Patent SG-11201805235X-A (SG)
Title: Polymorphic crystalline forms of obeticholic acid
Inventor: STEINER ANDRÉ
IPC: C07J51/00
Filed: 2016-01-08
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property -, Organization MD 1111101110101011111 HO 11111 01E33 0111111011111011111011 III International Bureau ... .... ..Yjd (10) International Publication Number (43) International Publication Date ..... ...r .....1 WO 2017/111979 Al 29 June 2017(29.06.2017) WIPO I PCT (51) International Patent Classification: morphix Ltd., 250 Cambridge Science Park, Milton Road, C07J 9/00 (2006.01) A61K 31/575 (2006.01) Cambridge CB4 OWE (GB). C07J 17/00 (2006.01) A61P 1/16 (2006.01) (74) Agent: IWAMOTO-FAN, Michelle; Intercept Pharma- C07J 51/00 (2006.01) ceuticals, Inc., 450 W. 15th Suite 505, New York, NY (21) International Application Number: 10011 (US). PCT/US2016/012651 (81) Designated States (unless otherwise indicated, for every (22) International Filing Date: kind of national protection available): AE, AG, AL, AM, 8 January 2016 (08.01.2016) AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, (25) Filing Language: English DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, (26) Publication Language: English HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, (30) Priority Data: MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, 14/979,005 22 December 2015 (22.12.2015) US PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, (71) Applicant: INTERCEPT PHARMACEUTICALS, INC. SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, [US/US]; 450 W. 15th Suite 505, New York, NY 10011 TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (US). (84) Designated States (unless otherwise indicated, for every (72) Inventors: STEINER, Andre; PharmaZell GmbH, Rosen- kind of regional protection available): ARIPO (BW, GH, heimer Str. 43, 83064 Raubling (DE). WAENERLUND GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, POULSEN, Heidi; FeF Chemicals A/S, Kobenbavnsvej TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, 216, 4600 Koge (DK). JOLIBOIS, Emilie; Pharmorphix TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, Ltd., 250 Cambridge Science Park, Milton Road, Cam- DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, bridge CB4 OWE (GB). REWOLINSKI, Melissa; 4350 LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, La Jolla Village Drive, Suite 960, San Diego, CA 92122 SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, (US). GROSS, Ralf; PharmaZell GmbH, Rosenheimer Str. GW, KM, ML, MR, NE, SN, TD, TG). = 43, 83064 Raubling (DE). SHARP, Emma; Pharmorphix Published: Ltd., 250 Cambridge Science Park, Milton Road, Cam- bridge CB4 OWE (GB). DUBAS-FISHER, Fiona; Phar- with international search report (Art. 21(3)) morphix Ltd., 250 Cambridge Science Park, Milton Road, Cambridge CB4 OWE (GB). EBERLIN, Alex; Phar- (54) Title: POLYMORPHIC CRYSTALLINE FORMS OF OBETICHOLIC ACID CO2H 1-1 C:r IN o, ,-, ,-, ,-, H 0 ‘ / OH - _ IN 1-1 (57) : The present application relates to crystalline forms A, D, F, G and I of obeticholic acid. These crystalline forms are 0 useful in the production of Obeticholic acid (in particular its purification), which is a drug useful for the treatment or prevention of a \" FXR mediated disease or condition, cardiovascular disease or cholestatic liver disease, and for reducing HDL cholesterol, for lower - 0 ing triglycerides in a mammal, or for inhibition of fibrosis.