Ex Parte Flores-Riveros et alDownload PDFPatent Trial and Appeal BoardFeb 18, 201611941934 (P.T.A.B. Feb. 18, 2016) Copy Citation UNITED STA TES p A TENT AND TRADEMARK OFFICE APPLICATION NO. FILING DATE 111941,934 11/17/2007 26551 7590 NeurMedix, Inc, 6165 Greenwich Drive Suite 150 San Diego, CA 92122 02/18/2016 FIRST NAMED INVENTOR Jaime Flores-Riveros UNITED STATES DEPARTMENT OF COMMERCE United States Patent and Trademark Office Address: COMMISSIONER FOR PATENTS P.O. Box 1450 Alexandria, Virginia 22313-1450 www .uspto.gov ATTORNEY DOCKET NO. CONFIRMATION NO. 334 1637 EXAMINER N ANOV A, SVETLANA M ART UNIT PAPER NUMBER 1627 MAILDATE DELIVERY MODE 02/18/2016 PAPER Please find below and/or attached an Office communication concerning this application or proceeding. The time period for reply, if any, is set in the attached communication. PTOL-90A (Rev. 04/07) UNITED STATES PATENT AND TRADEMARK OFFICE BEFORE THE PATENT TRIAL AND APPEAL BOARD Ex parte JAIME FLORES-RIVEROS, JAMES M. FRINCKE, CHRISTOPHER READING, DWIGHT STICKNEY, and CLARENCE AHLEM Appeal2013-007013 Application 11/941,934 Technology Center 1600 Before RICHARD M. LEBOVITZ, JEFFREY N. FREDMAN, and JACQUELINE T. HARLOW, Administrative Patent Judges. FREDMAN, Administrative Patent Judge. DECISION ON APPEAL This is an appeal1under35 U.S.C. § 134 involving claims to a pharmaceutical formulation. The Examiner rejected the claims as obvious. We have jurisdiction under 35 U.S.C. § 6(b). We affirm. 1 Appellants identify the Real Party in Interest as Harbor Therapeutics, Inc. (See Br. 1 ). Appeal2013-007013 Application 11/941,934 Statement of the Case Background "The invention relates to methods and compounds such as 4a-fluoro- l 7 a-ethynylandrost-5-ene-3 B, 7B, l 7B-triol to modulate inflammation, metabolic disorders and other conditions described herein. The compounds can be used to treat or slow the progression of conditions such as type 2 diabetes, hyperglycemia and insulin resistance" (Spec. iJ 2). The Claims Claims 18-20 are on appeal. Claim 18 is representative and reads as follows: 18. A pharmaceutical formulation comprising one or more pharmaceutically acceptable excipients and a compound having the structure R15 H wherein one R1 is-Hor C1-s optionally substituted alkyl and the other R1 is -OH, an ester or an ether; one R2 is-Hor C1-s optionally substituted alkyl and the other R2 is -OH or an ester, or both R2 together are =O; one R3 is-Hand the other R3 is -H, -OH, an ester or an ether; R4 in the a-configuration is optionally substituted C2-4 alkynyl; R4 in the B-configuration is -OH or an ester; R7 is -CH20H; and R15 is -OH, an ester or an ether wherein the pharmaceutical formulation is a unit oral dosage form containing about 5 mg to about 250 mg of the compound. 2 Appeal2013-007013 Application 11/941,934 The Issues A. The Examiner rejected claims 18-20 under 35 U.S.C. § 103(a) as obvious over Ahlem '2992 and Reading3 (Ans. 4-12). B. The Examiner rejected claims 18-20 under 35 U.S.C. § 103(a) as obvious over Ahlem '4254 and Reading (Ans. 22-28). Because the same issues are dispositive for both of these rejections, we will consider them together. The issue with respect to these rejection is: Does the evidence of record support the Examiner's conclusion that either Ahlem '299 or Ahlem '425, combined with Reading render claim 18 obvious? Findings of Fact 1. Ahlem '299 teaches a compound of formula 1, reproduced below: l R3 wherein "R1, R2, R3, R4, R5, R6 and R10 independently are-H, -ORPR, ... an ester, ... an ether, ... an optionally substituted alkynyl group" (Ahlem '299, col. 4, 11. 45-67). Ahlem '299 teaches "where RPR independently is hydrogen" (Ahlem '299, col. 9, 1. 1 ). 2 Ahlem et al., US 6,667,299 Bl, issued Dec. 23, 2003. 3 Reading et al., WO 2004/019953 Al, published Mar. 11, 2004. 4 Ahlem et al., US 2003/0060425 Al, published Mar. 27, 2003. 3 Appeal2013-007013 Application 11/941,934 2. Ahlem '299 teaches a compound 1.2.5.9 as reproduced below: tTh o~·· I l no~, (Ahlem '299, col. 66, 11. 30--40). 3. Ahlem '299 teaches that "one can administer the formula 1 compound(s) orally using about 4 to about 40 mg/kg/day, usually about 6-20 mg/kg/day" (Ahlem '299, col. 75, 11. 56-58). 4. Ahlem '425 teaches a compound of formula 1, reproduced below: wherein "each R1, R2, R3, R4, R5, R6 and R10 independently are -H, -ORPR, . . . an ester, ... an ether, ... an optionally substituted alkynyl group" (Ahlem '425 iii! 25-27). Ahlem '425 further teaches that "RPR independently is-Hor a protecting group" (Ahlem '425 iJ 35). 