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1. WO2020094008 - 2-OXO-1,2-DIHYDROQUINOLINE DERIVATIVES, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL APPLICATIONS THEREOF

Publication Number WO/2020/094008
Publication Date 14.05.2020
International Application No. PCT/CN2019/115718
International Filing Date 05.11.2019
IPC
C07D 215/227 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
215Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
02having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
16with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
20Oxygen atoms
22attached in position 2 or 4
227only one oxygen atom which is attached in position 2
C07D 215/48 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
215Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
02having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
16with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
48Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
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
A61P 7/02 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
7Drugs for disorders of the blood or the extracellular fluid
02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
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 11/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11Drugs for disorders of the respiratory system
Applicants
  • 天津药物研究院有限公司 TIANJIN INSTITUTE OF PHARMACEUTICAL RESEARCH CO., LTD. [CN]/[CN]
Inventors
  • 魏群超 WEI, Qunchao
  • 郑志超 ZHENG, Zhichao
  • 张士俊 ZHANG, Shijun
  • 王岩石 WANG, Yanshi
  • 高琪 GAO, Qi
  • 郑学敏 ZHENG, Xuemin
  • 李玉荃 LI, Yuquan
  • 刘巍 LIU, Wei
  • 黄长江 HUANG, Changjiang
  • 靳京 JIN, Jing
  • 刘磊 LIU, Lei
  • 孔晓华 KONG, Xiaohua
  • 刘旭圆 LIU, Xuyuan
  • 袁静 YUAN, Jing
  • 汤立达 TANG, Lida
  • 魏巍 WEI, Wei
Agents
  • 北京泛华伟业知识产权代理有限公司 PANAWELL & PARTNERS, LLC
Priority Data
201811310427.606.11.2018CN
Publication Language Chinese (ZH)
Filing Language Chinese (ZH)
Designated States
Title
(EN) 2-OXO-1,2-DIHYDROQUINOLINE DERIVATIVES, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL APPLICATIONS THEREOF
(FR) DÉRIVÉS DE 2-OXO-1,2-DIHYDROQUINOLÉINE, PROCÉDÉ DE PRÉPARATION CORRESPONDANT, ET UTILISATIONS PHARMACEUTIQUES ASSOCIÉES
(ZH) 2-氧代-1,2-二氢喹啉类衍生物、其制备方法及其在医药上的应用
Abstract
(EN)
Provided are a 2-oxo-1,2-dihydroquinoline compound represented by formula (I), a preparation method therefor, and use thereof in drugs for preventing and/or treating thromboembolic diseases and/or thromboembolic complications, wherein R 1 is selected from (II); R 2 is selected from C 1-6 alkyl groups; n is selected from 0, 1, and 2. The compound has high activity, high solubility and better pharmacokinetic properties. (I)
(FR)
L'invention concerne un composé de 2-oxo-1,2-dihydroquinoléine représenté par la formule (I), son procédé de préparation et son utilisation dans des médicaments pour la prévention et/ou le traitement de maladies thromboemboliques et/ou de complications thromboemboliques, R 1 étant choisi parmi (II) ; R 2 étant choisi parmi des groupes alkyle en C 1-6 ; n étant choisi parmi 0, 1 et 2. Le composé a une haute activité, une solubilité élevée et de meilleures propriétés pharmacocinétiques. (I)
(ZH)
涉及一种式(I)所示的2-氧代-1,2-二氢喹啉类化合物、其制备方法以及其在用于预防和/或治疗血栓栓塞性疾病和/或血栓栓塞并发症的药物中的用途,其中,R 1选自式(II);R 2选自C 1-6烷基;n选自0、1和2。所述化合物具有高活性、高溶解性和更好的药代动力学性质。
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