Nk1 receptor antagonist

A compound and pharmaceutical technology, applied in the field of NK1 receptor antagonists, can solve the problem that NK1 receptor antagonists do not have any description or prompt, and achieve excellent NK1 receptor antagonist activity

Inactive Publication Date: 2018-08-03
KISSEI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] However, in the above-mentioned documents, regarding the NK of the present invention 1 None of the receptor antagonists are described or suggested

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0212] The present invention will be further explained in more detail by the following reference examples, examples and test examples. However, the present invention is not limited thereto.

reference example 1

[0214] {4-[(S)-4-{[(R)-1-(3,5-bistrifluoromethylphenyl)ethyl]methylcarbamoyl}-3-(4-fluoro-2- Methylphenyl)piperazin-1-yl]cyclohexyl}acetate

[0215] (S)-2-(4-fluoro-2-methylphenyl)piperazine-1-carboxylic acid [(R)-1-(3,5-bistrifluoromethylphenyl)ethyl]methyl A solution of amide mesylate (1:1) (0.059g), methyl 4-oxo-cyclohexyl)acetate (0.026g) and triethylamine (0.020g) in tetrahydrofuran (3mL) was stirred at room temperature 10 minutes. To the reaction mixture were added sodium triacetoxyborohydride (0.042 g) and acetic acid (0.012 g) at room temperature, and the mixture was stirred at the same temperature overnight. To the reaction mixture was added saturated aqueous sodium bicarbonate solution, and the resulting mixture was extracted with ethyl acetate. The organic layer was washed with brine and dried over anhydrous magnesium sulfate, and the solvent was removed under reduced pressure. The obtained crude product was purified by silica gel column chromatography (eluent: ...

reference example 2 and 3

[0217] cis-benzyl 4-ethoxycarbonylmethylcyclohexanecarboxylate (reference example 2) and trans-benzyl 4-ethoxycarbonylmethylcyclohexanecarboxylate (reference example 3)

[0218] To a solution of 4-ethoxycarbonylmethylcyclohexanecarboxylic acid (8.96 g) in dichloromethane (50 mL) was added N,N-dimethylformamide (0.010 mL), and the resulting Oxalyl chloride (10.62 g) was added dropwise to the mixture, and the mixture was stirred at the same temperature for 2 hr. The reaction mixture was concentrated under reduced pressure, dichloromethane was added to the residue, and concentrated again. This step was repeated 3 times. To the obtained residue were added dichloromethane (50 mL) and triethylamine (6.35 g), to the resulting mixture was added dropwise benzyl alcohol (5.43 g) under ice-cooling, and the mixture was stirred at room temperature overnight. To the reaction mixture was added saturated aqueous sodium bicarbonate solution, and the resulting mixture was extracted with ethyl...

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Abstract

The present invention addresses the problem of providing a novel compound which has NK1 receptor antagonistic activity and which is useful in the prevention and treatment of nausea and vomiting accompanying the administration of antineoplastic agents. The present invention pertains to a compound represented by formula (I) (in the formula, W represents a fluorine atom or the like, ring A representsa cycloalkyl or the like, X1 represents CH or N, R represents a methyl group or the like, Y represents a number from 0 to 2, and U1, U2, and U3 each independently represent a single bond or the like), or a pharmacologically acceptable salt thereof. This compound or pharmacologically acceptable salt thereof has excellent NK1 receptor antagonistic activity and is useful as a prophylactic or therapeutic agent for nausea and vomiting accompanying the administration of antineoplastic agents.

Description

technical field [0001] The present invention relates to NK which can be used as medicine 1 receptor antagonists. [0002] More specifically, the present invention relates to NK 1 Receptor antagonist or pharmaceutically acceptable salt thereof, it has P substance / neurokinin 1 (NK 1 ) receptor antagonist activity and can be used as a preventive or therapeutic agent for cancer chemotherapy-induced nausea and vomiting (CINV) and the like. Background technique [0003] CINV occurs when the vomiting center located in the lateral medullary reticularis is stimulated. The area postrema and nucleus solitary tract of the medulla contain NK 1 receptors, and NK 1 The receptor is thought to be intimately involved in emesis. [0004] Administration of antineoplastic agents promotes serotonin secretion by enterochromaffin (EC) cells in the digestive tract, and serotonin passes through serotonin in the digestive tract 3 (5-HT 3 ) receptors directly stimulate the vomiting center. Als...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D241/04A61K31/451A61K31/495A61P1/08C07D211/62C07D401/06
CPCA61K31/451A61K31/495A61P1/08C07D211/32C07D211/62C07D241/04C07D401/06
Inventor 宫城贵史小林雅周西村俊洋
Owner KISSEI PHARMA
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