UNIV. OF ROCHESTER. G.D. SEARLE & CO., MONSANTO and PFIZER. 358 F.3d 916 (Fed. Cir. 2004)

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1 UNIV. OF ROCHESTER v. G.D. SEARLE & CO., MONSANTO and PFIZER 358 F.3d 916 (Fed. Cir. 2004)

2 Background ("NSAIDs") such as aspirin, ibuprofen, ketoprofen, and naproxen are believed to function by inhibiting the activity of enzymes called cyclooxygenases. Cyclooxygenases catalyze the production of a molecule called prostaglandin H 2, which is a precursor for other prostaglandins that perform various functions in the human body

3 Continue. COX-1 is expressed (i.e., produced biologically) in the gastrointestinal tract, where it is involved in the production of prostaglandins that serve a beneficial role by, for example, providing protection for the stomach lining. COX-2 is expressed in response to inflammatory stimuli, and is thought to be responsible for the inflammation associated with diseases such as arthritis NSAIDs inhibit both COX-1 and COX-2, and as a result they not only reduce inflammation, but also can cause undesirable side effects such as stomach upset, irritation, ulcers, and bleeding.

4 Claim 1 : The '850 patent A method for selectively inhibiting PGHS-2 activity in a human host, comprising administering a non-steroidal compound that selectively inhibits activity of the PGHS- 2 gene product to a human host in need of such treatment. Claim 5 : A method for selectively inhibiting PGHS-2 activity in a human host, comprising administering a non-steroidal compound that selectively inhibits activity of the PGHS- 2 gene product in a human host in need of such treatment, wherein the activity of the non-steroidal compound does not result in significant toxic side effects in the human host.

5 Continue. Claim 6 : A method for selectively inhibiting PGHS-2 activity in a human host, comprising administering a non-steroidal compound that selectively inhibits activity of the PGHS-2 gene product in a human host in need of such treatment, wherein the ability of the non-steroidal compound to selectively inhibit the activity of the PGHS-2 gene product is determined by:

6 Continue. All eight claims are directed to methods "for selectively inhibiting PGHS-2 activity in a human host" by "administering a non-steroidal compound that selectively inhibits activity of the PGHS-2 gene product to [or in] a human host in need of such treatment."

7 850 patent is invalid for written description and enablement requirements of 35 U.S.C. 112 Rochester asserts three grounds of error on appeal it argues that the district court erred by granting Pfizer's motion for summary judgment of invalidity for lack of written description it argues that the court erred by granting Pfizer's motion for summary judgment of invalidity for lack of enablement the court erred by denying its cross-motion for summary judgment with regard to written description

8 35 U.S.C. 112 requirement (1) "[t]he specification shall contain a written description of the invention" (2) "[t]he specification shall contain a written description... of the manner and process of making and using it [i.e., the invention] in such full, clear, concise, and exact terms as to enable any person skilled in the art to which it pertains, or with which it is most nearly connected, to make and use the same" (3) "[t]he specification... shall set forth the best mode contemplated by the inventor of carrying out his invention."

9 The CCPA held that.. The court observed that the claimed compound was not described in the specification Would not "convey clearly to those skilled in the art, to whom it is addressed It did not teach the specific compound

10 850 patent fails to The '850 patent does contain substantial description of the cyclooxygenases, including the nucleotide sequences of coding and promoter regions of the genes that encode human COX-1 and COX-2 and a comparison of those sequences '850 patent, figs. 6A-6B, 10A-10D, and 11A-11C. The patent also describes in detail how to make cells that express either COX-1 or COX-2, but not both

11 Continue. as well as "assays for screening compounds, including peptides, polynucleotides, and small organic molecules to identify those that inhibit the expression or activity of the PGHS-2 gene product; and methods of treating diseases characterized by aberrant PGHS-2 activity using such compounds the '850 patent does not disclose just "which `peptides, polynucleotides, and small organic molecules' have the desired characteristic of selectively inhibiting PGHS-2."

