Patent SG-11201407210S-A (SG)
Title: Pyrazole derivatives and their use as lpar5 antagonists
Inventor: NAZARÉ MARC
IPC: C07D231/12
Filed: 2013-05-16
Abstract: (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 21 November 2013 (21.11.2013) WIPOIPCT (10) International Publication Number WO 2013/171317 A1 (51) International Patent Classification: C07D 231/12 (2006.01) A61K31/4155 (2006.01) C07D 409/04 (2006.01) A61P 7/02 (2006.01) A61K31/415 ( 2006.01) (21) International Application Number: (22) International Filing Date: (25) Filing Language: (26) Publication Language: PCT/EP2013/060171 16 May 2013 (16.05.2013) English (30) Priority Data: 12305552.7 18 May 2012 (18.05.2012) English EP (71) Applicant: SANOFI [FR/FR]; 54 rue La Boetie, F-75008 Paris (FR). (72) Inventors: NAZARE, Marc; Sanofi-Aventis Deutschland GmbH, 65926 Frankfurt am Main (DE). KOZIAN, Detlef; Sanofi-Aventis Deutschland GmbH, 65926 Frankfurt am Main (DE). EVERS, Andreas; Sanofi-Aventis Deutsch­ land GmbH, 65926 Frankfurt am Main (DE). CZECHT- IZKY, Werngard; Sanofi-Aventis Deutschland GmbH, 65926 Frankfurt am Main (DE). (74) Agent: VENNE-DUNKER, Sabine; Sanofi-Aventis Deutschland GmbH, Patents Germany, Industriepark — Hochst, Geb. K 801, 65926 Frankfurt am Main (DE). (81) Designated States (unless otherwise indicated, for every 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, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (84) Designated States (unless otherwise indicated, for every kind of regional protection available)'. ARIPO (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, SZ, TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, 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, ML, MR, NE, SN, TD, TG). Declarations under Rule 4.17 : — of inventorship (Rule 4.17(iv)) Published: with international search report (Art. 21(3)) (54) Title: PYRAZOLE DERIVATIVES AND THEIR USE AS LPAR5 ANTAGONISTS N \ i> / R' H H R 4 R 5 R 2 V v>c° N-^ R 3 o G (i) i-H o CJ (57) Abstract: The present invention relates to compounds of the formula (I), wherein theresidues R 1 to R , 5 V, G and M have the meanings indicated in the claims. The compounds of the formula (I) are valuable pharmacologically active compounds for use in thetreatmentof diverse disorders, for example cardiovascular disorders like thromboembolic diseases or restenoses. The compounds of the invention are effective antagonists of the platelet LPA receptor LPAR5 (GPR92) and can in general be applied in conditions in which an undesired activation of the platelet LPA receptor LPAR5, the mast cell LPA receptor LPAR5 or the microglia cell LPA receptor LPAR5 present is or for the cure or prevention of which an inhibition of the platelet, mast cell or microglia cell LPA recept­ or LPAR5 is intended. The invention furthermore relates to processes for the preparation of compounds of the formula (I), their use, in particular as active ingredients in medicaments, and pharmaceutical compositions comprising them.