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Aporphine compound, medicinal composition thereof and application thereof

An apophine and compound technology, applied in the field of apophine compounds, can solve the problems of involuntary movements, monotonous stereotypes, etc.

Inactive Publication Date: 2010-01-06
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Moreover, after chronic medication, many PD patients (40% to 60%) have adverse reactions such as severe involuntary movement or dyskinesia. The patient shows involuntary movement, which can involve the head, face, limbs and trunk, and sometimes appears monotonous and stereotyped. and involuntary movements or dystonia necessitating discontinuation of treatment

Method used

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  • Aporphine compound, medicinal composition thereof and application thereof
  • Aporphine compound, medicinal composition thereof and application thereof
  • Aporphine compound, medicinal composition thereof and application thereof

Examples

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Embodiment Construction

[0038] The present invention will be further described below in conjunction with specific examples, but the present invention is not limited.

[0039] Preparation Example

[0040] 1 H-NMR is measured with a Varian Mercury AMX300 type instrument; MS is measured with a VG ZAB-HS or VG-7070 type instrument, and all are EI sources (70ev) unless otherwise noted; The water solvents were all obtained by drying according to standard methods; except for the instructions, all reactions were carried out under nitrogen protection and followed by TLC, and the post-treatment was washed with saturated sodium chloride aqueous solution and dried with anhydrous sodium sulfate; the purification of the product Unless otherwise specified, silica gel (200-300 mesh) column chromatography was used; among them, silica gel (200-300 mesh) was produced by Qingdao Ocean Chemical Factory, and GF254 thin-layer silica gel plate was produced by Yantai Jiangyou Silica Gel Development Co., Ltd.

[0041] Prepa...

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Abstract

The invention relates to an aporphine compound represented by general formula (I) or stereoisomer thereof, pharmaceutically acceptable salt or pharmaceutically acceptable solvate and medical application thereof. The compound can be used for preventing or treating diseases related with serotonin 1A receptors, wherein the diseases comprise central nervous system diseases, in particular schizophrenia, depression and movement disorder caused by Parkinson's resistant medicament. The invention also relates to a medicinal composition comprising the compound.

Description

technical field [0001] The present invention relates to apomorphine compounds which have activity on serotonin 1A receptors and are therefore useful in various therapeutic fields, especially in the treatment of diseases of the central nervous system, such as schizophrenia, depression and anti-parkinsonism Dyskinesia drug-induced movement disorders, etc. The present invention also relates to pharmaceutical compositions comprising the compounds described above. Background technique [0002] 1. Five serotonin 1A receptors [0003] Five serotonin (5-HT) is an important central neurotransmitter. The synthesis, storage, membrane uptake and metabolism of 5-HT together with the 5-HT receptor constitute the 5-HT nervous system. Currently, at least seven types of 5-HT receptors have been cloned, namely 5-HT 1 ~5-HT 7 . Some have several subtypes. Drugs acting on the 5-HT system are used to treat various mental diseases such as schizophrenia and depression, obesity, and sexual d...

Claims

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Application Information

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IPC IPC(8): C07D221/18C07D409/12A61K31/473A61P25/18A61P25/24A61P25/16
Inventor 张翱镇学初刘志礼陈学涛余蕾平
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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