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1. WO2022001331 - A CLASS OF TRICYCLIC COMPOUNDS, PREPARATION METHOD THEREFOR, AND MEDICAL USE THEREOF

Publication Number WO/2022/001331
Publication Date 06.01.2022
International Application No. PCT/CN2021/090073
International Filing Date 27.04.2021
IPC
C07D 405/04 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
405Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
02containing two hetero rings
04directly linked by a ring-member-to-ring- member bond
C07D 211/14 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
211Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
04with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
06having no double bonds between ring members or between ring members and non-ring members
08with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
10with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms
14with hydrocarbon or substituted hydrocarbon radicals attached to the ring nitrogen atom
C07D 401/06 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02containing two hetero rings
06linked by a carbon chain containing only aliphatic carbon atoms
Applicants
  • 合肥医工医药股份有限公司 HEFEI INSTITUTE OF PHARMACEUTICAL INDUSTRY CO., LTD. [CN]/[CN]
  • 合肥恩瑞特药业有限公司 HEFEI AMVITE PHARMACEUTICAL CO., LTD. [CN]/[CN]
Inventors
  • 何广卫 HE, Guangwei
  • 储昭兴 CHU, Zhaoxing
  • 许勤龙 XU, Qinlong
  • 莫佳佳 MO, Jiajia
  • 林高峰 LIN, Gaofeng
  • 赵炎 ZHAO, Yan
  • 邵莉 SHAO, Li
Priority Data
202010629198.503.07.2020CN
Publication Language Chinese (zh)
Filing Language Chinese (ZH)
Designated States
Title
(EN) A CLASS OF TRICYCLIC COMPOUNDS, PREPARATION METHOD THEREFOR, AND MEDICAL USE THEREOF
(FR) CLASSE DE COMPOSÉS TRICYCLIQUES, PROCÉDÉ DE PRÉPARATION CORRESPONDANT ET UTILISATION MÉDICALE ASSOCIÉE
(ZH) 一类三环化合物、制备方法及其医药用途
Abstract
(EN) Provided in the present invention is a class of tricyclic compounds, a preparation method therefor, and the medical use thereof. The tricyclic compounds are compounds having the structure of the following formula (I) or a pharmaceutically acceptable salt, a prodrug, a tautomer, a stereoisomer, or a mixture of stereoisomers thereof. The compounds of the present invention have a significant activity in terms of antagonizing histamine H 1 receptors, and has fewer side effects against anti-M-choline and a lower hERG toxicity. Specifically, the definitions of each group are as set forth in the description.
(FR) La présente invention concerne une classe de composés tricycliques, un procédé de préparation correspondant et une utilisation médicale associée. Les composés tricycliques sont des composés ayant la structure de la formule suivante (I) ou un sel pharmaceutiquement acceptable, un promédicament, un tautomère, un stéréoisomère ou un mélange de stéréoisomères de ceux-ci. Les composés selon la présente invention ont une activité significative en termes d'antagonisme des récepteurs de l'histamine H 1, et ont moins d'effets secondaires contre l'anti-M-choline et une très faible toxicité hERG. Plus précisément, les définitions de chaque groupe sont telles que représentées dans la description.
(ZH) 本发明提供一类三环化合物、其制备方法和医药用途,所述三环化合物是具有下列式(I)结构的化合物或其药学上可接受的盐、前药、互变异构体、立体异构体或者立体异构体的混合物。本发明化合物具有显著的拮抗组胺H 1受体的活性,且抗M-胆碱副作用更低,hERG毒性更低。其中,基团如说明书中所述定义。
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