is pain of unknown origin, for example, phantom limb paid are included especially. Neuropathic pain is caused by injury or infection of peripheral sensory nerves.

It includes, but is not limited to pain from peripheral nerve trauma, herpes virus infection, diabetes mellitus, causalgia, plexus avulsion, neuroma, limb amputation, and vasculitis. Neuropathic pain is also caused by nerve damage from chronic alcoholism, human immunodeficiency virus infection, hypothyroidism, uremia, or vitamin deficiencies. Neuropathic pain includes, but is not limited to pain caused by nerve injury such as, for example, the pain diabetics suffer from. Compounds of Formula I are also useful in the treatment of fibromyalgia pain.

The conditions listed above are known to be poorly treated by currently marketed analgesics such as narcotics or nonsteroidal anti-inflammatory drugs (NSAID) due to insufficient efficacy or limiting side effects. [ 47 ] The remaining portion of page 5, all of page 6 and the first paragraph of page 7 of the '652 patent is directed to chemistry, which is not of interest in respect of the matters at issue here. [ 48 ] The next three paragraphs on page 7 of the '652 patent are directed to the formulation of the compounds into pharmaceutical compositions and to dosages and administration to mammals, including humans. [ 49 ] At the bottom of page 7 and top half of page 8 is a report of a test upon rats injected with formalin, in which the effects of gabapentin, pregabalin and the racemate are measured. [ 50 ] At the lower half of page 8 over to line 11 of page 9, there is a report of a test upon rats injected with carrageenin in which the effects of gabapentin and pregabalin are measured. [ 51 ] At lines 13 and 14 of page 9, it is stated, in respect of these tests: These data show that gabapentin and CI-1008 (pregabalin) are effective in the treatment of inflammatory pain. [ 52 ] At line 14 to 19 of page 9, there is mention of a Bennett test and a Kim test; but no data, results or conclusions are presented. [ 53 ] At line 20, and following at page 9, there is a description of a Brennan test involving surgery to the hind paw of a rat.

Following that description and to the bottom of page 11, the surgical procedures and subsequent tests conducted on the rats are described

in detail. [ 54 ] The first two tests set out at page 12 describe administration to the rats, before surgery, of gababentin, pregabalin and morphine; and their reaction to heat and brushing. The third test, described at the bottom of page 12 and over to page 13, reports testing on rats after surgery, who have been administered pregabalin. [ 55 ] The conclusions in respect of these results is set out at page 13: Gabapentin and S-(+)-3-isoburylgaba did not affect PWL in the thermal hyperalgesia test or tactile allodynia scores in the contralateral paw up to the highest dose tested in any of the experiments.

In contrast, morphine (6 mg, s.c.) increased PWL of the contralateral paw in the thermal hyperalgesia test (data not shown). The results presented here show that incision of the rat plantaris muscle induces thermal hyperalgesia and tactile allodynia lasting at least 3 days. The major findings of the present study are that gabapentin and S-(+)-3-isoburylgaba are equally effective at blocking both nociceptive responses. In contrast, morphine was found to be more effective against thermal hyperalgesia than tactile allodynia.

Furthermore, S-(+)-3-isoburylgaba completely blocked induction and maintenance of allodynia and hyperalgesia. [ 56 ] The claims and drawings follow. [ 57 ] There are 16 claims in all. All are directed to a compound for use in treating pain in a mammal. Claim 1 claims the compound in very broad terms. Claim 2 narrows those terms somewhat. Claim 3 restricts the compounds to two; pregabalin and the racemate.

Claims 4 to 16, inclusive, all depend upon claim 1, which is the claim directed to a very broad number of compounds, and restrict the pain which the compound is to treat to very specific pain; claim 4 is inflammatory pain, claim 5 is neuropathic pain; claim 6 is cancer pain; claim 7 is postoperative pain; claim 8 is phantom limb pain; claim 9 is burn pain; claim 10 is gout pain; claim 11 is osteoarthritic pain; claim 12 is trigeminal neuralgia pain; claim 13 is acute herpetic and postherpetic pain; claim 14 is causalgia pain; claim 15 is idiopathic pain; claim 16 is fibromyalgia pain. [ 58 ] Claim 3 is the only claim at issue here.

CLAIM 3 [ 59 ] Claim 3 is a dependent claim. It depends on claim 1. Claims 1 and 3 read as follows: 1. For use in treating pain, in a mammal, a therapeutically effective amount of a compound of Formula I Or a pharmaceutically acceptable salt, diastereomer, or enantiomer thereof Wherein R1 is a straight or branched alkyl of from 1 to 6 carbon atoms, phenyl, or cycloalkyl of from 3 to 6 carbon atoms;

R2 is hydrogen or methyl; and R3 is hydrogen, methyl, or carboxyl. . . . 3. A compound according to claim 1 which is (S)-3-(aminomethyl)-S- methylhexanoic acid or 3-aminomethyl-5-methyl-hexanoic acid. [ 60 ] Incorporating claim 1 into claim 3, claim 3 reads as follows: 3. For use in treating pain, in a mammal, a therapeutically effective amount of a compound which is (S)-3-(aminomethyl)-5- methylhexanoic acid or 3-aminomethyl-5-methyl-hexanoic acid. [ 61 ] Using the terminology for the compounds as used in the evidence and argument in this case, claim 3 can be simplified to read: 3.

For use in treating pain, in a mammal, a therapeutically effective amount of pregabalin or its racemate. [ 62 ] There is no dispute raised that a mammal includes a human (see page 7, line 8 of the patent) and that the claim includes pregabalin or its racemate. The dispute between the parties is what is included in “pain”. CONSTRUCTION OF CLAIM 3 - PAIN [ 63 ] Claim 3 as set out above is directed to the use of pregabalin or its racemate in a mammal, including humans, in treating pain. Unlike claims 5 to 16, no particular pain or classification of pain is specified.

