Ex Parte Moinet et alDownload PDFBoard of Patent Appeals and InterferencesJul 26, 201010497491 (B.P.A.I. Jul. 26, 2010) Copy Citation UNITED STATES PATENT AND TRADEMARK OFFICE __________ BEFORE THE BOARD OF PATENT APPEALS AND INTERFERENCES __________ Ex parte GERARD MOINET, DOMINIQUE MARAIS, and PHILIPPE MAIZERAY __________ Appeal 2010-000898 Application 10/497,491 Technology Center 1600 __________ Before CAROL A. SPIEGEL, TONI R. SCHEINER, and STEPHEN WALSH, Administrative Patent Judges. WALSH, Administrative Patent Judge. DECISION ON APPEAL1 This is an appeal under 35 U.S.C. § 134(a) involving claims to a method for treating inflammation. The Patent Examiner rejected the claims on the ground of obviousness. We have jurisdiction under 35 U.S.C. § 6(b). We reverse. 1 The two-month time period for filing an appeal or commencing a civil action, as recited in 37 C.F.R. § 1.304, or for filing a request for rehearing, as recited in 37 C.F.R. § 41.52, begins to run from the “MAIL DATE” (paper delivery mode) or the “NOTIFICATION DATE” (electronic delivery mode) shown on the PTOL-90A cover letter attached to this decision. Appeal 2010-000898 Application 10/497,491 2 STATEMENT OF THE CASE The invention “relates to the use of a 4-oxobutanoic acid derivative for the preparation of a pharmaceutical composition for treating inflammation.” (Spec. 1, ll. 3-5.) “The inflammation treated according to the invention may be associated with pathologies of insulin-resistant metabolic syndrome, with pathologies resulting from diabetes, for instance retinopathy, nephropathy, neuropathy, micro- and macro-angiopathy, hypertension or atherosclerosis.” (Id. at 3, ll. 29-32.) Claims 2, 3, 10, 11, 13, 15, 17-19, 22 and 23 are on appeal.2 Claim 2 is representative; the full text appears in the Claims Appendix. (App. Br. 9.) Claim 2 lists several kinds of inflammation to be treated, and lists several compounds that may be used. At the start of examination, the Examiner required Appellants to elect a type of inflammation and a species of compound, “to which the claims shall be restricted if no generic claim is finally held to be allowable.” (Office action, July 17, 2007, page 4.) Appellants elected diabetic neuropathy and 2-benzyl-4-(4-fluorophenyl)-4- oxobutanoic acid. (Response, July 31, 2007, page 7.) Editing claim 2 to focus on the subject matter elected for examination yields a shortened version of the claim: 2. A method for treating inflammation, which inflammation is diabetic neuropathy . . . comprising administering to a subject in need thereof an effective amount of . . . 2-benzyl-4-(4- fluorophenyl)-4-oxobutanoic acid . . . or a salt thereof. 2 According to Appellants’ Brief, claims 1, 4-9, 12, 16, 20 and 21 were cancelled, and claim 14 was withdrawn from consideration. (App. Br. 1-2.) Appeal 2010-000898 Application 10/497,491 3 The Examiner rejected claims 2, 3, 10, 11, 13, 15, 17-19, 22 and 233 under 35 U.S.C. § 103(a) as unpatentable over Pharmacia & Upjohn S.O.A. (WO 97/17317)4 and Lal5. (Final Rej. 2.) OBVIOUSNESS The Issue The Examiner’s position is that Pharmacia taught treating inflammation with 4-phenyl-4-oxo-butanoic acid derivatives. (Ans. 3.) According to the Examiner, it would have been obvious to pick and choose various substituents from Pharmacia’s general formula of claim 1, “given the teaching that the class of compounds has similar kynurenine-3-hydoxyase [sic] inhibiting activity.” (Id.) Pharmacia disclosed compounds such as 2- benzyl-4-(3’,4’-dichlorophenyl)-4-oxo-butanoic acid, having two halogens (chlorine), in contrast to Appellants’ elected compound which has one atom of fluorine. (Id.) The Examiner found that “replacing two halogens for a different halogen would be expected to have the same activity,” and that the elected species therefore would have been obvious. (Id. at 4.) In the absence of an allegation of an unexpected result, the Examiner concluded that any kynurenine hydroxylase inhibitor within Pharmacia’s generic formula, including Appellants’ elected species, would have been obvious. 3 We list the claims rejected in the Final Rejection. The Examiner’s Answer has apparent typos adding claims 20 and 21 and omitting claim 23. (Ans. 3.) Appellants’ Brief tracks the claims listed in the Final Rejection (App. Br. 2), and the Answer’s “Status of Claims” agrees with Appellants’ statement (Ans. 2). 4 WO 97/17317, filed by Pharmacia & Upjohn S.O.A., published May 15, 1997. 