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1. (WO2017111979) POLYMORPHIC CRYSTALLINE FORMS OF OBETICHOLIC ACID
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2017/111979 International Application No.: PCT/US2016/012651
Publication Date: 29.06.2017 International Filing Date: 08.01.2016
IPC:
C07J 9/00 (2006.01) ,C07J 17/00 (2006.01) ,C07J 51/00 (2006.01) ,A61K 31/575 (2006.01) ,A61P 1/16 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
J
STEROIDS
9
Normal steroids containing carbon, hydrogen, halogen, or oxygen, substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
J
STEROIDS
17
Normal steroids containing carbon, hydrogen, halogen, or oxygen, having an oxygen-containing hetero ring not condensed with the cyclopenta[a]hydrophenanthrene skeleton
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
J
STEROIDS
51
Normal steroids with unmodified cyclopenta[a]hydrophenanthrene skeleton not provided for in groups C07J1/-C07J43/151
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
56
Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
575
substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1
Drugs for disorders of the alimentary tract or the digestive system
16
for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
Applicants:
INTERCEPT PHARMACEUTICALS, INC. [US/US]; 10 Hudson Yards, 37th Floor New York, NY 10001, US
Inventors:
STEINER, André; DE
WAENERLUND POULSEN, Heidi; DK
JOLIBOIS, Emilie; GB
REWOLINSKI, Melissa; US
GROSS, Ralf; DE
SHARP, Emma; GB
DUBAS-FISHER, Fiona; GB
EBERLIN, Alex; GB
Agent:
IWAMOTO-FAN, Michelle; US
Priority Data:
14/979,00522.12.2015US
Title (EN) POLYMORPHIC CRYSTALLINE FORMS OF OBETICHOLIC ACID
(FR) FORMES CRISTALLINES POLYMORPHES DE L'ACIDE OBÉTICHOLIQUE
Abstract:
(EN) The present application relates to crystalline forms A, D, F, G and I of obeticholic acid. These crystalline forms are 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 lowering triglycerides in a mammal, or for inhibition of fibrosis.
(FR) La présente invention concerne des formes cristallines A, D, F, G et I de l'acide obéticholique. Ces formes cristallines sont utiles dans la production d'acide obéticholique (en particulier dans sa purification), qui est un médicament utile pour le traitement ou la prévention d'une maladie ou d'une affection, d'une maladie cardiovasculaire ou une maladie hépatique cholestatique médiées par le FXR et pour la réduction du cholestérol HDL, pour la diminution des triglycérides chez un mammifère ou pour l'inhibition de la fibrose.
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Designated States: 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, IR, IS, JP, KE, KG, KN, KP, KR, 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
African Regional Intellectual Property Organization (ARIPO) (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (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)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)
Also published as:
AU2016375566CA3009149MYPI 2018000967IL259998SG11201805235XKR1020180095070
CN108495858EP3394081MX2018007776BR112018012590EA201891491PH1/2018/501318
ID2019/01700