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1. WO2020001304 - FXR RECEPTOR AGONIST

Publication Number WO/2020/001304
Publication Date 02.01.2020
International Application No. PCT/CN2019/091482
International Filing Date 17.06.2019
IPC
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
453
Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
06
containing iso-quinuclidine ring systems
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
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
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
3
Drugs for disorders of the metabolism
08
for glucose homeostasis
10
for hyperglycaemia, e.g. antidiabetics
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
04
for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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
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
C07D 453/06 (2006.01)
A61P 9/10 (2006.01)
A61P 1/16 (2006.01)
A61P 7/02 (2006.01)
A61P 3/10 (2006.01)
A61P 1/04 (2006.01)
CPC
A61K 31/439
A61P 1/04
A61P 1/16
A61P 3/10
A61P 35/00
A61P 7/02
Applicants
  • 轩竹(海南)医药科技有限公司 XUANZHU (HAINAN) BIOPHARMACEUTICAL CO., LTD. [CN/CN]; 中国海南省海口市 龙华区海滨大道85号天邑国际大厦27楼 27th Floor, Tianyi International Building, No. 85 Binhai Avenue, Longhua District Haikou, Hainan 570105, CN
Inventors
  • 方文奎 FANG, Wenkui Ken; CN
  • 王听中 WANG, Tingzhong; CN
  • 程静 CHENG, Jing; CN
Priority Data
201810665888.926.06.2018CN
Publication Language Chinese (ZH)
Filing Language Chinese (ZH)
Designated States
Title
(EN) FXR RECEPTOR AGONIST
(FR) AGONISTE DU RÉCEPTEUR FXR
(ZH) FXR受体激动剂
Abstract
(EN)
The present invention falls within the field of medical technology, and in particular relates to a compound as shown in formula (I), and a pharmaceutically acceptable salt, ester or stereoisomer thereof, wherein R1, R2, X1, X2, X3, M, Ar, and rings B and L are as defined in the description. Also involved are the preparation methods and pharmaceutical preparations of the compounds, and the uses of same in the preparation of drugs for treating and/or preventing related diseases mediated by FXR receptors, such as alcoholic fatty liver, nonalcoholic fatty liver, primary biliary cirrhosis, lipid metabolism disorders, diabetic complications, and malignant tumors.
(FR)
La présente invention se rapporte au domaine de la technologie médicale, et concerne en particulier un composé tel que représenté par la formule (I), et un sel, ester ou stéréoisomère pharmaceutiquement acceptable de celui-ci, R1, R2, X1, X2, X3, M, Ar et les cycles B et L étant tels que définis dans la description. L'invention concerne également des procédés de préparation et des préparations pharmaceutiques des composés, et leurs utilisations dans la préparation de médicaments pour le traitement et/ou la prévention de maladies associées à médiation par des récepteurs FXR, tels que le foie gras alcoolique, le foie gras non alcoolique, la cirrhose biliaire primaire, les troubles du métabolisme lipidique, les complications diabétiques et des tumeurs malignes.
(ZH)
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、酯或其立体异构体,R 1、R 2、X 1、X 2、X 3、M、Ar、环B和L如说明书中所定义;还涉及这些化合物的制备方法、药物制剂及在用于制备治疗和/或预防由FXR受体介导的酒精性脂肪肝、非酒精性脂肪肝、原发性胆汁性肝硬化、脂质代谢紊乱、糖尿病并发症及恶性肿瘤等相关疾病的药物中的应用。
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