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1. WO2020114307 - ISOXAZOLE DERIVATIVE, PREPARATION METHOD THEREFOR AND USE THEREOF

Publication Number WO/2020/114307
Publication Date 11.06.2020
International Application No. PCT/CN2019/121534
International Filing Date 28.11.2019
IPC
C07D 413/12 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
413Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
02containing two hetero rings
12linked by a chain containing hetero atoms as chain links
A61K 31/422 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
41having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
42Oxazoles
422not condensed and containing further heterocyclic rings
C07D 413/14 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
413Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
14containing three or more hetero rings
Applicants
  • 四川科伦博泰生物医药股份有限公司 SICHUAN KELUN-BIOTECH BIOPHARMACEUTICAL CO., LTD. [CN]/[CN]
Inventors
  • 刘金明 LIU, Jinming
  • 蔡家强 CAI, Jiaqiang
  • 吴勇勇 WU, Yongyong
  • 崔洪 CUI, Hong
  • 王超磊 WANG, Chaolei
  • 田强 TIAN, Qiang
  • 宋宏梅 SONG, Hongmei
  • 薛彤彤 XUE, Tongtong
  • 王利春 WANG, Lichun
  • 王晶翼 WANG, Jingyi
Agents
  • 北京永新同创知识产权代理有限公司 NTD UNIVATION INTELLECTUAL PROPERTY AGENCY LTD
Priority Data
201811492827.307.12.2018CN
Publication Language Chinese (ZH)
Filing Language Chinese (ZH)
Designated States
Title
(EN) ISOXAZOLE DERIVATIVE, PREPARATION METHOD THEREFOR AND USE THEREOF
(FR) DÉRIVÉ D'ISOXAZOLE, SON PROCÉDÉ DE PRÉPARATION ET SON UTILISATION
(ZH) 异噁唑衍生物及其制备方法和用途
Abstract
(EN)
The present invention relates to an isoxazole derivative, a preparation method therefor and a use thereof. Specifically, provided are a farnesoid X receptor (FXR) agonist compound and stereoisomers, tautomers, polymorphs, solvates (such as hydrates), pharmaceutically acceptable salts, esters, metabolites, N-oxides, chemically protected forms and prodrugs thereof. Further provided are a method for preparing the described compound, intermediates, pharmaceutical compositions and kits containing the compound, and a use thereof in treating diseases or conditions mediated by FXR.
(FR)
La présente invention concerne un dérivé d'isoxazole, son procédé de préparation et son utilisation. L'invention concerne particulièrement un composé agoniste du récepteur farnésoïde X (FXR) et des stéréoisomères, des tautomères, des polymorphes, des solvates (tels que des hydrates), des sels pharmaceutiquement acceptables, des esters, des métabolites, des N-oxydes, des formes chimiquement protégées et des promédicaments de celui-ci. L'invention concerne en outre un procédé de préparation dudit composé, des intermédiaires, des compositions pharmaceutiques et des kits contenant le composé, et une utilisation de celui-ci dans le traitement de maladies ou d'états pathologiques à médiation par FXR.
(ZH)
涉及一种异噁唑衍生物及其制备方法和用途。具体地,提供类法尼醇X受体(FXR)激动剂化合物以及其立体异构体、互变异构体、多晶型物、溶剂合物(如水合物)、药学可接受的盐、酯、代谢物、N-氧化物以及其化学保护的形式和前药。还提供所述化合物的制备方法、中间体、包含所述化合物的药物组合物和药盒以及它们用于治疗由FXR介导的疾病或病症的用途。
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