pSivida US.Inc.Download PDFPatent Trials and Appeals BoardMay 22, 20202019004931 (P.T.A.B. May. 22, 2020) Copy Citation UNITED STATES PATENT AND TRADEMARK OFFICE 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 APPLICATION NO. FILING DATE FIRST NAMED INVENTOR ATTORNEY DOCKET NO. CONFIRMATION NO. 15/147,198 05/05/2016 Paul Ashton 047167-171012 1217 24633 7590 05/22/2020 HOGAN LOVELLS US LLP IP GROUP, COLUMBIA SQUARE 555 THIRTEENTH STREET, N.W. WASHINGTON, DC 20004 EXAMINER FAY, ZOHREH A ART UNIT PAPER NUMBER 1617 NOTIFICATION DATE DELIVERY MODE 05/22/2020 ELECTRONIC 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. Notice of the Office communication was sent electronically on above-indicated "Notification Date" to the following e-mail address(es): HLUSDocketing@hoganlovells.com dcptopatent@hoganlovells.com PTOL-90A (Rev. 04/07) UNITED STATES PATENT AND TRADEMARK OFFICE __________ BEFORE THE PATENT TRIAL AND APPEAL BOARD __________ Ex parte PAUL ASHTON __________ Appeal 2019-004931 Application1 15/147,198 Technology Center 1600 __________ Before DONALD E. ADAMS, RACHEL H. TOWNSEND, and JAMIE T. WISZ, Administrative Patent Judges. TOWNSEND, Administrative Patent Judge. DECISION ON APPEAL This is an appeal under 35 U.S.C. § 134 involving claims to an injectable sustained release composition, which have been rejected as obvious. We have jurisdiction under 35 U.S.C. § 6(b). We affirm. STATEMENT OF THE CASE “[M]acular degeneration can produce a slow or sudden loss of vision” and “[a]ge related macular degeneration (“AMD”) is the leading cause of blindness worldwide.” (Spec. 1) “Two forms of AMD exist: dry AMD and 1 We use the word “Appellant” to refer to “applicant” as defined in 37 C.F.R. § 1.42. Appellant identifies the real party in interest as EyePoint Pharmaceuticals, Inc. (Appeal Br. 1.) Appeal 2019-004931 Application 15/147,198 2 wet AMD.” (Id.) “[T]reatments for wet AMD exist, such as use of anti- neovascular agents[, e.g., agents that block the action of vascular endothelial growth factor (VEGF), thereby slowing angiogenesis,] and photodynamic therapy (i.e., laser irradiation of the macula).” (Id.) Appellant’s invention is concerned with compositions that include kinase inhibitors that can be used to treat macular degeneration. (Id. at 2.) Claims 1–10 are on appeal. Claim 1 is representative and reads as follows: 1. An injectable sustained release composition, comprising a kinase inhibitor dissolved in a water-miscible organic solvent, wherein: the concentration of the kinase inhibitor in the composition is at least 200 μg/mL; and the concentration of the kinase inhibitor in the composition is at least 100 times higher than the solubility of the kinase inhibitor in water at 37°C. (Appeal Br. 10.) The prior art relied upon by the Examiner is: Name Reference Date Jessen et al. US 2015/0030588 A1 Jan. 29, 2015 The following ground of rejection by the Examiner is before us on review:2 Claims 1–10 under 35 U.S.C. § 103(a) as unpatentable over Jessen. 2 The Examiner’s rejection of claims 1–10 under 35 U.S.C. § 112, first paragraph as lacking an adequate written description made in the Final Action is deemed to have been withdrawn by the Examiner in light of the Answer, which indicates that only the 103 rejection over Jesse is “applicable to the appealed claims.” (Ans. 3.) Appeal 2019-004931 Application 15/147,198 3 DISCUSSION The Examiner finds that Jessen teaches a sustained release formula of protein kinase inhibitors. (Final Action 5.) The Examiner also finds that Jessen teaches (a) the use of the claimed compounds for treating macular degeneration, (b) liquid formulations, and (c) employing intravitreal or intraocular injection for treating ophthalmic condition. (Id. (citing Jessen ¶¶ 242 and 247 (macular degeneration); id. ¶ 536 (intravitreal or intraocular injection for ophthalmic condition); id. ¶ 504 (liquid composition).) The Examiner finds that the concentration of inhibitor claimed is taught by Jessen, as is the use of the claimed solvents/solubilizers, such as alcohols. (Final Action 5; Ans. 5 (indicating that “the concentration of 200 μg/ml [of the kinase inhibitor], falls between the concentrations of 0.0001%, to 50%” taught in Jessen ¶ 463 and that Jessen ¶ 495 teaches that “the composition may include a solubilizer to ensure good solubilization, which is especially important for non-oral compositions, such as the ones used by injection.”).) In view of the foregoing, the Examiner concludes that it would have been obvious to one having ordinary skill in the art to use the claimed protein kinase inhibitors for the treatment of ophthalmic conditions by injection. (Final Action 5.) The Examiner acknowledges that Jessen “does not specifically teach[] the sustained release for administration by injection.” (Ans. 4.) However, the Examiner concludes that, in light of Jessen teaching a kinase inhibitor, which is dissolved in water miscible organic solvent such as, ethanol, at the concentrations that encompass the claimed concentrations, and that those two components are the same two components required by Appellant’s claim, Jessen’s composition would function as sustained release just as Appeal 2019-004931 Application 15/147,198 4 Appellant’s claimed invention would. (Id. at 4–5; see also Final Action 5, 8.) The Examiner also concludes that the function of the composition “such as the higher solubility in organic solvent in comparison with water is the expected property of the prior art composition,” which has the same concentration claimed of the kinase inhibitor and is present with an organic solvent and solubilizer. (Final Action 8; Ans. 5.) We determine that the Examiner has established a prima facie case of obviousness. In particular, we agree with the Examiner that Jessen teaches the claimed active ingredient, a kinase inhibitor, (see, e.g., Jessen ¶ 17) may be used in treating macular degeneration (see id.