Patent SG-11201803627X-A (SG)
Title: N-substituted indole derivatives as pge2 receptor modulators
Inventor: FRETZ HEINZ
IPC: C07D417/14
Filed: 2016-11-17
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 26 May 2017(26.05.2017) WIPOIPCT (10) International Publication Number WO 2017/085198 A1 (51) International Patent Classification: (30) (71) (72) C07D 403/12 (2006.01) C07D 413/14 (2006.01) C07D 403/14 (2006.01) C07D 409/14 (2006.01) C07D 417/14 (2006.01) A61K31/506 (2006.01) A61P 35/00 (2006.01) A61P 25/00 (2006.01) A61P9/00 (2006.01) A61P11/00 (2006.01) A61P15/00 (2006.01) (21) International Application Number: PCT/EP2016/078028 (22) International Filing Date: (25) Filing Language: (26) Publication Language 17 November 2016 (17.11.2016) English English Priority Data: PCT/EP2015/077269 20 November 2015 (20.11.2015) EP Applicant: ACTELION PHARMACEUTICALS LTD [CH/CH]; Gewerbestrasse 16, 4123 Allschwil (CH). Inventors: FRETZ, Heinz; c/o Actelion Pharmaceuticals Ltd, Gewerbestrasse 16, 4123 Allschwil (CH). LYOTHI- ER, Isabelle; c/o Actelion Pharmaceuticals Ltd, Gewerbe­ strasse 16, 4123 Allschwil (CH). POTHIER, Julien; c/o Actelion Pharmaceuticals Ltd, Gewerbestrasse 16, 4123 Allschwil (CH). RICHARD-BILDSTEIN, Sylvia; c/o Ac­ telion Pharmaceuticals Ltd, Gewerbestrasse 16, 4123 All­ schwil (CH). SIFFERLEN, Thierry; c/o Actelion Phar­ maceuticals Ltd, Gewerbestrasse 16, 4123 Allschwil (CH). WYDER PETERS, Lorenza; c/o Actelion Pharmaceutic­ als Ltd, Gewerbestrasse 16, 4123 Allschwil (CH). POZZI, Davide; c/o Actelion Pharmaceuticals Ltd, Gewerbestrasse 16, 4123 Allschwil (CH). CORMINBOEUF, Olivier; c/o Actelion Pharmaceuticals Ltd, Gewerbestrasse 16, 4123 Allschwil (CH). (74) Agent: VELKER, Jorg; c/o Actelion Pharmaceuticals Ltd, Gewerbestrasse 16, 4123 Allschwil (CH). (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, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, 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, SA, 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, ST, 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, KM, ML, MR, NE, SN, TD, TG). Declarations under Rule 4.17: — as to applicant's entitlement to apply for and be granted a patent (Rule 4.17(H)) [Continued on next page] (54) Title: N - SUB STITUTED INDOLE DERIVATIVES AS PGE2 RECEPTOR MODULATORS 00 ON ICi 00 n O Ar 1 (I) (57) : The present invention relates to derivativesof formula (I) wherein (R*)n, R2, R3, R4a, R4b, R5a, R5b and Ar1 are as de­ scribed in the description, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as modulators of the prostaglandin 2 receptors EP2 and/or EP4. WO 2017/085198 A11II III IIII III III III 11II III Hill lllll lllll II lllll III mill llll Ill III Published: — with international search report (Art. 21(3))