5. Ahlem '425 teaches a compound 1.2.5.9 as reproduced below: 4 Appeal2013-007013 Application 11/941,934 (Ahlem '425 iJ 422). 6. Ahlem '425 teaches "[i]ntermittent dosing embodiments include administration of a formula 1 compound, e.g., orally ... as follows: (1) daily dosing for about 3 to about 190 days (e.g., about 3 to about 20 days)" (Ahlem '425 iJ 461 ). 7. Ahlem '425 teaches that "step (1) may comprise daily dosing of about 20 mg/day to about 1500 mg/day (e.g., about 50, 75, 100, 125, 150, 175, 200, 225, 250, 275, 300, 325, 350 or 400 mg/day) of a formula 1 compound" (Ahlem '425 iJ 462). 8. Reading teaches a compound as shown below: R5 R4 .... 11\\\R4 Rs wherein "each R1, R2, R3, R4, R5, R6, ... R10B ... independently are -H, - OH, ... an ester, ... an ether, ... an optionally substituted alkynyl group" (Reading iii! 15, 23). 5 Appeal2013-007013 Application 11/941,934 Principles of Law [T]he cases establish that if an examiner considers that he has found prior art close enough to the claimed invention to give one skilled in the relevant chemical art the motivation to make close relatives (homologs, analogs, isomers, etc.) of the prior art compound(s), then there arises what has been called a presumption of obviousness or a prim a facie case of obviousness .... The burden then shifts to the applicant, who then can present arguments and/or data to show that what appears to be obvious, is not in fact that, when the invention is looked at as a whole. In re Dillon, 919 F.2d 688, 696 (Fed. Cir. 1990). Analysis We adopt the Examiner's findings of fact and reasoning regarding the scope and content of the prior art (Ans. 4-12; 22-28; FF 1-8) and agree that claim 18 is rendered obvious by either Ahlem '299 or Ahlem '425 and Reading. We address Appellants' arguments below. Appellants contend that "the Examiner did not articulate why any alleged lead compound(s) would in fact be considered a lead under the law" (Br. 9). Appellants contend that the "Examiner did not explain why one of ordinary skill in the art would have selected the specific chemical modifications of the alleged lead compound(s) needed to arrive at a claimed composition in normal course of research and development" (Br. 9). We find this argument unpersuasive because the rejected claims do not fall into the paradigm established by the lead compound analysis. In Takeda, the court applied the lead compound analysis to a claim to a specific compound, not a genus of compounds as in instant claim 18, finding that "in cases involving new chemical compounds, it remains necessary to identify 6 Appeal2013-007013 Application 11/941,934 some reason that would have led a chemist to modify a known compound in a particular manner to establish prima facie obviousness of a new claimed compound." Takeda Chemical Industries, Ltd. v. Alphapharm Pty., Ltd., 492 F.3d 1350, 1357 (Fed. Cir. 2007). That is, the Takeda court was not analyzing a claim drawn to millions of compounds, like instant claim 18, but rather was analyzing a claim drawn to a compound with one specific chemical formula. Id. at 1353. Similarly, Otsuka also applied the lead compound analysis in the context of a claim to the specific compound, Ariprazole, and Daiichi to the specific compound Olmesartan, so neither decision was drawn to a genus claim of millions of compounds as in the instant fact pattern. Otsuka Pharm. Co., Ltd. v. Sandoz, Inc., 678 F.3d 1280, 1284 (Fed. Cir. 2012); Daiichi Sankyo Co., Ltd. v. Matrix Labs., Ltd., 619 F.3d 1346 (Fed. Cir. 2010). Therefore, the Examiner properly rejected rote application of the lead compound analysis to a fact pattern for which the analysis is inappropriate. See KSR. Intern. Col. v. Teleflex Inc., 550 US 398, 419 (2007) ("Helpful insights, however, need not become rigid and mandatory formulas . . . when a court transforms the general principle into a rigid rule that limits the obviousness inquiry ... it errs)" We recognize, but find unpersuasive, Appellants' argument that the "'close structural similarity' the Examiner alleges is cobbled together from generic structures that encompass millions of species and many individual disclosed compound species with no obvious reason to do so and no pertinent properties to guide the selection process" (Br. 17). Unlike Takeda 's claim to an antidiabetic composition, Otsuka 's claim to a schizophrenia treating composition, or Daiichi 's claim to treatment of 7 Appeal2013-007013 Application 11/941,934 high blood pressure, Appellants' claim 18 does