5 US 6,060,250, issued to Preeti Lal et al., May 9, 2000. Appeal 2010-000898 Application 10/497,491 4 The Examiner found that although “Pharmacia … does not relate inflammations of the brain to diabetic neuropathy,” Lal taught treating diabetic neuropathy by inhibiting the kynurenine metabolic pathway, and it would have been obvious to use a Pharmacia compound, modified as the Examiner suggested, in Lal’s treatment method. (Id.) Appellants contend that the rejection did not provide a reason “why one of ordinary skill in the art would have picked the allegedly closest compound to the claimed invention as the lead compound as a candidate for modifications.” (App. Br. 5.) Appellants further contend that there was no specific guidance to convert Pharmacia’s benzyl-4-(3’,4’-dichlorophenyl)-4- oxo-butanoic acid to Appellants’ 2-benzyl-4-(4-fluorophenyl)-4-oxobutanoic acid. (Id. at 8.) Appellants argue that Lal does not support the Examiner’s conclusions. (Reply 4-5.) Specifically, Appellants dispute that Lal taught inhibiting the kynurenine pathway with compounds like Pharmacia’s. (Id.) According to Appellants, Lal instead taught administering HUTRAN, or a derivative thereof, to treat neurological disorders. (Id. at 5, quoting Lal, col. 20, ll. 49-53.) The issues with respect to this rejection are: whether there was a reason to select benzyl-4-(3’,4’-dichlorophenyl)- 4-oxo-butanoic acid from the compounds in Pharmacia’s claim 10; whether there was a reason to convert the compound selected from Pharmacia’s claim 10 to 2-benzyl-4-(4-fluorophenyl)-4-oxobutanoic acid; and whether the evidence supports the Examiner’s findings concerning the content of the Lal disclosure. Appeal 2010-000898 Application 10/497,491 5 Findings of Fact 1. Pharmacia taught 4-phenyl-4-oxo-butanoic acid derivatives for use as kynurenine-3-hydroxylase inhibitors in the prevention and treatment of neurodegenerative disease. (Pharmacia, Abstract.) 2. Pharmacia disclosed generic formula (I) in which hydrogen and halogen were potential substituents, among others. (Id., claim 1.) 3. Pharmacia claimed the compound benzyl-4-(3’,4’-dichlorophenyl)-4- oxo-butanoic acid, among others. (Id., claim 10.) 4. The Examiner found that it would be obvious to substitute[] halogens, i.e. fluorine for a chlorine, as substituent Y. These substitutions would have been obvious to one of ordinary skill in the art because the halogens are not reactive and simply stabilize the aromatic ring. Therefore, replacing two halogens for a different halogen would be expected to have the same activity. (Ans. 3-4.) 5. The Examiner found that Lal taught that “inhibition of kynurenine metabolic pathway stops the conversion of kynurenine to kynurenic acid, which is an antagonist of the N-methyl-D-asparta[t]e (NMDA) receptor in the brain.” (Ans. 4.) 6. The Examiner found that Lal disclosed using compounds that stop the conversion of kynurenine to kynurenic acid to treat diabetic neuropathy. (Id.) 7. In the “Background of the Invention,” Lal disclosed that the enzyme glutamine-phenylpyruvate aminotransferase, aka glutamine transaminase (GTK) catalyzes the conversion of kynurenine to kynurenic acid, and that “[k]ynurenic acid . . . is an antagonist of the Appeal 2010-000898 Application 10/497,491 6 N-methyl-D-aspartate (NMDA) receptor in the brain and may exert a neuromodulatory function.” (Lal, col. 1, ll. 22-32.) 8. In the “Background of the Invention,” Lal disclosed that “the enzyme kynurenine/α-aminoadipate aminotransferase (AadAT) catalyzes … the reversible conversion of α-aminoadipate and α-ketoglutarate to α- ketoadipate and L-glutamate. . . . AadAT also catalyzes the transamination of kynurenine acid to kynurenic acid.” (Id. at col. 1, ll. 50-56.) 9. Lal stated that its invention “features substantially purified polypeptides, human transferases, referred to collectively as ‘HUTRAN’ and individually as ‘HUTRAN-1’, ‘HUTRAN-2’, and ‘HUTRAN-3.’” (Id. at col. 2, ll. 40-44.) 9. Lal taught that “HUTRAN or a fragment or derivative thereof may be administered to a subject to treat or prevent a neurological disorder.” (Id. at col. 20, ll. 33-35.) 10. Diabetic neuropathy was among the neurological disorders that Lal listed for treatment. (Id. at col. 20, l. 61.) 