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1. (WO2019007418) FXR RECEPTOR AGONIST
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Pub. No.: WO/2019/007418 International Application No.: PCT/CN2018/094813
Publication Date: 10.01.2019 International Filing Date: 06.07.2018
IPC:
C07D 417/14 (2006.01) ,C07D 413/14 (2006.01) ,C07D 417/12 (2006.01) ,C07D 413/12 (2006.01) ,A61K 31/422 (2006.01) ,A61K 31/439 (2006.01) ,A61K 31/428 (2006.01) ,A61P 1/00 (2006.01) ,A61P 3/00 (2006.01) ,A61P 7/02 (2006.01) ,A61P 9/10 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
417
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/196
14
containing three or more hetero rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
413
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
14
containing three or more hetero rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
417
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/196
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
413
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
41
having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
42
Oxazoles
422
not condensed and containing further heterocyclic rings
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
435
having six-membered rings with one nitrogen as the only ring hetero atom
439
the ring forming part of a bridged ring system, e.g. quinuclidine
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
41
having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
425
Thiazoles
428
condensed with carbocyclic rings
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
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
7
Drugs for disorders of the blood or the extracellular fluid
02
Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
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
10
for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
Applicants:
山东轩竹医药科技有限公司 XUANZHU PHARMA CO., LTD. [CN/CN]; 中国山东省济南市 高新区天辰路2518号 2518 Tianchen Road, National High-Tech Development Zone Jinan, Shandong 250101, CN
Inventors:
方文奎 FANG, Wenkui Ken; CN
陈博 CHEN, Bo; CN
王听中 WANG, Tingzhong; CN
程静 CHENG, Jing; CN
Agent:
中国国际贸易促进委员会专利商标事务所 CCPIT PATENT AND TRADEMARK LAW OFFICE; 中国北京市 西城区阜成门外大街2号万通新世界广场8层 8th Floor, Vantone New World Plaza 2 Fuchengmenwai Street, Xicheng District Beijing 100037, CN
Priority Data:
201710547157.X06.07.2017CN
Title (EN) FXR RECEPTOR AGONIST
(FR) AGONISTE DU RÉCEPTEUR FXR
(ZH) FXR受体激动剂
Abstract:
(EN) The present invention relates to the technical field of pharmacy, and specifically relates to a compound as represented by formula (I), and a pharmaceutically acceptable salt, an ester or stereoisomers thereof. R1, X1, X2, M, Ar, ring A, ring B, and L are as defined in the description. The present invention further relates to a method for preparing the compound, and the pharmaceutically acceptable salt, the ester or the stereoisomers thereof, a pharmaceutical composition and a pharmaceutical preparation comprising the compound, and the pharmaceutically acceptable salt, the ester or the stereoisomers thereof, and an application of the compound, and the pharmaceutically acceptable salt, the ester or the stereoisomers thereof in preparation of a drug for treating and/or preventing an FXR receptor-mediated disease.
(FR) La présente invention se rapporte au domaine technique de la pharmacie, et concerne particulièrement un composé tel que représenté par la formule (I), et un sel pharmaceutiquement acceptable, un ester ou des stéréoisomères de celui-ci. R1, X1, X2, M, Ar, le cycle A, le cycle B et L sont tels que définis dans la description. La présente invention concerne en outre un procédé de préparation du composé, et le sel pharmaceutiquement acceptable, l'ester ou les stéréoisomères de celui-ci, une composition pharmaceutique et une préparation pharmaceutique comprenant le composé, et le sel pharmaceutiquement acceptable, l'ester ou les stéréoisomères de celui-ci, et une application du composé, et le sel pharmaceutiquement acceptable, l'ester ou les stéréoisomères de celui-ci dans la préparation d'un médicament pour le traitement et/ou la prévention d'une maladie induite par un récepteur FXR.
(ZH) 本发明属于医药技术领域,具体涉及式(I)所示的化合物、其药学上可接受的盐、其酯或它们的立体异构体,其中,R 1、X 1、X 2、M、Ar、环A、环B、L如说明书中所定义;本发明还涉及所述化合物、其药学上可接受的盐、其酯或它们的立体异构体的制备方法、含有所述化合物、其药学上可接受的盐、其酯或它们的立体异构体的药物组合物和药物制剂,及所述化合物、其药学上可接受的盐、其酯或它们的立体异构体在用于制备治疗和/或预防由FXR受体介导的疾病的药物中的应用。
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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, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JO, 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)