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1. WO2020107500 - 2-(1-ACYLOXYPENTYL) BENZOIC ACID SALT FORMED BY BASIC AMINO ACID OR AMINOGUANIDINE, PREPARATION METHOD THEREFOR AND USES THEREOF

Publication Number WO/2020/107500
Publication Date 04.06.2020
International Application No. PCT/CN2018/118879
International Filing Date 03.12.2018
IPC
C07C 69/157 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
69Esters of carboxylic acids; Esters of carbonic or haloformic acids
02Esters of acyclic saturated monocarboxylic acids having the carboxyl group bound to an acyclic carbon atom or to hydrogen
12Acetic acid esters
14of monohydroxylic compounds
145of unsaturated alcohols
157containing six-membered aromatic rings
C07C 279/14 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
279Derivatives of guanidine, i.e. compounds containing the group the singly-bound nitrogen atoms not being part of nitro or nitroso groups
04having nitrogen atoms of guanidine groups bound to acyclic carbon atoms of a carbon skeleton
14being further substituted by carboxyl groups
C07C 69/78 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
69Esters of carboxylic acids; Esters of carbonic or haloformic acids
76Esters of carboxylic acids having an esterified carboxyl group bound to a carbon atom of a six-membered aromatic ring
78Benzoic acid esters
C07C 229/26 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
229Compounds containing amino and carboxyl groups bound to the same carbon skeleton
02having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
04the carbon skeleton being acyclic and saturated
26having more than one amino group bound to the carbon skeleton, e.g. lysine
C07D 233/64 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
233Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
54having two double bonds between ring members or between ring members and non-ring members
64with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
C07C 279/02 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
279Derivatives of guanidine, i.e. compounds containing the group the singly-bound nitrogen atoms not being part of nitro or nitroso groups
02Guanidine; Salts, complexes or addition compounds thereof
CPC
A61P 7/02
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
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
C07C 229/26
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
229Compounds containing amino and carboxyl groups bound to the same carbon skeleton
02having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
04the carbon skeleton being acyclic and saturated
26having more than one amino group bound to the carbon skeleton, e.g. lysine
C07C 277/08
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
277Preparation of guanidine or its derivatives, i.e. compounds containing the group , the singly-bound nitrogen atoms not being part of nitro or nitroso groups
08of substituted guanidines
C07C 279/02
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
279Derivatives of guanidine, i.e. compounds containing the group , the singly-bound nitrogen atoms not being part of nitro or nitroso groups
02Guanidine; Salts, complexes or addition compounds thereof
C07C 279/14
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
279Derivatives of guanidine, i.e. compounds containing the group , the singly-bound nitrogen atoms not being part of nitro or nitroso groups
04having nitrogen atoms of guanidine groups bound to acyclic carbon atoms of a carbon skeleton
14being further substituted by carboxyl groups
Applicants
  • 中国药科大学 CHINA PHARMACEUTICAL UNIVERSITY [CN]/[CN]
Inventors
  • 张奕华 ZHANG, Yihua
  • 黄张建 HUANG, Zhangjian
  • 朱嘉熠 ZHU, Jiayi
Agents
  • 南京苏高专利商标事务所(普通合伙) NANJING SUGAO PATENT AND TRADEMARK FIRM ( ORDINARY PARTNERSHIP )
Priority Data
201811440339.828.11.2018CN
Publication Language Chinese (ZH)
Filing Language Chinese (ZH)
Designated States
Title
(EN) 2-(1-ACYLOXYPENTYL) BENZOIC ACID SALT FORMED BY BASIC AMINO ACID OR AMINOGUANIDINE, PREPARATION METHOD THEREFOR AND USES THEREOF
(FR) SEL DE 2-(1)-ACYLOXYPENTYL) ACIDE BENZOÏQUE FORMÉ PAR UN ACIDE AMINÉ BASIQUE OU AMINOGUANIDINE, SON PROCÉDÉ DE PRÉPARATION ET SES APPLICATIONS
(ZH) 2-(1-酰氧正戊基)苯甲酸与碱性氨基酸或氨基胍形成的盐、其制备方法及用途
Abstract
(EN)
The present invention provides a 2-(1-acyloxypentyl) benzoic acid salt formed by basic amino acid or aminoguanidine, a preparation method thereof, a pharmaceutical preparation containing the salt and the uses of the pharmaceutical preparation in preparing drugs for preventing or treating cardiovascular diseases and cerebral ischemia, antithrombotic disorders while improving heart-cerebral circulation disorders. The compound disclosed therein has excellent water solubility, water solution stability, and pharmacokinetic properties, while showing reinforced resisting platelet aggregation, antithrombotic action, anti-cerebral ischemia and neuroprotective effect.
(FR)
L’invention concerne un sel de 2-(1)-acyloxypentyl) acide benzoïque formé par un acide aminé basique ou aminoguanidine, son procédé de préparation, sa préparation pharmaceutique et les applications de la préparation pharmaceutique pour la préparation de médicaments pour la prévention ou le traitement de maladies cardiovasculaires, de l’ischémie cérébrale et de la thrombose tout en améliorant les troubles de la circulation sanguine coeur-cerveau. Le composé est remarquable de par son hydrosolubilité, sa stabilité aqueuse et ses propriétés pharmacocinétiques tout en faisant preuve d’une agrégation plaquettaire renforcée, son action antithrombose et antiischémie cérébrale et son effet neuroprotecteur.
(ZH)
本发明提供了一种2-(1-酰氧正戊基)苯甲酸与碱性氨基酸或氨基胍形成的盐、其制备方法、含有这些盐的药物制剂,及其在制备预防或治疗心脑缺血性疾病、抗血栓、改善心脑循环障碍药物中的应用。本发明的化合物具有优良的水溶性、水溶液稳定性及药代动力学性质,还具有强效的抗血小板聚集、抗血栓、抗脑缺血以及保护神经的活性。
Also published as
Latest bibliographic data on file with the International Bureau