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1. (WO2017008773) CRYSTALLINE FORMS OF OBETICHOLIC ACID
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2017/008773 International Application No.: PCT/CZ2016/000078
Publication Date: 19.01.2017 International Filing Date: 18.07.2016
IPC:
C07J 9/00 (2006.01) ,A61K 31/575 (2006.01) ,A61P 3/00 (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
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
3
Drugs for disorders of the metabolism
Applicants:
ZENTIVA, K.S. [CZ/CZ]; U Kabelovny 130 102 37 Praha 10, CZ
Inventors:
OBADALOVA, Iva; CZ
DAMMER, Ondrej; CZ
KREJCIK, Lukas; CZ
HERT, Jakub; CZ
Agent:
JIROTKOVA, Ivana; ROTT, RUZICKA & GUTTMANN Vinohradska 37, 120 00 Praha 2, CZ
Priority Data:
PV 2015-50416.07.2015CZ
Title (EN) CRYSTALLINE FORMS OF OBETICHOLIC ACID
(FR) FORMES CRISTALLINES D’ACIDE OBÉTICHOLIQUE
Abstract:
(EN) Obeticholic acid is a semi-synthetic bile acid analogue with an agonist effect upon the farnesoid X receptor (FXR). It is designed for the treatment of liver diseases, e.g. primary biliary cirrhosis (PBC), non-alcoholic steatohepatitis (NASH) or primary sclerosing cholangitis (PSC). The present invention relates to crystalline forms of obeticholic acid of formula I, with the systematic name (3α,5β,6α,7α)-6-ethyl-3,7-dihydroxycholan-24-oic acid, a method for preparation and use thereof for the production of a dosage form. These crystalline forms can be advantageously used to increase purity of obeticholic acid and also for the preparation of its amorphous form.
(FR) La présente invention concerne l’acide obéticholique qui est un analogue de l’acide semi-synthétique biliaire avec un effet agoniste sur le récepteur farnésoïde X (FXR). Il est conçu pour le traitement des maladies hépatiques, par exemple la cirrhose biliaire primaire (PBC), la stéatohépatite non alcoolique (NASH) ou la cholangite sclérosante primaire (PSC). La présente invention concerne les formes cristallines de l’acide obéticholique de formule I, avec le nom systémique d'acide (3α,5β,6α,7α)-6-éthyl-3,7-dihydroxycholan-24-oïque, un procédé pour sa préparation et son utilisation pour la production d’une forme dosifiée. Lesdites formes cristallines peuvent être avantageusement utilisées pour accroître la pureté de l’acide obéticholique et également pour la préparation de sa forme amorphe.
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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)