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1. (WO2017152677) CHOLANIC ACID COMPOUND FOR PREVENTING OR TREATING FXR-MEDIATED DISEASES
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Pub. No.: WO/2017/152677 International Application No.: PCT/CN2016/109851
Publication Date: 14.09.2017 International Filing Date: 14.12.2016
IPC:
C07J 9/00 (2006.01) ,C07B 59/00 (2006.01) ,A61K 31/575 (2006.01) ,A61P 35/00 (2006.01) ,A61P 1/16 (2006.01) ,A61P 1/00 (2006.01) ,A61P 13/12 (2006.01) ,A61P 9/00 (2006.01) ,A61P 3/00 (2006.01) ,A61P 3/10 (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
B
GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
59
Introduction of isotopes of elements into organic compounds
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
35
Antineoplastic agents
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
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
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
13
Drugs for disorders of the urinary system
12
of the kidneys
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9
Drugs for disorders of the cardiovascular system
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
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
08
for glucose homeostasis
10
for hyperglycaemia, e.g. antidiabetics
Applicants:
深圳市塔吉瑞生物医药有限公司 SHENZHEN TARGETRX, INC. [CN/CN]; 中国广东省深圳 南山区科苑路15号科兴科学园A1栋301 Room 301,Building A1 Kexing Science Park, No.15 of Keyuan Road, Nanshan District Shenzhen, Guangdong 5180057, CN
Inventors:
王义汉 WANG, Yihan; CN
任兴业 RE, Xingye; CN
Priority Data:
201610141005.511.03.2016CN
201610409536.812.06.2016CN
Title (EN) CHOLANIC ACID COMPOUND FOR PREVENTING OR TREATING FXR-MEDIATED DISEASES
(FR) COMPOSÉ D'ACIDE CHOLANIQUE POUR LA PRÉVENTION OU LE TRAITEMENT DE MALADIES MÉDIÉE PAR FXR
(ZH) 用于预防或治疗FXR-介导疾病的胆烷酸化合物
Abstract:
(EN) The present invention relates to a cholanic acid compound for preventing or treating FXR-mediated diseases. Specifically, disclosed are a cholanic acid compound represented by formula (I) and a pharmaceutical composition containing the compound, or a crystalline form, a pharmaceutically-acceptable salt, a prodrug, a tautomer, a stereoisomer, an enantiomer, and a hydrate or a solvate thereof. The compound in the present invention can be used as a farnesol X receptor agonist and can therefore be applied to the preparation of drugs for treating FXR-related diseases (for example, fatty liver).
(FR) La présente invention concerne un composé d'acide cholanique pour prévenir ou traiter des maladies médiées par FXR. L'invention concerne plus particulièrement un composé d'acide cholanique représenté par la formule (I) et une composition pharmaceutique contenant le composé, ou une forme cristalline, un sel pharmaceutiquement acceptable, un promédicament, un tautomère, un stéréo-isomère, un énantiomère et un hydrate ou un solvate correspondants. Le composé de la présente invention peut être utilisé en tant qu'agoniste du récepteur de farnésol X et peut par conséquent être appliqué à la préparation de médicaments pour le traitement de maladies liées au FXR (par exemple, la stéatose hépatique).
(ZH) 本发明涉及了一种用于预防或治疗FXR-介导疾病的胆烷酸化合物。具体地,该发明公开了式(I)所示的胆烷酸化合物以及含有该化合物、或其晶型、药学上可接受的盐、前药、互变异构体和立体异构体、对映异构体、水合物或溶剂合物的药物组合物。本发明所述化合物可作为法尼醇X受体激动剂,进而可适用于制备治疗FXR相关疾病(如脂肪肝等)的药物。
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, DJ, 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, 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
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 Office (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (EPO) (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: Chinese (ZH)
Filing Language: Chinese (ZH)