¶¶ 242, 247), and can be used in treating ophthalmic conditions via injection (id. ¶ 536). Furthermore, Jessen teaches that the form of the composition for injection may be a solution of the claimed compound in an appropriate solvent and that ethanol is a suitable solubilizer for use in a “composition[] for injection.” (Id. ¶¶ 494, 503–505.) Regarding the concentration range claimed, “at least 200 μg/mL” and “at least 100 times higher than the solubility of the kinase inhibitor in water at 37 ºC,” we find the following. Appellant’s Specification teaches that “the solubility of many kinase inhibitors in water is about 1 to about 50 μM (about 0.5 μg/mL to about 25 μg/mL for small molecules with a molecular weight of 500 AMU).” (Spec. 2.) In other words, many kinase inhibitors have a very low solubility in water. Jessen discloses use of inhibitors of platelet-derived growth factor receptors (PDGFR), such as sorafenib, a compound that also inhibits vascular endothelial growth factor receptor (VEGFR), present in an alcohol diluent such as ethanol so as to be able to administer the active as an Appeal 2019-004931 Application 15/147,198 5 injectable solution. (Jessen ¶ 254 (disclosing specific inhibitors of PDGFR), ¶¶ 494–495, 503–504 (disclosing an alcohol diluent such as ethanol for injectable solutions).) Appellant’s Specification exemplifies a composition that is within the scope of the invention that includes sorafenib as the kinase inhibitor. (Spec. 16.) Thus, we find Jessen teaches the use of a known protein kinase inhibitor that is poorly soluble in water. Furthermore, Jessen teaches a wide concentration range of kinase inhibitors may be employed including greater than 0.0001% and up to 50% w/v, with many smaller ranges also being disclosed. (Jessen ¶ 463.) Appellant does not dispute the Examiner’s position that the disclosed concentration ranges in Jessen for protein kinase inhibitors overlaps the claimed range. (Appeal Br. 8; Reply Br. 7.) Rather, Appellant argues that while Jessen lists many concentration ranges, nowhere does it (or any other passage in Jessen) teach or suggest that there are some concentrations that can be used advantageously to cause particular kinase inhibitors to precipitate, leading to injectable sustained release formulations. (Reply Br. 7; accord Appeal Br. 8 (“there is no recognition that with suitable concentrations (as recited in Applicant’s claims) one can actually arrive at an injectable formulation that has a sustained release profile.”).) That argument is concerned with whether Jessen recognized the use of the range of concentrations in an injectable composition to achieve sustained release. However, that Jessen does not describe the injectable compositions as being sustained release does not establish that Jessen’s injectable compositions Appeal 2019-004931 Application 15/147,198 6 would not have such a functional characteristic.3 In re Baxter Travenol Labs., 952 F.2d 388, 392 (Fed. Cir. 1991) (“Mere recognition of latent properties in the prior art does not render nonobvious an otherwise known invention.”). We address this in more detail below with respect to whether Appellant has established that the claimed invention achieves an unexpected result. Turning back to the concentration limitation per se, we note that “where there is a range disclosed in the prior art, and the claimed invention falls within that range, there is a presumption of obviousness.” Iron Grip Barbell Co. v. USA Sports, Inc., 392 F.3d 1317, 1322 (Fed. Cir. 2004). Based on Appellant’s argument directed to whether Jessen recognized the claimed functional requirement that the composition be sustained release, we conclude that Appellant concedes that Jessen teaches ranges of protein kinase for use in injectable compositions that overlap the claimed concentrations. “[T]he existence of overlapping or encompassing ranges shifts the burden to the applicant to show that his invention would not have been obvious.” In re Peterson, 315 F.3d 1325, 1330 (Fed. Cir. 2003). The presumption can be rebutted by demonstrating “unexpected properties in the range claimed” or by showing that the art teaches away from the claimed 3 We agree with Appellant that Jessen only explicitly mentions sustained release in connection with oral formulations. (Appeal Br. 7; Jessen ¶¶ 474, 525.) But we do not rely on the Examiner’s finding that Jessen teaches sustained release oral composition to determine a prima facie case of obviousness has been established with respect to sustained release injectable compositions. Thus, we do not find persuasive Appellant’s argument that the Examiner’s rejection “is based on nothing more than taking portions of Jessen’s disclosure completely out of context” (Appeal Br. 7.) Appeal 2019-004931 Application 