The court has been called upon by the parties to construe claim 3 and, in particular, what is meant by “pain”. [ 64 ] There have been many judicial instructions as to the construction of a claim.

To summarize: • construction must be done before considering the issues of validity and infringement; • construction is done by the Court alone, as a matter of law; • the Court is to construe the claim through the eyes of the person skilled in the art to which the patent pertains; • the Court may obtain the assistance of experts to explain the meaning of particular words and phrases, and as to the state of the art as of the date the claim was published; • the Court should read the claim in the context of the patent as a whole, including the description and other claims;

• The Court should avoid importing this or that gloss from the description; • the Court should not restrict the claim to specific examples in the patent; • the Court should endeavour to interpret the claim in a way that gives effect to the intention of the inventor; • the Court should endeavour to support a meritorious invention. [65] I reviewed at length in Merck & Co, Inc v Pharmascience Inc, 2010 FC 510, the development of patent claims from thebeginning of the time when patents were first granted for inventions. At first, there were no claims at all.

Then, there were generalizedstatements such as “I claim the invention of X as described herein”. Then, there came the stricter requirements, such as those set out insection 27 of the Patent Act, RSC 1987, c P-4. [66] The current state of the law has been expressed in the unanimous reasons of the Supreme Court of Canada, written by JusticeBinnie, in Free World Trust v Électro-Santé Inc., 2000 SCC 66 , [2000] 2 SCR 1024, where he described claims as fences, andthat the task of the Court is to separate the essential from the inessential.

He wrote at paragraph 15: 15 In reality, the "fences" often consist of complex layers of

definitions of different elements (or "components" or "features" or"integers") of differing complexity, substitutability and ingenuity. A matrix of descriptive words and phrases defines the monopoly, warnsthe public and ensnares the infringer. In some instances, the precise elements of the "fence" may be crucial or "essential" to the workingof the invention as claimed; in others the inventor may contemplate, and the reader skilled in the art appreciate, that variants couldeasily be used or substituted without making any material difference to the working of the invention.

The interpretative task of the courtin claims construction is to separate the one from the other, to distinguish the essential from the inessential, and to give to the "field"framed by the former the legal protection to which the holder of a valid patent is entitled. [67] At paragraph 33 and following, Justice Binnie considered two approaches to claim construction; the central claim draftingprinciple, and the peripheral claiming principle.

Canadian courts have preferred the latter, which emphasizes the language of the claimsas defining not the underlying technical idea, but the legal boundary of the state-conferred monopoly. He wrote at paragraph 33: 33 The Patent Act requires the letters patent granting a patent monopoly to include a specification which sets out a correct and full"disclosure" of the invention, i.e., "correctly and fully describe[s] the invention and its operation or use as contemplated by the inventor"(s. 34(1)(a)).

The disclosure is followed by "a claim or claims stating distinctly and in explicit terms the things or combinations that theapplicant regards as new and in which he claims an exclusive property or privilege" (s. 34(2)). It is the invention thus claimed to whichthe patentee receives the "exclusive right, privilege and liberty" of exploitation (s. 44). These provisions, and similar provisions in otherjurisdictions, have given rise to two schools of thought.

One school holds that the claim embodies a technical idea and claimsconstruction ought to look to substance rather than form to protect the inventive idea underlying the claim language. This is sometimescalled the "central claim drafting principle" [page1045] and is associated with the German and Japanese patent systems: T. Takenaka,"Doctrine of Equivalents after Hilton Davis: A Comparative Law Analysis" (1996), 22 Rutgers Computer & Tech. L. J. 479, at pp. 491,502 and 519.

The other school of thought supporting what is sometimes called the "peripheral claiming principle" emphasizes thelanguage of the claims as defining not the underlying technical idea but the legal boundary of the state-conferred monopoly.Traditionally, for reasons of fairness and predictability, Canadian courts have preferred the latter approach. [68] The conclusions were set out at paragraphs 42 and 43. Discretionary or subjective

interpretation is to be kept to a minimum. Aclaim must be interpreted in an informed and purposive way: 42 The patent system is designed to advance research and development and to encourage broader economic activity. Achievement ofthese objectives is undermined however if competitors fear to tread in the vicinity of the patent because its scope lacks a reasonablemeasure of precision and certainty. A patent of uncertain scope becomes "a public nuisance" (R.C.A. Photophone, Ld. v. Gaumont-British Picture Corp. (1936), 53 R.P.C. 167 (Eng. C.A.), at p. 195).

Potential competitors are deterred from working in areas that are notin fact covered by the patent even though costly and protracted litigation (which in the case of patent disputes can be very costly andprotracted indeed) might confirm that what the competitors propose to do is entirely lawful. Potential investment is lost or otherwisedirected. Competition is "chilled". The patent owner is getting more of a monopoly than the public bargained for. There is a higheconomic cost attached to uncertainty and it is the proper policy of patent law to keep it to a minimum.

43 The patent owner, competitors, potential infringers and the public generally are thus entitled to clear and definite rules as to theextent of the [page1050] monopoly conferred. This in turn requires that the subjective or discretionary element of claims

interpretation(e.g., the elusive quest for "the spirit of the invention") be kept to the minimum, consistent with giving "the inventor protection for thatwhich he has actually in good faith invented" (Western Electric Co. v. Baldwin International Radio of Canada, (SCC),[1934] S.C.R. 570, at p. 574).

Predictability is achieved by tying the patentee to its claims; fairness is achieved by interpreting thoseclaims in an informed and purposive way. [69] The effect of a purposive construction was set out at paragraph 50, it disciplines the scope of substantive claim construction: 50 I do not suggest that the two-stage approach necessarily ends at a different destination than the one-stage approach, or that thetwo-stage approach has resulted in abuse.

