SG11201811412XA - Cyclic peptides as c5 a receptor antagonists - Google Patents

Abstract

INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property 11111111111 0 DOI HIM 011101 0 011101 01011111 OM H 11011111111111 OEN Organization International Bureau (10) International Publication Number (43) International Publication Date .....0\" WO 2018/020358 Al 01 February 2018 (01.02.2018) WIP0 I PCT (51) International Patent Classification: DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, CO7K 7/56 (2006.01) A61P 37/00 (2006.01) HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, A61K 38/12 (2006.01) A61P 13/12 (2006.01) KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, (21) International Application Number: MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, PCT/1B2017/054314 OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, (22) International Filing Date: TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. 17 July 2017 (17.07.2017) (84) Designated States (unless otherwise indicated, for every (25) Filing Language: English kind of regional protection available): ARIPO (BW, GH, (26) Publication Language: English GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, (30) Priority Data: TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, 62/368,262 29 July 2016 (29.07.2016) US EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, 62/517,215 09 June 2017 (09.06.2017) US MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, (71) Applicant: PFIZER INC. [US/US]; 235 East 42nd Street, KM, ML, MR, NE, SN, TD, TG). New York, New York 10017 (US). (72) Inventors: CHE, Ye; 15 Freedom Way Unit 5, Niantic, Declarations under Rule 4.17: Connecticut 06357 (US). FENG, Yiqing; 263 Ohio Ave, — as to the identity of the inventor (Rule 4.17(i)) — Groton, Connecticut 06340 (US). HAYWARD, Matthew — as to applicant's entitlement to apply for and be granted a Merrill; 3 Pyrus Court, Old Lyme, Connecticut 06371 patent (Rule 4.17(0) (US). HEPWORTH, David; 282 Sudbury Road, Concord, — as to the applicant's entitlement to claim the priority of the = Massachusetts 01742 (US). JONES, Peter; 61 Hender- earlier application (Rule 4.17(iii)) son Street, Arlington, Massachusetts 02474 (US). KAILA, Published: Neelu; 17 Augustus Road, Lexington, Massachusetts 02421 — with international search report (Art. 21(3)) (US). PAPAIOANNOU, Nikolaos; 70 Spiers Road, New- _ = _ - ton, Massachusetts 02459 (US). = Agent: WALDRON, Roy F.; Pfizer Inc., 235 East 42nd (74) Street, MS 235/9/S20, New York, NY 10017 (US). Designated States (unless otherwise indicated, for every (81) = = = kind of national protection available): AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, = = Title: CYCLIC PEPTIDES AS C5 A RECEPTOR ANTAGONISTS = (54) R 1 ', :. Rib = 0 1,1 0 H R4 N,,,,,„-- 7 H = = R 3 , 0 0 ... NH „, 0 .--- ;-, 0 N HO O o O ~ R Z HO O o 0 R 2 = H — Il .4 NH NH -. N .IL. NH2 \ A GC kr) N (la) H (Ib) H NH2 , Cr) © ei © (57) : The invention relates to cyclic peptide derivatives, to their use in medicine, to compositions containing them, to processes . 3 - t\" for their preparation and to intermediates used in such processes. More particularly the invention relates to cyclic peptide C5a receptor Il antagonists of formula (Ia)or formula (Ib), or pharmaceutically acceptable salts thereofwherein Ria, Rib, fc -2, R3 and R 4 areas defined in N the description. C5a receptor antagonists are potentially useful in the treatment of a wide range of 1 disorders,including inflammatory ..., disorders and immune disorders.