10344884 (P.T.A.B. Jul. 23, 2013)

Ex Parte Rimpler et al

Patent Trial and Appeal BoardJul 23, 2013

10344884 (P.T.A.B. Jul. 23, 2013)

UNITED STATES PATENT AND TRADEMARKOFFICE 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. 10/344,884 02/11/2003 Stephan Rimpler 6102-000063/US/NP 3489 28997 7590 07/24/2013 HARNESS, DICKEY, & PIERCE, P.L.C 7700 Bonhomme, Suite 400 ST. LOUIS, MO 63105 EXAMINER BASQUILL, SEAN M ART UNIT PAPER NUMBER 1613 MAIL DATE DELIVERY MODE 07/24/2013 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 STEPHAN RIMPLER, SABINE GRAPATIN, CLIFF KREIN, and MARKUS THELEN __________ Appeal 2011-013406 Application 10/344,884 Technology Center 1600 __________ Before ERIC GRIMES, ERICA A. FRANKLIN, and ANNETTE R. REIMERS, Administrative Patent Judges. FRANKLIN, Administrative Patent Judge. DECISION ON APPEAL This is an appeal under 35 U.S.C. § 134(a) involving claims to a method for producing a thermally treated sterile depot suspension of rotigotine. The Patent Examiner rejected the claims as obvious. We have jurisdiction under 35 U.S.C. § 6(b). We reverse. Appeal 2011-013406 Application 10/344,884 2 STATEMENT OF THE CASE Rotigotine, S(-)-2-(N-propyl-N-2-thienylethylamino)-5- hydroxytetralin, is “a potent and selective dopamine D2 agonist playing a significant role in the treatment of all diseases associated with a dopamine- related metabolic disorder such as Parkinson’s disease and Restless Leg.” (Spec. [0005].) The claimed invention relates to a depot formulation of pharmaceutical compositions containing rotigotine. (Id. at [0027].) According to the Specification, when the recited oily suspension of rotigotine is heated during the thermal sterilization process, the compound remains stable, avoiding the substantial thermal decomposition seen with heat-sterilized dissolved rotigotine. (Id. at [0022].) Claims 76-79, 93-96 and 109 are on appeal. Claim 76 is representative and reads as follows: 76. A method for producing an injectable pharmaceutical composition, comprising preparing an oily suspension of solid-phase rotigotine or a pharmaceutically acceptable salt thereof in a pharmaceutically acceptable hydrophobic liquid phase that comprises a wetting agent free of phosphatides; and thermally treating said oily suspension to provide a sterile depot suspension of said rotigotine or salt thereof. (Emphasis added.) The Examiner rejected the claims as follows: • claims 76-79, 93-95 and 109 under 35 U.S.C. § 103(a) as unpatentable over Horn,1 Iwata,2 and Anschel;3 and 1 US Patent No. 4,564,628 issued to Alan S. Horn, Jan. 14, 1986. Appeal 2011-013406 Application 10/344,884 3 • claims 76-79, 93-96 and 109 under 35 U.S.C. § 103(a) as unpatentable over Horn, Iwata, Anschel, and Thompson.4 OBVIOUSNESS The Examiner found that Horn disclosed that crystalline rotigotine or rotigotine hydrochloride may be prepared in a variety of oral dosage formulations, including an oily suspension. (Ans. 6.) The Examiner also found that Horn disclosed that its formulation may be administered orally or parenterally, i.e., by injection. (Id.) However, the Examiner found that Horn did not disclose the recited formulation of rotigotine, or heat treating the formulation to provide a sterile depot suspension. (Id.) The Examiner found that Iwata disclosed a formulation for delivery of a water-soluble drug comprising the drug, an oily vehicle, and a surfactant, preferably sorbitan fatty acid esters. (Id.) The Examiner also found that Anschel disclosed a formulation for relaxin, a hormone, wherein relaxin is suspended in an injectable oil and heat treated via autoclave to improve its stability and prolong its activity. (Id.) According to the Examiner, it would have been obvious to a person of ordinary skill in the art at the time the invention was made to have prepared crystalline rotigotine or rotigotine hydrochloride in an oily suspension comprising a surfactant such as a sorbitan fatty acid ester for administration parenterally, and to heat treat the suspension via autoclave to provide a 2 Patent Application Publication No. WO 89/03671 by Motokazu Iwata et al., published May 5, 1989. 3 US Patent No. 2,964,448 issued to Joachim Anschel, Dec. 13, 1960. 4 US Patent No. 2,992,165 issued to Robert E. Thompson, Jul. 11, 1961. Appeal 2011-013406 Application 10/344,884 4 sterile formulation. (Id. at 6-7.) The Examiner reasoned that the artisan would have been motivated to do so because: Horn taught that rotigotine could be formulated into an injectable dose; Iwata taught how to formulate such a water soluble drug in an injectable oily suspension comprising a surfactant (wetting agent) free of phosphatides; and “Anschel describe[d] the sterilization via autoclave of injectable oily suspensions.” (Id. at 7.) Appellants contend, among other things, that contrary to the Examiner’s statement, Anschel does not broadly indicate “‘that oily suspensions of water soluble drugs are commonly delivered via injection following heat treatment and duration of dosing.’” (App. Br. 15.) Rather, according to Appellants, “Anschel’s exclusive focus is relaxin,” such that “there is no teaching, motivation or suggestion to apply Anschel to rotigotine….” (Id.) We agree with this argument by Appellants. Specifically, we do not find that Anschel taught or suggested heat treating water soluble drugs, in general, for any reason. Rather, Anschel teaches that “[t]he heat treatment of [a] mixture of relaxin, a fatty acid salt of aluminum and an injectable oil . . . imparts to the relaxin mixture an extraordinarily prolonged repository activity when injected” (Anschel, col. 2, ll. 60-63). The Examiner has not provided an adequate reason for concluding that this disclosure would have suggested the heat treatment of an oily suspension of rotigotine. Accordingly, we reverse the obviousness rejection over Horn, Iwata and Anschel. Regarding the rejection over Horn, Iwata, Anschel and Thompson, the Examiner again found that the combination of Horn, Iwata and Anschel taught the claimed method of preparing an oily suspension of rotigotine and Appeal 2011-013406 Application 10/344,884 5 thermally treating the suspension. (Ans. 7.) The Examiner further found that Thompson taught autoclaving an aqueous injectable pharmaceutical formulation in a nitrogen atmosphere. However, we do not find that Thompson taught or suggested autoclaving an oily suspension of a water- soluble drug such as rotigotine, so as to overcome the deficiency in the combination of Horn, Iwata and Anschel. Accordingly, we also reverse the rejection over Horn, Iwata, Anschel and Thompson. SUMMARY We reverse each of the obviousness rejections. REVERSED clj