I think we should now recognize, however, that the greater the level of discretion left to courtsto peer below the language of the claims in a search for "the spirit of the invention", the less the claims can perform their public noticefunction, and the greater the resulting level of unwelcome uncertainty and unpredictability. "Purposive construction" does away with thefirst step of purely literal

interpretation but disciplines the scope of "substantive" claims construction in the interest of fairness to boththe patentee and the public. In my view its endorsement by the Federal Court of Appeal in O'Hara was correct. [70] Thus, I will turn to claim 3, and in particular, “pain”, and endeavour to construe “pain” in the context of that claim in aninformed and purposive way. [71] First, I note that claims 4 to 16 are each directed to a specific type of pain. An informed and purposive construction must,therefore, mean that the “pain” of claim 3 must include at least the specific “pains” claimed in claims 4 to 16. [72] Next, I turn to the description. At page 1, in the

SUMMARY OF THE INVENTION, there are a variety of types of pain setout as those which may be treated by the claimed compounds. That variety is greater than those claimed in claims 4 to 16. That variety issomewhat constrained by the initial words “…especially for treatment of chronic pain disorders”, but is subsequently broadened by thewords “but are not limited to”, and the inclusion of at least one type of acute pain - “acute herpetic and postherpetic neuralgia” - whichparticular pain is the subject of claim 13. [73] ‘Pain” is again discussed under the caption DETAILED DESCRIPTION at page 5 of the patent.

The description includes“pain as listed above”, clearly a reference to the description at page 1. A number of types of pain not listed in page 1 are included andsome are omitted. The words “but not limited” reappear. [74] It appears that the patent draughtsman is endeavouring to take advantage of two worlds; narrow and broad.

In patent academiccircles, this has sometimes been referred to as the “Angora Cat” approach as noted by Lord Justice Jacob in European Central Bank vDocument Security Systems Inc, [2008] EWCA Civ 192, where he said, at paragraph 5 of the report: Professor Mario Franzosi likens a patentee to an Angora cat. When validity is challenged, the patentee says his patent is very small: thecat with its fur smoothed down, cuddly and sleepy.

But when the patentee goes on the attack, the fur bristles, the cat is twice the sizewith teeth bared and eyes ablaze”. [75] A full description of Professor Franzosi’s recipe respecting parties and Angora cats can be found at: http://ipkitten.blogspot.com-uk/2010/01/more-on-that-angora-cat.html [76] The experts are, as expected, divided as to their

interpretation of “pain”. I take the answer of Dr. McMahon as given in hiscross-examination, found at Volume 4, page 859 of the Record: …I think again the affidavits all try to explain some or the potential confusion around nomenclature in this field.

[77] The Applicants, at paragraphs 16 to 19 of their Memorandum of Fact and Law, as found in Volume 24 of the Record, concedethat there are many forms of pain, acute and chronic, that do not comfortably fit within one category or the other. [78] Dr. McMahon, at paragraphs 24 and 25 of his first affidavit as found at Volume 3, page 505 of the Record, sets out fourdifferent types of pain and concludes: These different types of classifications necessarily mean that a patient’s pain cannot be given a single label. [79] Dr.

McCarson, at page 82 of his affidavit as found at Volume 1, page 114 of the Record says: Claim 3 of the Patent would therefore be understood by a person of skill in the art to encompass a broad spectrum of human pain, all ofwhich have features of inflammatory or neuropathic pain or both. [80] Dr.

McMahon argues a somewhat narrower definition at paragraph 58 of his affidavit as found at Volume 3, page 514: A skilled person would thus have understood that claim 3 of the 652 Patent claims that pregabalin will be useful in treating a widevariety of pain states that have a central sensitization as a feature, and in particular those pain states listed at page 1 of the Patent. [81] The central sensitization theory or commonality is nowhere set out in the '652 patent. Dr.

McCarson, in his cross-examination,at Volume 2, page 270 of the Record; and Dr.Cowan at paragraph 90 of his affidavit, Volume 20, page 6001, in the Record; state that, atleast for idiopathic and fibromyalgia pain, no animal model existed in 1996. Dr. McCarson, in his Reply Affidavit, paragraphs 13 and 15,found in the Record at Volume 1, pages 194 and 195, states that the central sensitization theory was, except for a few individuals, widelyaccepted by 1997. [82] Given all of the aforesaid, I construe that the meaning of “pain” as found in claim 3 of the '652 patent is to be a broad one.

Itencompasses all of the specific pains claimed in claims 4 to 16, and all of the specific pains mentioned at page 1, and at page 5 of thePatent. When the pains listed at pages 1 and 5 are broadened by the words “…but not limited to”, I find that the broadening would belimited to those pains that, as of January 1998, would be reasonably related to the named pains.

CLAIMS BROADER THAN THE INVENTION MADE OR DISCLOSED [83] The first ground upon which Pharmascience alleges that claim 3 of the '652 patent is invalid is that it is broader than theinvention made or disclosed. [84] The classic statement of the law is that of Thurlow JA, for the Court, in Leithiiser v Pengo Hydra-Pull of Canada Ltd, (FCA), [1974] 2 FC 954 at para 21: The first is whether the claims of the appellant’s patent claim more than he invented. The second is whether the claims are broader thanthe invention which is described in the specification.

If the answer to either question is in the affirmative, as I understand the law, theclaims are invalid. [85] The genesis of the law on this patent is the statement of Lord MacMillan in Mullard Radio Valve Co v Phelan Radio &Television Corp of Great Britain Ltd (1936), 53 RPC 323 (HC) at page 347: …If an inventor claims an

article as his invention but the

article will only achieve his avowed object in a particular juxtaposition and hisinventive idea consists in the discovery that in the particular juxtaposition it will give new and useful results, I do not think that he isentitled to claim the

article at large apart from the juxtaposition which is essential to the achievement of those results. [86] These principles have been followed in many decisions of this Court and the Federal Court of Appeal, including: Amfac

