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Alkylpyridyl quinolines as NK3 receptor modulators

A technology of alkyl and pyridine, applied in the field of alkyl pyridyl quinoline derivatives, which can solve problems such as limited evaluation

Inactive Publication Date: 2008-10-08
ASTRAZENECA AB
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] For each of the tachykinin receptors, non-peptide ligands have been developed, however, known non-peptide NK-3 receptor antagonists have many problems such as species selectivity, which limits their use in many suitable disease models. Possibility to evaluate these compounds in

Method used

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  • Alkylpyridyl quinolines as NK3 receptor modulators
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  • Alkylpyridyl quinolines as NK3 receptor modulators

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 37

[0165] Example 37: 2-Phenyl-N-[(1S)-1-phenylpropyl]-3-(pyridin-4-ylmethyl)quinoline-4-formyl Amines (1)

[0166]

[0167] The compound of Example 37 was prepared according to the following scheme:

[0168]

[0169] (a) N-methoxy-N-methyl-3-pyridin-4-yl-propionamide

[0170]

[0171] To a mixture of 3-pyridin-4-ylpropionic acid (3.91 g, 25.8 mmol) and N-hydroxybenzotriazole (3.49 g, 25.8 mmol) in N,N-dimethylformamide (75 mL), Add N,N'-dicyclohexylcarbodiimide (5.33 g, 25.8 mmol). After stirring the mixture for 4 h, N,O-dimethylhydroxylamine hydrochloride (3.78 g, 38.8 mmol) and triethylamine (9 mL, 64.6 mmol) were added, and the resulting slurry was shaken using a wrist shaker. Mix overnight. The mixture was quenched by the addition of water (10 mL) and concentrated under reduced pressure with heating at 70 °C to remove most of the N,N-dimethylformamide. The resulting slurry was partitioned between dichloromethane and water which had been acidified with 1M HCl...

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Abstract

Compounds of Formula I wherein R<1>, A, R<2>, R<3>, R<4>, R<5>, n, m and p are as described in the specification, pharmaceutically-acceptable salts, methods of making, pharmaceutical compositions containing and methods for using the same.

Description

technical field [0001] The present invention relates to alkylpyridylquinoline derivatives, pharmaceutical compositions comprising them and the use of these compounds in the treatment of central nervous system and peripheral diseases or disorders. The invention also relates to the use of these compounds in combination with one or more other CNS drugs to enhance the effect of the other CNS drugs. The compounds of the invention are also useful as probes for localization of cell surface receptors. Background technique [0002] Tachykinin receptors are the targets of a class of structurally related peptides including substance P (SP), neurokinin A (NKA) and neurokinin B (NKB), collectively referred to as "tachykinins". Tachykinins are synthesized in the central nervous system (CNS) as well as in peripheral tissues, and exert various biological activities in the CNS and peripheral tissues. Three tachykinin receptors are known, named neurokinin-1 (NK-1) receptor, neurokinin-2 (NK...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/06A61K31/4709A61P11/00A61P25/00A61P25/18A61P25/22A61P25/24A61P25/28A61P29/00A61P35/00
CPCC07D401/06A61P1/04A61P1/12A61P11/00A61P13/08A61P15/00A61P25/00A61P25/10A61P25/18A61P25/22A61P25/24A61P25/28A61P29/00A61P3/04A61P35/00A61P43/00A61P5/26
Inventor 杰弗里·S·艾伯特克里斯托巴尔·阿尔汉布拉詹姆斯·康杰勒德·M·凯瑟托马斯·R·辛普森詹姆斯·伍兹李艳
Owner ASTRAZENECA AB
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