1H-quinolin-4-one compounds, with affinity for the GABA receptor, processes, uses and compositions

A compound, quinoline technology, applied in the direction of drug combination, active ingredient of heterocyclic compounds, organic chemistry, etc., can solve problems such as the central nervous system of undisclosed related compounds

Inactive Publication Date: 2009-09-02
FERRER INT SA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

No related compounds belonging to this chemical class have been disclosed as having GABA A Receptor ligand activity and any other central nervous system activity

Method used

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  • 1H-quinolin-4-one compounds, with affinity for the GABA receptor, processes, uses and compositions
  • 1H-quinolin-4-one compounds, with affinity for the GABA receptor, processes, uses and compositions
  • 1H-quinolin-4-one compounds, with affinity for the GABA receptor, processes, uses and compositions

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0273] Compounds 1-146, Table 4 were prepared according to the above-mentioned Preparation Examples.

[0274] Table 4

[0275]

[0276]

[0277]

[0278]

[0279]

[0280]

[0281]

[0282]

[0283]

Embodiment 1

[0284] Composition example 1: 5 mg tablet

[0285]

Embodiment 2

[0286] Composition Example 2: 10 mg Capsules

[0287]

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PUM

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Abstract

The invention provides new 1H-quinolin-4-one compounds of formula (I), wherein R1, R2, R3, R4 and R 5 have different meanings, and pharmaceutically acceptable salts and hydrates thereof. Compounds of formula (I) are useful for treating or preventing diseases associated with GABAA receptors modulation, anxiety, epilepsy, sleep disorders including insomnia, and for inducing sedation-hypnosis, anesthesia, sleep and muscle relaxation. The invention also provides synthetic procedures for preparing said compounds.

Description

technical field [0001] The present invention relates to having GABA A A new class of agents for receptor affinity. In particular, the present invention relates to novel 1H-quinolin-4-one compounds useful for the treatment or prevention of anxiety, epilepsy and sleep disorders including insomnia, and for inducing sedation-hypnosis, anesthesia, sleep and muscle relaxation. Background technique [0002] GABA A receptor (gamma-aminobutyric acid A ) are pentameric proteins that form membrane ion channels. GABA A The receptors have been implicated in the regulation of sedation, anxiety, muscle tone, epileptogenic activity and memory function. These effects should be attributed to the identified GABA A Subunits of receptors, especially alpha 1 -subunit and alpha 2 - Subunits. [0003] Sedative effect via alpha 1 - Subunits are regulated. Zolpidem is characterized by the presence of alpha 1 - The receptors have high affinity and their sedative and hypnotic effects are m...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D215/06C07D215/18C07D401/06C07D401/14C07D409/06C07D413/06C07D405/06C07D417/06A61K31/47A61P25/20A61P25/22
CPCC07D401/14C07D405/06C07D417/06C07D215/18C07D401/06C07D215/06C07D409/06C07D413/06A61P21/02A61P25/00A61P25/08A61P25/20A61P25/22
Inventor J·L·法尔科A·帕洛莫A·古格列塔
Owner FERRER INT SA
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