Foods Inc v Irving Pulp & Paper Ltd (1986), 12 CPR (3d) 193 (FCA) at pages 202 to 204 ; Eli Lilly Canada Inc v Apotex Inc , 2008 FC 142 at paras 180 to 182 ; and Biovail Pharmaceuticals Inc v Canada (Minister of National Health and Welfare) , 2005 FC 9 , at paragraphs 59 to 61 , to name a few. [ 87 ] The obvious corollary to this proposition was stated by Thorson P in Lovell Manufacturing Co v Beatty Bros Ltd (1962), 41 CPR 18 (Ex Ct) at page 66 : If the claims fairly read on what has been disclosed and illustrated in the specification and drawings…they are not wider than the invention. [ 88 ] Turning to claim 3 as I have construed it, it claims that either pregabalin or its racemate may be used in the treatment of a variety of pains as disclosed in the descriptive portion of the patent including those pains, which as of 1997, would be considered by a person skilled in the art to be reasonably related to those pains, in a mammal, including a human. [ 89 ] The Applicants, in their memorandum, Volume 24 of the Record at paragraph 85, describe the “inventive concept” of the '652 patent as: …the novel therapeutic usefulness of pregabalin to treat pain. [ 90 ] It must be noted that this description ignores the fact that claim 3 includes not only pregabalin, but also the racemate.

Nowhere in the description of the patent (taking into account the agreed-upon error) is there any reference to the racemate. Pfizer argues that a “person skilled in the art” would “infer” a reference to the racemate. I will return to this assertion. [ 91 ] With respect to “pain”, the Applicants argue at paragraph 68 of their Memorandum that the “pain” referred to in claim 3 is “chronic or persistent pain disorders; and in particular, pain disorders listed on page 1 of the '652 Patent”.

This assertion ignores the fact that the description also includes “ acute herpetic and postherpetic neuralgia” (which is also claimed in claim 13; and thus, as I have construed it, is one of the “pains” included in the more generalized term “pain” in claim 3. [ 92 ] I turn to the evidence of the inventor himself, Dr. Singh. At paragraph 10 of his affidavit, he makes it clear that his objective was to test pregabalin, as it was a compound already in development by the company that he worked for, for epilepsy. Nowhere does he state that he ever tested or even thought of testing the racemate.

From paragraphs 10 to 21 of his affidavit, Dr. Singh explains how he tested pregabalin for chronic or persistent pain. There is no mention of acute pain. He goes further in his cross-examination in answer to questions 125 to 147, where he again explains that he tested only for chronic pain and, most importantly, in answer to question 147, he says: Pregabalin only blocks or works in the presence of some nasty stimulus. It doesn’t block acute pain. [ 93 ] The evidence shows, therefore, that the inventor never tested or contemplated the testing of the racemate.

The inventor stated that pregabalin is useful only in respect of chronic or persistent pain, not acute pain. [ 94 ] The Applicants argue that the effectiveness of the racemate can be inferred as predicted from the disclosure of the patent. I disagree for reasons that I will set out in dealing with sound prediction. The Applicants make no argument in respect of the acute pain listed at page 1, and claimed in claim 13, of the patent. [ 95 ] I find that Pharmascience’s allegation that claim 3 of the '652 patent is invalid as being broader than the invention made or disclosed, is justified.

SOUND PREDICTION-UTILITY-DISCLOSURE [ 96 ] Much argument in this case focused on the question of sound prediction. The decision of the Supreme Court of Canada in Teva Canada Limited v Pfizer Canada Inc , 2012 SCC 60 ,(referred to as Viagra ) is the most recent pronouncement of that Court on the

subject. The manner in which our Courts have dealt with the matter of sound prediction has appeared to cause some to raise concerns, in Canada and elsewhere, as to how the subject is treated. [ 97 ] The Patent Act ,

section 2 , defines “invention” as: “invention” means any new and useful art, process, machine, manufacture or composition of matter, or any new and useful improvement in any art, process, machine, manufacture or composition of matter; « invention »

Toute réalisation, tout procédé, toute machine, fabrication ou composition de matières, ainsi que tout perfectionnement de l’un d’eux, présentant le caractère de la nouveauté et de l’utilité. [ 98 ] Subsection 27(1) of the Patent Act states that the Commissioner of Patents shall grant a patent to a person who has filed an application that is “in accordance with this Act” and meets “all other requirements for the issuance of a patent under this Act”.

Subsection 27(2) requires that an application for a patent “must contain a petition and a specification of the invention”. [ 99 ] Subsection 27(3) sets out what a specification must contain: Specification

(3) The specification of an invention must (

a) correctly and fully describe the invention and its operation or use as contemplated by the inventor; (

b) set out clearly the various steps in a process, or the method of constructing, making, compounding or using a machine, manufacture or composition of matter, in such full, clear, concise and exact terms as to enable any person skilled in the art or science to which it pertains, or with which it is most closely connected, to make, construct, compound or use it; (

c) in the case of a machine, explain the principle of the machine and the best mode in which the inventor has contemplated the application of that principle; and Mémoire descriptif

(3) Le mémoire descriptif doit :

a) décrire d’une façon exacte et complète l’invention et son application ou exploitation, telles que les a conçues son inventeur;

b) exposer clairement les diverses phases d’un procédé, ou le mode de construction, de confection, de composition ou d’utilisation d’une machine, d’un objet manufacturé ou d’un composé de matières, dans des termes complets, clairs, concis et exacts qui permettent à toute personne versée dans l’art ou la science dont relève l’invention, ou dans l’art ou la science qui s’en rapproche le plus, de confectionner, construire, composer ou utiliser l’invention;

c) s’il s’agit d’une machine, en expliquer clairement le principe et la meilleure manière dont son inventeur en a conçu l’application;

(

d) in the case of a process, explain the necessary sequence, if any, of the various steps, so as to distinguish the invention from other inventions.

(4) The specification must end with a claim or claims defining distinctly and in explicit terms the subject-matter of the invention for which an exclusive privilege or property is claimed.

(5) For greater certainty, where a claim defines the subject- matter of an invention in the alternative, each alternative is a separate claim for the purposes of sections 2 , 28.1 to 28.3 and 78.3.

