Patent SG-11201810600W-A (SG)
Title: Fxr (nr1h4) modulating compounds
Inventor: BLOMGREN PETER A
IPC: A61K31/415
Filed: 2017-06-09
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property 1111111011110111011111111010111110011111101111111101H1111111111111111111111111111 Organization International Bureau (10) International Publication Number (43) International Publication Date .....0\"\"\"1 WO 2017/218337 Al 21 December 2017 (21.12.2017) WIP0 I PCT (51) International Patent Classification: MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, C07D 401/14 (2006.01) A61P 1/16 (2006.01) TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, CO7D 413/14 (2006.01) A61P 3/10 (2006.01) KM, ML, MR, NE, SN, TD, TG). A61K 31/42 (2006.01) A61P 35/00 (2006.01) A61K 31/415 (2006.01) Declarations under Rule 4.17: (21) International Application Number: — as to applicant's entitlement to apply for and be granted a PCT/US2017/036743 patent (Rule 4.17(H)) — as to the applicant's entitlement to claim the priority of the (22) International Filing Date: earlier application (Rule 4.17(iii)) 09 June 2017 (09.06.2017) Published: (25) Filing Language: English — with international search report (Art. 21(3)) (26) Publication Language: English — with sequence listing part of description (Rule 5.2(a)) (30) Priority Data: 62/349,479 13 June 2016 (13.06.2016) US (71) Applicant: GILEAD SCIENCES, INC. [US/US]; 333 Lakeside Drive, Foster City, CA 94404 (US). _ (72) Inventors: BLOMGREN, Peter A.; c/o Gilead Sciences, Inc., 333 Lakeside Drive, 333 Lakeside Drive, Foster City, CA 94404 (US). CURRIE, Kevin S.; c/o Gilead Sciences, — Inc., 333 Lakeside Drive, 333 Lakeside Drive, Foster City, CA 94404 (US). FARAND, Julie; c/o Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, CA 94404 (US). GEGE, Christian; c/o Phenex Pharmaceuticals AG, Donnersberg- = =_ weg 1, 67059 Ludwigshafen (DE). KROPF, Jeffrey E.; c/o _ Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, CA = 94404 (US). XU, Jianjun; c/o Gilead Sciences, Inc., 333 = Lakeside Drive, Foster City, CA 94404 (US). Agent: CAPPS, Kevin J. et al.; Gilead Sciences, Inc., 333 = (74) Lakeside Drive, Foster City, California 94404 (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, = DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, 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. = Designated States (unless otherwise indicated, for every (84) kind of regional protection available): ARIPO (BW, GH, = 1-1 IN er) er) 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, GC 1-1 ! (54) Title: FXR (NR1H4) MODULATING COMPOUNDS IN ,-1 (57) : The present disclosure relates generally to compounds which bind to the NR1H4 receptor (FXR) and act as agonists of 0 FXR. The disclosure further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/ \" or conditions through binding of said nuclear receptor by said compounds and to a process for the synthesis of said compounds.