Patent SG-11201407216Y-A (SG)
Title: Benzo[1,3]dioxine derivatives and their use as lpar5 antagonists
Inventor: NAZARÉ MARC
IPC: C07D319/08
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 2013/171318 A1 (51) International Patent Classification: C07D 319/08 (2006.01) C07D 401/04 (2006.01) C07D 401/12 (2006.01) C07D 403/04 (2006.01) C07D 403/12 (2006.01) C07D 413/04 (2006.01) A61K 31/357 (2006.01) A61K31/4025 (2006.01) A61K 31/41 (2006.01) A61K31/4433 (2006.01) A61P9/00 (2006.01) (21) International Application Number: (22) International Filing Date: (25) Filing Language: (26) Publication Language: PCT/EP2013/060172 16 May 2013 (16.05.2013) English English (30) Priority Data: 12305553.5 18 May 2012 (18.05.2012) EP (71) Applicant: SANOFI [FR/FR]; 54 rue La Boetie, F-75008 Paris (FR). (72) Inventors: NAZARE, Marc; c/o Sanofi-Aventis Deutsch- land GmbH, 65926 Frankfurt am Main (DE). KOZIAN, Detlef; c/o Sanofi-Aventis Deutschland GmbH, 65926 Frankfurt am Main (DE). BOSSART, Martin; c/o Sanofi- Aventis Deutschland GmbH, 65926 Frankfurt am Main (DE). CZECHTIZKY, Werngard; c/o Sanofi-Aventis Deutschland GmbH, 65926 Frankfurt am Main (DE). EVERS, Andreas; c/o Sanofi-Aventis Deutschland GmbH, 65926 Frankfurt am Main (DE). (74) Agent: VENNE-DUNKER, Sabine; K 801, c/o San­ ofi-Aventis Deutschland GmbH, Patents Germany, Indus - triepark 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)) [Continued on next page] (54) Title: BENZO[l,3]DIOXINE DERIVATIVES AND THEIR USE AS LPAR5 ANTAGONISTS 00 i-H m i-H l> i-H cn i-H o CJ o & (I) (57) Abstract: The present invention relates to compounds of the formula (I), wherein the residues A, R 1 to R , 5 Z 1 and Z 2 have the meanings indicated in the claims. The compounds of the formula (I) are valuable pharmacologically active compounds for use in the treatment of 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 re - ceptor LPAR5 present is or for the cure or prevention of which an inhibition of the platelet, mast cell or microglia cell LPA receptor 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. WO 2013/171318 AlllllllH Published: — with international search report (Art. 21(3))