(6) Where an application does not completely meet the requirements of subsection (2) on its filing date, the Commissioner shall, by notice to the applicant, require the application to be completed on or before the date specified in the notice.

(7) The specified date must be at least three months after the date of the notice and at least twelve months after the filing date of the application. Marginal note: What may not be patented

(8) No patent shall be granted for any mere scientific principle or abstract theorem.

d) s’il s’agit d’un procédé, expliquer la suite nécessaire, le cas échéant, des diverses phases du procédé, de façon à distinguer l’invention en cause d’autres inventions.

(4) Le mémoire descriptif se termine par une ou plusieurs revendications définissant distinctement et en des termes explicites l’objet de l’invention dont le demandeur revendique la propriété ou le privilège exclusif.

(5) Il est entendu que, pour l’application des articles 2 , 28.1 à 28.3 et 78.3, si une revendication définit, par variantes, l’objet de l’invention, chacune d’elles constitue une revendication distincte.

(6) Si, à la date de dépôt, la demande ne remplit pas les conditions prévues au paragraphe (2), le commissaire doit, par avis, requérir le demandeur de la compléter au plus tard à la date qui y est mentionnée.

(7) Ce délai est d’au moins trois mois à compter de l’avis et d’au moins douze mois à compter de la date de dépôt de la demande. Note marginale : Ce qui n’est pas brevetable

(8) Il ne peut être octroyé de brevet pour de simples principes scientifiques ou conceptions théoriques. [ 100 ] It is noteworthy to point out that : • subsection 27(3)(

a) requires that the specification must correctly and fully describe the invention and its operation and use as contemplated by the inventor • subsection 27(3)(

b) requires that the various steps in a process or method be set out in full, clear and exact terms • subsection 27(3)(

c) requires in a case of a machine , that the principles and best mode be set out

• subsection 27(3)(

d) requires in the case of a process that the various steps be set out [101] Subsection 27(4) of the Patent Act requires that the specification end with a claim or claims defining distinctly and in explicitterms the subject matter of the invention. Pharmaceutical Claims [102] In the circumstances of this case, we are dealing with a pharmaceutical substance. It is not a process or method; it is not amachine. Therefore, subsections 27(3)(b), (

c) and (

d) of the Patent Act do not apply. Only subsections 27(3)(

a) and 27(4) apply. [103] The law is clear that where a new compound, such as a pharmaceutical, is the invention, the specification must state the utilityof that compound so as to satisfy the definition of “invention” in

section 2 of the Patent Act; however, the utility need not be part of theclaim. The claim may be directed simply to the compound itself.

Where, however, the invention lies in the new use of a knowncompound, then the claim must include that use (Apotex Inc v Wellcome Foundation Ltd, (FCA), [2001] 1 FC 495,at para 81 (FCA); aff’d 2002 SCC 77 , [2002] 4 SCR 153). [104] Where the invention lies in the selection of certain compounds out of a group of known compounds as being exceptionallyuseful for the known purpose, the claim must be clearly directed to those compounds as selected, and all such compounds should exhibitthe exceptional characteristics ( Re I.G.

Farbenindustrie, infra.). [105] Lastly, where a claim is directed to a large number of compounds, all compounds within that number, possibly with theexception of de minimis, must possess the utility as set out in the specification and, if claimed, as set out in the claim ( Olin Matheson,infra.). Invention [106] The act of invention is not defined in the Patent Act.

Section 2 defines an “invention” as “new and useful”. [107] Subsection 28.1 defines a “claim date” as the date of filing an application in Canada or filing in a foreign country in respect ofwhich priority up to twelve months may be claimed. Subsection 28.2 states, in respect of the requirement that the subject matter be“new”, that it shall not have been “disclosed” by any third party before the claim date.

Subsection 28.3 requires that in order that therebe an “invention”, the subject matter shall not, as of the claim date, have been “obvious”. [108] Thus, the act of invention does not normally give rise to an inquiry as to the activities of the inventor. All that is relevant is that,as of the “claim date”, the subject matter has not been previously disclosed, and is not obvious. [109] There are, however, situations where the act of invention may become relevant. One is where persons other than those named asinventors, or in addition to those so named, seek to be substituted or added as inventors.

There the activities of the named inventors andthose others may well come under scrutiny by the Commissioner of Patents or the Court. [110] Another exception arose under the provisions of the Patent Act as it existed prior to the October 1, 1989 amendments. There theact of invention would become relevant in considering obviousness, as obviousness was to be considered as of the “date of theinvention”.

While that date, in the absence of other evidence, was presumed to be the filing date of the application in Canada - or thepriority date, if any - a patentee may have wished to establish an even earlier date; for instance, so as to make a certain interveningpublication irrelevant as to the issue of obviousness. In such a circumstance, the Courts have said that the “date of the invention” is thedate when the invention was reduced to a definite and practical shape by building it or by fully describing how it will be practiced and showing that it has utility (e.g.

Weatherford Canada Inc v Corlac Inc (2010), 2010 FC 602 , 84 CPR (4th) 237, at para 239, aff’d 2011 FCA 228 , 95 CPR (4th) 101, (FCA) leave to appeal to SCC denied). [111] Another instance, arising from the pre-October 1, 1989 provisions of the Patent Act, was conflict proceedings where a patent(unlike the new provisions where a patent is granted to the first person to file for a patent on the same invention) was granted to the “firstto invent”.

Where two or more persons filed applications for a patent for the same invention, the Commissioner of Patents, andsubsequently the Courts, were required to determine who was the “first to invent”; thus, be the person entitled to the patent. The sametest as to date of invention as discussed previously, applies.

History of the Jurisprudence [ 112 ] With this background, the relevant jurisprudence respecting patents directed to pharmaceutical compounds and the like, and the emergence of the “sound prediction” concept can be examined. [ 113 ] A good starting place is the decision of Justice Maugham of the English Chancery Division in In the Matter of I.G. Farbenindustrie A.G.’s Patent , (1930), 47 RPC 289. In that case, Farbenindustrie had been granted a patent for the manufacture of dyestuff by coupling chemical A with chemical B.

