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1. WO2019034031 - TETRAHYDROPROTOBERBERINE COMPOUND, PREPARATION METHOD THEREFOR AND USES THEREOF, AND PHARMACEUTICAL COMPOSITION

Publication Number WO/2019/034031
Publication Date 21.02.2019
International Application No. PCT/CN2018/100340
International Filing Date 14.08.2018
IPC
C07D 455/03 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
455Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberine; Alkylenedioxy derivatives of dibenzo quinolizines, e.g. berberine
03containing quinolizine ring systems directly condensed with at least one six-membered carbocyclic ring, e.g. protoberberine; Alkylenedioxy derivatives of dibenzo quinolizines, e.g. berberine
A61K 31/4375 2006.1
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
435having six-membered rings with one nitrogen as the only ring hetero atom
4353ortho- or peri-condensed with heterocyclic ring systems
4375the heterocyclic ring system containing a six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
A61P 25/06 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
06Antimigraine agents
A61P 25/16 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
14for treating abnormal movements, e.g. chorea, dyskinesia
16Anti-Parkinson drugs
A61P 25/18 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
A61P 25/30 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
30for treating abuse or dependence
CPC
A61P 25/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
A61P 25/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
06Antimigraine agents
A61P 25/14
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
14for treating abnormal movements, e.g. chorea, dyskinesia
A61P 25/16
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
14for treating abnormal movements, e.g. chorea, dyskinesia
16Anti-Parkinson drugs
A61P 25/18
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
A61P 25/20
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
20Hypnotics; Sedatives
Applicants
  • 中国科学院上海药物研究所 SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES [CN]/[CN]
  • 上海特化医药科技有限公司 TOPHARMAN SHANGHAI CO., LTD. [CN]/[CN]
Inventors
  • 何洋 HE, Yang
  • 蒋翔锐 JIANG, Xiangrui
  • 李剑峰 LI, Jianfeng
  • 王瑜 WANG, Yu
  • 王震 WANG, Zhen
  • 陈伟铭 CHEN, Weiming
  • 朱富强 ZHU, Fuqiang
  • 吴春晖 WU, Chunhui
  • 张容霞 ZHANG, Rongxia
  • 沈敬山 SHEN, Jingshan
  • 蒋华良 JIANG, Hualiang
Agents
  • 北京金信知识产权代理有限公司 KINGSOUND & PARTNERS
Priority Data
201710693250.114.08.2017CN
Publication Language Chinese (zh)
Filing Language Chinese (ZH)
Designated States
Title
(EN) TETRAHYDROPROTOBERBERINE COMPOUND, PREPARATION METHOD THEREFOR AND USES THEREOF, AND PHARMACEUTICAL COMPOSITION
(FR) COMPOSÉ DE TÉTRAHYDROPROTOBERBÉRINE, SON PROCÉDÉ DE PRÉPARATION, SES UTILISATIONS ET COMPOSITION PHARMACEUTIQUE
(ZH) 一类四氢原小檗碱类化合物,其制备方法、用途及药物组合物
Abstract
(EN) The present invention provides a tetrahydroprotoberberine compound represented by general formula (I), an enantiomer, a diastereoisomer and a raceme thereof and a mixture thereof, a pharmaceutically acceptable organic or inorganic salt thereof, and a crystalline hydrate and a solvate thereof. The present invention also provides a method for preparing the compound, and applications thereof in the preparation of drugs for preventing and/or treating central nervous system diseases.
(FR) La présente invention concerne un composé de tétrahydroprotoberbérine représenté par la formule générale (I), et un énantiomère, un diastéréoisomère, un racémique de celui-ci et un mélange de ceux-ci; l'invention concerne également un sel organique ou inorganique pharmaceutiquement acceptable de celui-ci, et un hydrate cristallin ainsi qu'un solvate de celui-ci. La présente invention concerne en outre un procédé de préparation du composé, et ses applications dans la préparation de médicaments destinés à la prévention et/ou le traitement de maladies du système nerveux central.
(ZH) 本发明提供了一种由通式(I)表示的四氢原小檗碱类化合物、其对映异构体、非对映异构体、外消旋体及其混合物,以及其药学上可接受的无机或有机盐、结晶水合物及溶剂合物。本发明还提供了所述化合物的制备方法以及其在制备预防和/或治疗中枢神经系统疾病的药物中的应用。
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