12 CONCLUSION Because the court did not err in holding the '850 patent to be invalid for failing to comply with the written description requirement of 35 U.S.C , and in granting summary judgment in favor of Pfizer on that ground, the decision of the district court is Affirmed.

13 Application Of RUSCHIG (1967)

14 Claim N-(p-chlorobenzenesulfonyl) -n'- propylurea: chlorpropamide Not named or identified by formula in the specification One would have to make a choice between several variables Reagents for the preparation of chlorpropamide are listed

15 General disclosure of the application encompasses half a million possible compounds Narrowest genus including the claimed species encompasses more than a thousand compounds Specific claims to single compounds require reasonably specific supporting disclosure

16 Naming is not essential Eleven processes for making the many compounds of the invention are disclosed, five of which employ an "alkylamine." (R2) To lead to claim 13, R must be hydrogen and R1 must be chlorine and the alkylamine, R2, must be propylamine Taught that the primary amine could be a primary butylamine or another primary alkylamine

17 One skilled in the art could see that "if n- butylamine is a reactant, then ethylamine, n- propylamine, etc., Are also possible reactants." This is not a guide to the use of n- propylamine.

18 It is an old custom in the woods to mark trails by making blaze marks on the trees. It is no help in finding a trail or in finding one's way through the woods where the trails have disappeared or have not yet been made, which is more like the case here to be confronted simply by a large number of unmarked trees. Appellants are pointing to trees. We are looking for blaze marks which single out particular trees. We see none.

19 Best guide is the activity table in which in eight of the ten compounds, R2 is a primary alkyl radical One of them, n-(4- chlorobenzenesulphonyl)-n'n-butyl urea is a homolog of the compound of claim 13 One skilled in the art would be enabled by the specification to make chlorpropamide

20 Presumes some motivation for wanting to make the compound in preference to others Question is not whether he would be so enabled but whether the specification discloses the compound specifically, as something appellants actually invented

21 GLAXO INC. V. NOVOPHARM LTD.

22 Background In 1976, Glaxo synthesized ranitidine, obtained patent No. 4,128,658 ('658 patent) on December 5, The '658 patent claims a number of structurally similar compounds, including ranitidine and its hydrochloride salt.

23 Background Synthesis of Crystalline ranitidine hydrochloride that was visibly different from all previous batches of the salt Infra-red (IR) spectroscopy and x-ray powder diffraction showed that the new product was a crystalline form, or polymorph, of ranitidine hydrochloride

24 Background Form 2 had better filtration and drying properties Form 2 was hampered by poor flow properties Azeotroping process developed to overcome these problems.

25 Background United States Patent No. 4,521,431 ('431 patent) issued. The '431 patent claims a specific crystalline form of the compound ranitidine hydrochloride

26 The litigation. ANDA- Novopharm admitted that infringement existed but Patent invalid because anticipated by 658 Patent. Court rejected because the polymorph variety had significant commercial advantages.

27 Best mode Glaxo knew of the Azeotroping method but failed to disclose it. Court held that the inventor himself did not know. The method developed by other employees working in a different department.

28 Significant dissent With this case, the court blesses corporate shell games resulting from organizational gerrymandering and willful ignorance by which one can secure the monopoly of a patent while hiding the best mode of practicing the invention the law expects to be made public in return for its protection

29 Learning When your invalidity charge is based on the assertion of a fact, then you must provide clear and compelling evidence as to the existence of that fact Novopharm failed to do that It may be difficult to prove a best mode violation because the inquiry involves an analysis of the state of mind of the inventor and not the company

30 Learning A method of producing the claimed compound which relates to a scale up or commercialization process may not have to be disclosed in the patent It does not matter even if the company has deliberately screened the inventor from the process The practical realities of the corporate scenario and the entire research & development and commercial production process must be taken into account

31 Learning When you are filing a Para IV for a polymorph, you might be better of coming up with a noninfringing crystal structure rather than trying to prove the invalidity of the patent There may be a basis for saying that a polymorph claim is invalid for non-enablement, but you must have clear evidence to prove that