Another company, Imperial Chemical, sought to invalidate the patent on a variety of grounds, including arguing that not all members of the family of chemicals A and B would achieve the resulting dyestuff. Maugham J held the patent to be invalid on this as well as other grounds.

He said as reported at pages 322 to 323: Three general propositions may, however, I think, be asserted as true: - First, a selection patent to be valid must be based on some substantial advantage to be secured by the use of the selected members. (The phrase will be understood to include the case of a substantial disadvantage to be thereby avoided.) Secondly, the whole of the selected members must possess the advantage in question. Thirdly, the selection must be in respect of a quality of a special character which can fairly be said to be peculiar to the selected group.

The first proposition is plain (see the statement of Mr. Justice Parker in Clyde Nail Co. Ld. V. Russell, (1916) 33 R.P.C. 291, at p. 306). I will add that this condition must not be assimilated with the doctrine of utility as applied to an originating patent. In such a patent there may well be invention without utility. In a selection patent the condition that there must be a substantial advantage attributable to the use of the selected members is inherent in the so-called invention.

The second proposition is derived from the circumstances that, if the selection embraces selected members which do not possess the alleged advantages, the selection is defective and the patent would be misleading and would also fail for insufficiency and non-utility. It is not, however, intended to suggest that a few exceptions here and there would be regarded as invalidating to the patent. The third proposition requires a little explanation.

If there are five thousand possible members of the group, and a hundred have been selected as possessing some new and definite advantage, it is not intended to assert that such a selection patent would be bad if it were shown as the result of further research that there existed another hundred members possessing the same advantage. If, on the other hand, it were to be established that there were a thousand unselected members which possessed the same advantage, I doubt very much whether the patent could be sustained. The quality must be of a special character.

It must not be one which those skilled in the art will expect to find in a large number of the members. It would be rash to attempt a closer definition; for the question is ultimately one of appreciation. Returning to the same old fashioned metaphor I would say that the citadel must be defended, and that there is no reward if the gates have been opened at the first blast of the trumpet. I must add a word on the subject of the drafting of the specification of such a patent.

It should be obvious, after what I have said as to the essence of the inventive step, that it is necessary for the patentee to define in clear terms the nature of the characteristic which he alleges to be possessed by the selection for which he claims a monopoly. He has in truth disclosed no invention whatever if he merely says that the selected group possesses advantages. Apart altogether from the question of what is called sufficiency, he must disclose an invention; he fails to do this in the case of a selection for special characteristics, if he does not adequately define them.

The cautions repeatedly expressed in the House of Lords as regards ambiguity have, I think, special weight in relation to selection patents. (Natural Colour etc. Ld. V. Bioschemes Lt., (1915) 32 R.P.C. 256, at p. 266; and see British Ore etc. Ld. V.

Minerals Separation Ld., (1910) 27 R.P.C. 33, at p. 47.) I will summarize the conclusion at which I have arrived by saying that in a selection patent the inventive step lies in the selection for a useful and special property or characteristic adequately defined; and this is the proposition which has to be kept in mind in considering the application to amend and the Petition for revocation. [ 114 ] Here we have the genesis of the current doctrines respecting “selection” patents. [ 115 ] Next comes the decision of the English Court of Appeal in May & Baker Limited et al v Boots Pure Drug Company Limited (1950), 67 RPC 23.

In that case, the Court was asked to invalidate a patent which claimed a large number of compounds, sulpha- thiozoles, which were said to “find application in therapeutics”. It was argued that not all such compounds could have such utility. The patentee sought to amend the patent (a procedure available in the United Kingdom, but not Canada) to restrict the patent to two compounds only. The Court refused the amendment, stating that the result would be a different invention.

In his speech, as reported at page 50, Lord MacDermott said: 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 make 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. [ 116 ] We see in this paragraph the genesis of “sound prediction”.

Can an inventor “have found some law or principle by which he may predicate therapeutic effect in advance” for “each of the various new products”? [ 117 ] This speech of Lord MacDermott was recast by the English barrister Sir Lionel Heald, as recited by Justice Graham in Olin Matheson Chemical Corporation et al v Biorex Laboratories Limited et al , [1970] RPC 157. That case involved a class of pharmaceutical compounds said to have therapeutic effect. It was alleged that the claims were invalid as being directed to a large class, not all of which could be said to have therapeutic effect.

The Court found the patent to be valid. [ 118 ] Justice Graham used the words “sound prediction” in repeating Sir Lionel Heald’s

summary of what Lord MacDermott said in May & Baker at page 182 of the report: On several occasions the argument appeared to go as far as stating that it was impossible in a drug patent such as this to have a valid claim unless the body or all the bodies covered by such claim had actually been tested on man and proved to have at least some therapeutic usefulness as drugs.

However, Sir Lionel submitted that the question of “fairly based” and consideration must be judged after looking at the specification and all the surrounding circumstances, and after examination of a number of cases which he cited, and particularly Lord MacDermott’s speech in the House of Lords in May & Baker case (1950) 67 R.P.C. 23 at 50.

Sir Lionel very fairly summarized his position in the following words: “If it is really possible, according to the evidence, to make a sound prediction about a certain area, then prima facie it would be reasonable that the patentee should have a claim accordingly, but that is not the case according to the evidence in this field.” This, as will be seen later, I have found to be a most helpful statement in considering the difficult questions of consideration and width of claim.

Sir Lionel’s argument, on its face, logically, if it is right, must apply to all claims in the specification, whether of a general formula type or to specific compounds, except such as have actually been tested and found to be useful in man – for example, trifluopromazine.

