Patent SG-11201408501U-A (SG)
Title: Preparation, uses and solid forms of obeticholic acid
Inventor: STEINER ANDRÉ
IPC: A61K31/575
Filed: 2013-06-17
Abstract: (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 27 December 2013 (27.12.2013) WIPOIPCT (10) International Publication Number WO 2013/192097 A1 (51) International Patent Classification: C07J9/00 (2006.01) A61P1/16 (2006.01) A61K31/575 (2006.01) C07J51/00 (2006.01) (21) International Application Number: (22) International Filing Date: (25) Filing Language: (26) Publication Language: PCT/US2013/046150 17 June 2013 (17.06.2013) English (30) Priority Data: 61/661,531 19 June 2012 (19.06.2012) English US (71) Applicant: INTERCEPT PHARMACEUTICALS, INC. [US/US]; 18 Desbrosses Street, New York, NY 10013 (US). (72) Inventors: STEINER, Andre; PharmaZell GmbH, Rosen- heimer Str. 43, 83064 Raubling (DE). WAENERLUND POULSEN, Heidi; FeF Chemicals A/S, Kobenhavnsvej 216, DK-4600 K0ge (DK). JOLIBOIS, Emilie; Phar- morphix Ltd., 250 Cambridge Science Park, Milton Road, Cambridge CB4 OWE (GB). REWOLINSKI, Melissa; 4350 La Jolla Village Drive, Suite 960, San Diego, CA 92122 (US). GROSS, Ralf; PharmaZell GmbH, Rosen- heimer Str. 43, 83064 Raubling (DE). SHARP, Emma; Pharmorphix Ltd., 250 Cambridge Science Park, Milton Road, Cambridge CB4 OWE (GB). DUBAS-FISHER, Fiona; Pharmorphix Ltd., 250 Cambridge Science Park, Milton Road, Cambridge CB4 OWE (GB). EBERLIN, Alex; Pharmorphix Ltd., 250 Cambridge Science Park, Milton Road, Cambridge CB4 OWE (GB). (74) Agents: ELRIFI, Ivor, R. et al.; Mintz Levin Cohn Ferris Glovsky and Popeo, P.C., One Financial Center, Boston, MA 02111 (US). (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, 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, [Continued on next page] (54) Title: PREPARATION, USES AND SOLID FORMS OF OBETICHOLIC ACID l> 0\ © CJ 0\ FIG. 5 1600 1500 1400 1300 1200 1100- I\" 1000 o 900 O .S 800 • 700 600 500 400 300 200 100 0 I /^ir VVJVVH A*V. 20 2-Theta - Scale 30 40 (57) Abstract: The present invention relates to obeticholic acid: or a pharma- ceutically acceptable salt, solvate or amino acid conjugate thereof. Obetich­ olic acid is useful for the treatment or prevention of a FXR mediated disease or condition, cardiovascular disease or cholestatic liver disease, and for redu­ cing HDL cholesterol, for lowering triglycerides in a mammal, or for inhibi­ tion of fibrosis. The present invention also relates processes to for the synthes­ is of obeticholic acid. i-H o CJ o & WO 2013/192097 A1IIH 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, FT, 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). Published: — with international search report (Art. 21(3))