not encompass any particular "pertinent properties" or functional requirements nor is the formulation in claim 18 directed to any particular disease. Therefore, even the attempt to apply the lead compound analysis fails because claim 18 lacks one specific activity or function to serve as the target for optimization using a lead compound. See Takeda, 492 F.3d 1353; Otsuka, 678 F.3d at 1285; and Daiichi, 619 F.3d at 1347. Indeed, the instant Specification recites a laundry list of possible disease targets that is more than two pages in length encompassing conditions ranging from pain and graft versus host disease to sleep disturbance, chemical bums, multiple sclerosis, obesity, and atherosclerosis (see Spec. iii! 64-69). The Specification states that it "provides compounds or compositions to treat, prevent, slow the progression of or ameliorate an unwanted inflammation condition[,] an autoimmune disease or a metabolic disorder or a symptom thereof' (id. at iJ 20), but Appellants did not direct us to a common activity or property by which the compounds exerted their beneficial effect. Therefore neither claim 18 nor the Specification provide specific limitations that would distinguish a desirable lead compound from an undesirable lead compound. Instead, the instant facts are more similar to those in Susi, where the CCP A determined that a prior art genus reference Knapp rendered the subgenus claim at issue obvious, finding that "[p ]lacing a simple representative of each side by side, it is obvious that the subject matter of appellant's claim 6 is very nearly within the generic teaching of Knapp." In re Susi, 440 F.2d 442, 444 (CCPA 1971). Susi found unpersuasive "the position of one who argues that the selection of a relatively small subgenus 8 Appeal2013-007013 Application 11/941,934 from a genus disclosed in the prior art would have been unobvious at the time of his invention to one skilled in the art." Id. at 445. In this case, the genus of compounds encompassed by Appellants' claim 18 represents a subgenus fully disclosed by each of Ahlem '299, Ahlem '425, and Reading (FF 1, 4, 8). Ahlem '299 or Ahlem '425 each teach specific compound species that differ from the genus of compounds of claim 18 by the presence of a single hydroxyl group (FF 2, 5) that is a suggested alternative in the generic compound disclosures (FF 1, 4). Thus, the claimed subgenus is reasonably suggested by the cited prior artWe further agree with the Examiner's finding that the prior art teaches "'ring walking' of the -OH substituent, including where it can be in the C-4 (i.e. R- 15, per Appellant's formula) position" (Ans. 24-25). Consistent with Dillon, the Examiner has identified compound 1.2.5.9 as a species structurally similar to the claimed genus of compounds, differing only in the R15 group of claim 18 (FF 2, 5). The Examiner recognized that each of Ahlem '299, Ahlem '425, and Reading suggest generic structures which teach the placement of substituents including -OH substituents at that position (FF 1, 4, 8). In response to the Examiner's position, Appellants have provided no evidence of secondary considerations. We recognize, but find unpersuasive, Appellants' argument that "Examiner also ignored the limitation that the claimed formulations are oral unit doses" (Br. 9-10). Ahlem '299 and Ahlem '425 specifically teach oral dosages in amounts that overlap those required by claim 18 (FF 3, 6). Appellants provide no reason why those overlapping oral dosages do not render the oral dosages required by claim 18 obvious. See In re Peterson, 9 Appeal2013-007013 Application 11/941,934 315 F.3d 1325, 1329 (Fed. Cir. 2003) ("In cases involving overlapping ranges, we and our predecessor court have consistently held that even a slight overlap in range establishes a prim a facie case of obviousness.") Conclusion of Law The evidence of record supports the Examiner's conclusion that either Ahlem '299 or Ahlem '425, combined with Reading render claim 18 obvious. SUMMARY In summary, we affirm the rejection of claim 18 under 35 U.S.C. § 103 (a) as obvious over Ahl em '299 and Reading. Claims 19 and 20 fall with claim 18. 37 C.F.R. § 41.37(c)(l)(iv). We affirm the rejection of claim 18 under 35 U.S.C. § 103(a) as obvious over Ahlem '425 and Reading. Claims 19 and 20 fall with claim 18. 37 C.F.R. § 41.37(c)(l)(iv). No time period for taking any subsequent action in connection with this appeal may be extended under 37 C.F.R. § l.136(a). AFFIRMED cdc 10 Copy with citationCopy as parenthetical citation