15/147,198 7 invention. In re Geisler, 116 F.3d 1465, 1469 (Fed. Cir. 1997). We conclude Appellant has done neither for the reasons that follow. No evidence establishing unexpected properties compared to Jessen Appellant has not demonstrated that sustained release from an injectable solution suggested by Jessen is an unexpected property in the broad concentration range claimed. Appellant’s Specification teaches sustained release is a natural function of the general low solubility of protein kinase inhibitors in water and their presence in a diluent such as ethanol. Appellant’s Specification explains “limited solubility in water is a key factor in achieving extended release.” (Spec. 5.) Appellant’s Specification discloses that as water infiltrates the solution of kinase inhibitor dissolved in organic solvent that is miscible with water, after it is injected, the kinase inhibitor precipitates from the solution and the water dissolves the kinase inhibitor “to provide sustained release” of that inhibitor. (Id. at 2.) Thus, because the teachings of Jessen would have made it obvious to one of ordinary skill in the art to dissolve a protein kinase inhibitor, such as those recited in the dependent claims (see, e.g., Jessen ¶ 254 (disclosing use of inhibitors of platelet- derived growth factor receptors (PDGFR), such as sorafenib, that also inhibits vascular endothelial growth factor receptor (VEGFR)), in an alcohol diluent such as ethanol in up to 50% w/v (see id. ¶¶ 463, 494–495, 503– 504), we determine there is sufficient evidence of record to establish a prima facie case that the sustained release requirement of the claim is met. “Where . . . the claimed and prior art products are identical or substantially identical . . . the PTO can require an applicant to prove that the prior art products do not necessarily or inherently possess the characteristics Appeal 2019-004931 Application 15/147,198 8 of his claimed product.” In re Best, 562 F.2d 1252, 1254–55, (CCPA 1977). This is true even where the rejection is one premised on obviousness. Id. (“Whether the rejection is based on ‘inherency’ under 35 U.S.C. § 102, on ‘prima facie obviousness’ under 35 U.S.C. § 103, jointly or alternatively, the burden of proof is the same, and its fairness is evidenced by the PTO’s inability to manufacture products or to obtain and compare prior art products.”). Appellant has not demonstrated that there are concentrations disclosed in Jessen that do not result in sustained release injectable solutions of protein kinase dissolved in alcohol. Thus, we do not find the Examiner’s position that the sustained release characteristic is an inherent property of the range of compositions suggested by Jessen has been proven to be erroneous. Jessen does not teach away from the claimed invention We also do not find persuasive Appellant’s argument that Jessen teaches away from the claimed invention because it teaches “that one should use solubilizers to prevent precipitation” (Reply Br. 7). We understand the suggestion that precipitation should be prevented in Jessen to be with respect to “minimiz[ing] precipitation of the compound” out of solution prior to injection. (See Jessen ¶ 494 (quoted by Appellant at Reply Br. 7).) In particular, the paragraph relied upon by Appellant teaches the use of a solubilizer that minimizes precipitation is also “to ensure good solubilization and/or dissolution of the compound,” both of which are said to be “especially important for compositions for non-oral use, e.g., compositions for injection.” (Jessen ¶ 494.) Such is consistent with the later discussion in the paragraph that the solubilizer is used to “maintain the composition as a stable or homogeneous solution or dispersion” (id.) and further noting, in a separate paragraph, the importance of maintaining “the proper fluidity” of Appeal 2019-004931 Application 15/147,198 9 injectable solutions (id. ¶ 504). Avoiding such precipitation is common knowledge in the medicinal and formulation arts to ensure that the dosage amount provided to the patient is the amount indicated to be in the formulation. Appellant does not provide evidence that one of ordinary skill in the art would interpret Jessen’s discussion of minimizing precipitation in a solution passage otherwise; instead, there is only attorney argument. “Attorneys’ argument is no substitute for evidence.” Johnston v. IVAC Corp., 885 F.2d 1574, 1581 (Fed. Cir. 1989). Consequently, we conclude that Appellant has not rebutted the Examiner’s prima facie case of obviousness. Claims 2–10 have not been argued separately from claim 1. (Appeal Br. 8 (“Applicant respectfully submits that these [dependent] claims are allowable at least for depending from an allowable independent claim.”).) Consequently, these claims fall with claim 1. 37 C.F.R. § 41.37(c)(1)(iv)(2018). For the reasons discussed above, we affirm the Examiner’s rejection of claims 1–10 as being obvious over Jessen. DECISION SUMMARY In summary: Claims Rejected 35 U.S.C. § Reference(s)/Basis Affirmed Reversed 1–10 103 Jessen 1–10 Appeal 2019-004931 Application 15/147,198 10 TIME PERIOD FOR RESPONSE No time period for taking any subsequent action in connection with this appeal may be extended under 37 C.F.R. § 1.136(a). See 37 C.F.R. § 1.136(a)(1)(iv). AFFIRMED Copy with citationCopy as parenthetical citation