It follows, of course, that the basis of fact which must be proved before the argument can be applied successfully is that it is impossible fairly to predict that the various compounds included in areas of several claims in question are likely to have any utility as drugs until they have actually been so tested. [ 119 ] Hence, the words “sound prediction”. [ 120 ] Justice Graham in Olin Matheson continued to consider the arguments in much the same way as our Courts do today. At pages 192 to 193 of the reported case, he wrote:

(1) The construction of the claim is the first consideration, and if, as here, the claim is for a large class of chemical bodies as such, then it is on this basis that the consideration must first be tested. If it is shown that some bodies falling within such claim have no utility, then, apart possibly from a de minimis case where there are only a few exceptions, such as Maugham, J., had in mind in the case of I.F. Farbenindustrie A.G.’s Patents (1930) 47 R.P.C. 289 at 323, line 14, the claim is bad. It may, of course, be possible to amend it so as to cut out the useless cases, but that is a different question.

But where, as here, the objection of inutility was originally pleaded and subsequently withdrawn – and it must be remembered the onus is on the defendants to show that the patent is invalid and not on the plaintiffs to show that it is valid – it is quite impossible for the defendants, in the absence of an admission to that effect, to argue successfully that there is any body covered by the claim which does not have utility of some sort, whether it be of a therapeutic or other nature. If the defendants had been able to show that there were some bodies within the claim which had no utility at all or could not be

used as drugs because they were too toxic, it would have been perfectly simple for them to have proved it by experiment or otherwise.

(2) From the point of view of the public and patentees it is desirable that research in the drug or other fields,, as the case may be,should continue. In the drug field in particular research is very expensive and the number of “winners” found is only a minuteproportion of those synthesized and tested. Once a winner is found, however, it is very common also to find that bodies more or lessclosely related to it have the same or even greater activity. Here, for example, trifluoperazine is some five times more active thanchlorpromazine, and fluphenazine some twenty times more active than chlorpromazine.

All are phenothiazine derivatives, all substitutedin the “2” position, trifluoperazine and fluphenazine having the new – CF3 substitution rather than the – CI substitution ofchlorpromazine, and therefore falling within claim 1. Furthermore, a difference between five and twenty times the activity ofchlorpromazine is achieved in the case of fluphenazine by only the small alteration of the – NCH3 radical at the end of the chain oftrifluoperazine into – NCH2 CH2 OH – in other words one H atom in – NCH3 is replaced by – CH2 OH.

Unless, therefore, theoriginal inventor of the – CF3 substitution can properly be given reasonably broad cover, it is likely that soon after others hear of hissuccess similar bodies will be made by others having as good or better activity. Unless he can control such activities, any reward he mayobtain for his invention and research is likely to be of little value.

(3) This last consideration must be balanced by another, which is that his claim must not be so broad as unjustifiably to stifleresearch by others – but here also it must be remembered that the “abuse of monopoly” sections 37 to 42 in the Act in proper cases willenable someone who makes a discovery or wishes to sell something within the field covered by another’s claim to obtain a licence uponreasonable terms from such other person.

Furthermore, if, as here, it is necessary for a drug company, as potential infringer of twopatens belonging to two other proprietors, to obtain two compulsory licences, one under each patent, it is to be expected that theComptroller will apportion the total royalty which he considers proper equitably between the two patentees having regard to all therelevant circumstances of the case, whilst at the same time ensuring that the potential infringer does not have to pay tribute twice over orat an exorbitant rate, see

section 41. Activities or the genuine research worker and of a drug company, which result in the making of, ordesire to use, an invention already covered by the claim of someone else’s earlier patent are therefore in proper cases safeguarded. Thecompulsory licence already grated to the defendants in this case under patent No. 813,861 is an example of the working of these sections. Where, then, is the line to be drawn between a claim which goes beyond the consideration and one which equiparates with it?

Inmy judgment this line was drawn properly by Sir Lionel when he very helpfully stated in the words quoted above that it depended uponwhether or not it was possible to make a sound prediction. If it is possible for the patentee to make a sound prediction and to frame aclaim which does not go beyond the limits within which the prediction remains sound, then he is entitled to do so.

Of course, in so doinghe takes the risk that a defendant may be able to show that his prediction is unsound or that some bodies falling within the words he hasused have no utility or are old or obvious or that some promise he has made in his specification is false in a material respect; but if,when attacked, he survives the risk successfully, then his claim does not go beyond the consideration given by his disclosure, his claim isfairly based on such disclosure in these respects, and is valid. [121] All of this is reflected in the decision of the Supreme Court of Canada, Apotex Inc v Wellcome Foundation Limited, 2002 SCC77 , [2002] 4 SCR 153 (referred to as AZT), which will be discussed later. [122] First, the decision of the Supreme Court of Canada in Monsanto Company v The Commissioner of Patents, (SCC), [1979] 2 SCR 1108 should be considered.

In that case, Monsanto was seeking a patent claiming a class of some 126 compoundssaid to prevent premature vulcanization of rubber. The specification disclosed the preparation of only three of those compounds. TheCommissioner of Patents refused to grant a patent on the basis that the disclosure of only three compounds could not justify a claim toone hundred and twenty-six. The Federal Court of Appeal upheld that refusal. The Supreme Court reversed that decision.

It did so, on thebasis that the Commissioner (his decision is referred to as that of the Board) had the onus of justifying a refusal; the applicant did nothave the onus of justifying sound prediction. [123] Justice Pigeon wrote the decision of the Supreme Court.

At page 1118 he wrote: Although the report of the Board is quite lengthy, in the end with respect to claim 9 all it says after stating the principle with which Iagree, is that a claim has to be restricted to the area of sound prediction and “we are not satisfied that three specific examples areadequate. [124] At page 1119 he wrote: I have underlined by law (section 42 of the Patent Act) to stress that this is not a matter of discretion: the Commissioner has to justify anyresult.