11. According to Lal: a) “HUTRAN-1 activity may be demonstrated by the ability to convert L-phenylalanine and α-keto-γ-methiolbutyrate to phenylpyruvate and L-methionine” (id. at col. 38, ll. 55-57); b) “HUTRAN-2 activity may be demonstrated by the ability to convert L-glutamate and α-ketoadipate to α-aminoadipate and α- ketoglutarate” (id. at col. 39, ll. 2-4); and c) “HUTRAN-3 activity may be demonstrated by the ability to m ethylate hnRNP A1 protein in vitro” (id. at col. 39, ll. 25-26). Appeal 2010-000898 Application 10/497,491 7 Principles of Law “Rejections on obviousness grounds cannot be sustained by mere conclusory statements; instead, there must be some articulated reasoning with some rational underpinning to support the legal conclusion of obviousness.” In re Kahn, 441 F.3d 977, 988 (Fed. Cir. 2006), cited with approval in KSR Int’l Co. v. Teleflex Inc., 550 U.S. 398, 417-18 (2007). When identifying a reason for modifying a prior art compound, “‘it is sufficient to show that the claimed and prior art compounds possess a ‘sufficiently close relationship . . . to create an expectation,’ in light of the totality of the prior art, that the new compound will have ‘similar properties’ to the old.’” Eisai Co. Ltd. v. Dr. Reddy’s Labs., Ltd., 533 F.3d 1353, 1357 (Fed. Cir. 2008) (quoting Aventis Pharma Deutschland GmbH v. Lupin, Ltd., 499 F.3d 1293, 1301 (Fed. Cir. 2007) (quoting In re Dillon, 919 F.2d 688, 692 (Fed. Cir. 1990)). An obviousness rejection based on similarity in chemical structure and function entails the motivation of one skilled in the art to make a claimed compound, in the expectation that compounds similar in structure will have similar properties. . . . When prior art compounds essentially “bracketing” the claimed compounds in structural similarity are all known as pesticides, one of ordinary skill in the art would clearly be motivated to make those claimed compounds in searching for new pesticides. In re Payne, 606 F.2d 303, 313-14 (CCPA 1979) (internal citations omitted). Analysis The Examiner found the selection of Appellants’ elected compound to have been simply a matter of picking and choosing from Pharmacia’s “various substituents with the expectation the resulting compounds will have Appeal 2010-000898 Application 10/497,491 8 the desired effect in varying degrees.” (Ans. 5.) Because Pharmacia taught that all the compounds included in its genus would be kynurenine-3- hydroxylase inhibitors (FF 1), we agree. As the Examiner noted, this is not a case where evidence of unexpected results has been offered to show that a particular selection from Pharmacia’s genus would have been nonobvious. In this circumstance, Pharmacia’s explicit disclosure was sufficient evidence to create an expectation that the compounds in its genus, including Appellants’ choice, would have the expected properties. See Eisai, 533F.3d at 1357. Put another way, Pharmacia’s disclosure also bracketed the species Appellants chose with structurally similar compounds that all had the same function. See Payne, 606 F.2d at 313-14. We are not persuaded of error on that ground. The rejection on appeal is also based on a finding that Lal taught administering a compound that could stop the conversion of kynurenine to kynurenic acid to treat diabetic neuropathy. (FF 6.) We do not see that idea explicitly stated in Lal, and the Examiner has not explained how Lal can be read as implicitly disclosing it. We agree with the Examiner that Lal’s “Background of the Invention” discusses some enzymes that act in kynurenine metabolism (FF 7 and 8), but we see no teaching to administer them. Instead, Lal taught administering HUTRAN-1, -2, or -3, which are said to be transferase enzymes. (FF 9.) The Examiner has not provided evidence or explained that a person of ordinary skill would have understood Lal to disclose that any of the HUTRANs could stop the kynurenine reaction. On this record, we conclude that the rejection is insufficient to support a conclusion of obviousness. Appeal 2010-000898 Application 10/497,491 9 CONCLUSIONS A person of ordinary skill in the art would have selected any compound from Pharmacia’s genus with the expectation that it would function as Pharmacia taught. The Examiner has not established that the content of Lal’s disclosure supports the finding that Lal taught administering a compound that stops the conversion of kynurenine to kynurenic acid as a treatment for diabetic neuropathy. SUMMARY We reverse the rejection of claims 2, 3, 10, 11, 13, 15, 17-19, 22 and 23 under 35 U.S.C. § 103(a) as unpatentable over Pharmacia & Upjohn S.O.A. (WO 97/17317) and Lai. REVERSED lp MILLEN, WHITE, ZELANO & BRANIGAN, P.C. 2200 CLARENDON BLVD. SUITE 1400 ARLINGTON VA 22201 Copy with citationCopy as parenthetical citation