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1. WO2020087901 - RHO KINASE INHIBITOR, METHOD FOR PREPARING SAME AND USES THEREOF

Publication Number WO/2020/087901
Publication Date 07.05.2020
International Application No. PCT/CN2019/085689
International Filing Date 06.05.2019
IPC
C07D 401/12 2006.01
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
12linked by a chain containing hetero atoms as chain links
A61K 31/551 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
55having seven-membered rings, e.g. azelastine, pentylenetetrazole
551having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep
A61P 9/10 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9Drugs for disorders of the cardiovascular system
10for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
A61P 25/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
Applicants
  • 北京盈科瑞创新药物研究有限公司 BEIJING INCREASE INNOVATIVE DRUG CO., LTD [CN]/[CN]
Inventors
  • 张保献 ZHANG, Baoxian
  • 张宏武 ZHANG, Hongwu
  • 胡杰 HU, Jie
  • 康志云 KANG, Zhiyun
  • 薛春美 XUE, Chunmei
  • 李文慧 LI, Wenhui
  • 宋艳威 SONG, Yanwei
  • 吴珍珍 WU, Zhenzhen
  • 陈安平 CHEN, Anping
  • 王芳 WANG, Fang
  • 任恒春 REN, Hengchun
  • 李军 LI, Jun
Agents
  • 中国国际贸易促进委员会专利商标事务所 CCPIT PATENT AND TRADEMARK LAW OFFICE
Priority Data
201811275571.030.10.2018CN
Publication Language Chinese (ZH)
Filing Language Chinese (ZH)
Designated States
Title
(EN) RHO KINASE INHIBITOR, METHOD FOR PREPARING SAME AND USES THEREOF
(FR) INHIBTEUR DE RHO KINASE, SON PROCÉDÉ DE PRÉPARATION ET SON UTILISATION
(ZH) 一种Rho激酶抑制剂及其制备方法和应用
Abstract
(EN)
Provided are an Rho kinase inhibitor, a method for preparing same and the uses thereof. The Rho kinase inhibitor designates a compound of formula (I), a stereoisomer or pharmaceutically acceptable salt thereof. The Rho kinase inhibitor promotes endothelial cells and endothelin expression, prostenin expression, and vascular factors NO synthesis and secretion, has a promoting effect on proprostin expression independently of the doses used, shows lower toxicity, while being safer.
(FR)
L’invention concerne un inhibiteur de Rho kinase, son procédé de préparation et son utilisation. Cet inhibiteur de Rho kinase désigne un composé de formule I, un stéréo-isomère et son sel pharmaceutiquement acceptable. L’inhibiteur de Rho kinase favorise les cellules endothéliales et l'expression d’endothéline, l'expression de prosténine, ainsi que la synthèse et la sécrétion de NO sur les facteurs vasomoteurs. Il agit sur l'expression de proprostine en la promouvant quelles que soient les doses utilisées, fait preuve d’une faible toxicité tout en étant plus sûr.
(ZH)
一种Rho激酶抑制剂及其制备方法和应用。所述Rho激酶抑制剂为式I所示的化合物、其立体异构体或其药学上可接受的盐。该Rho激酶抑制剂对内皮细胞内皮素的表达、对前列环素的表达、舒血管因子NO的合成和分泌均为促进作用,无论在高、中、低剂量均对前列环素的表达起到促进作用,并且表现出更低的毒性,更好的安全性。
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