[125] At pages 1121 to 1122 he wrote: Under that

section the Commissioner is instructed to refuse the patent when “satisfied that the applicant is not by law entitled” to it.Here what he has said in approving the decision of the Board is in effect “I am not satisfied you are entitled to it”. In my opinion theCommissioner cannot refuse a patent because the inventor has not fully tested and proved it in all its claimed applications. This is whathe has done in this case by refusing to allow claims 9 and 16 unless restricted to what had been tested and proved before the applicationwas filed.

If the inventors have claimed more than what they have invented and included substances which are devoid of utility, theirclaims will be open to attack. But in order to succeed, such attack will have to be supported by evidence of lack of utility.

At present thereis no such evidence and there is no evidence that the prediction of utility for every compound named is not sound and reasonable. [126] Thus, the Monsanto case dealt with sound prediction, in the context of who bore the burden of demonstrating sound predictionwhen seeking the grant of a patent, the Commissioner or the applicant? [127] Now I turn to the AZT case; first with reference to the decision of the trial judge, Wetston J, as reported, (1998), (FC), 79 CPR (3d) 193. The patent claimed a drug named AZT, used in the treatment of AIDS.

Several issues were raised, whichmade the making of the invention and the date of the invention relevant.

One issue was whether the correct inventors were named;another was whether, as of the “date of the invention”, the inventors had, in fact, made the invention. [128] Wetston J began by writing at paragraphs 34 and 35 of his Reasons: 34 As to the matter of timing, there are several points in the patent process which are of possible relevance to considerations ofvalidity, including: the date of invention, the application date, the priority date, and the date the patent is issued. 35 The date of invention is presumed to be the filing date, or the date the original priority application was filed.

However, an inventoris entitled to claim priority based on an invention date prior to the first filing date. Usually an inventor will claim an earlier date wherea competing inventor is also seeking to obtain a patent, although the entitlement is not limited to these circumstances. The test fordetermining an earlier invention date is, "the date at which the inventor can prove he has first formulated, either in writing or verbally, adescription which affords the means of making that which is invented": Christiani & Nielsen v.

Rice, (SCC), [1930]S.C.R. 443 at 456. [129] The ground of attack as to whether an invention was made as of the date of the invention was set out at paragraphs 77 and 78 ofhis Reasons: 77 A&N allege that the patent is invalid on the grounds that, at the date of invention, the inventors did not have an invention withinthe meaning of s. 2 of the Act. Similar to the arguments under subject matter, a key question in this line of attack is what constitutes aninvention for the purposes of s.2. As previously stated, the invention herein is not a chemical composition, process or formulation.

It is anew use for a previously known compound. The alleged inventive step was devising the use of AZT as a medicine in respect of AIDS andrelated illnesses. 78 A&N argue that there is no invention at the claimed date of invention and that the claims are overbroad at the claimed date ofinvention. A&N argue that the claims may not exceed the invention made or the invention disclosed. In other words, they assert that thepatent claims more than was invented and, secondly, that the claims are greater than the invention described in the specification.

Theycontend that a patentee must have more than stated utility, it must know there is utility. At the claimed date, they contend that theinventors only had an idea, hypothesis or theory. A&N submit, therefore, that at the claimed date of invention the named inventorscould demonstrate utility in one of two ways. Namely, they could have: 1) demonstrated utility at that time; or 2) had a sound basis forpredicting the utility of the compound: Monsanto Co. v.

Commissioner of Patents, (SCC), [1979] 2 S.C.R. 1108 at1117. [130] Then, at paragraphs 84 to 87 of his Reasons, Wetston J set out the basic principles of law respecting the act of inventing: 84 The act of inventing may be different in different circumstances: Barrigar, Canadian Patent Act, Annotated, Canada Law Book(1989), p. 5. The range of expertise required in the pharmaceutical field, the nuances between theoretical and clinical proof, and theunderlying public policy concerns of the safe and effective development of medicines, all serve to make utility in the pharmaceutical area

highly complex. Certainly, the inventor of such items as a paper clip or an elastic band will not be required to call upon a multitude ofspecialists, or engage in months or years of intensive labratory and clinical tests in order to claim a useful invention under s. 2 of theAct. The task incumbant upon such inventors may indeed be no greater than deducing and setting down in writing conclusions as to theeffect that a loop of metal or an elastic band will bind paper. However, it is clear that more is required of an invention that is a new usefor a known compound in the pharmaceutical field.

Thus, the question is, what is required under s.2 in such circumstances? 85 The determination of whether an invention has utility for the purposes of s. 2 of the Act is a question of fact which the Courtdetermines on the basis of a person or persons having the technical skills and knowledge as required. Canadian patent law requires thatan inventor reduce an idea to a definite and practical shape before it can be said that an invention has been made: Permutit Co. v.Borrowman, (UK JCPC), [1926] 4 D.L.R. 285 at 287 (J.C.P.C.).

An inventor will be able to demonstrate that theinvention will work, or will have reduced it to a definite and practical shape, by either building it, if an apparatus, using the process, orfully describing how it is to be practiced: Ernest Scraggs & Sons Ltd. v. Leesona Corp., supra. There is no patent protection availablefor a discovery or mere idea: Comstock Canada v. Electec Ltd. (1991), 38 C.P.R. (3d) 29 at 51 (F.C.T.D.). Likewise, a mere hypothesiswhich has not been tested will not be patentable: Farberwerke Hoechst A/G v. Commissioner of Patents, (CA EXC),[1966] Ex. C.R. 91, at page 97.

To that end, the idea which leads to the invention is not part of the invention: Reynolds v. Herbert Smith& Co. Ltd. (1903), 20 R.P.C. 123 at 127. Sound Prediction 86 A&N's submission that the doctrine of sound prediction should be applied seems compelling on its face. However, whether thedoctrine should be applied is not immediately apparent. Indeed, as stated, Glaxo contends that the doctrine does not apply. Therefore, Ishall begin by considering whether or not the doctrine will be beneficial to resolve the question in these circumstances. 87 The doctrine of sound prediction arose where inventors were claimin

[…]