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N-piperidino-1-(2,4-dichlorophenyl)-4-methyl-5-(4-chlorophenyl)pyrazole-3-formamide organic salts and their pharmaceutical compositions

A technology of dichlorophenyl and organic acid salts, applied to N-piperidinyl-1-(2, can solve the problems of large human body irritation, and achieve the effect of no side effects

Inactive Publication Date: 2005-11-23
江西圣佳格医药技术研究有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Among the salts mentioned above, most of the acids are inorganic acids or strong organic acids that cannot be directly eaten, which are highly irritating to the human body and have certain defects.

Method used

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  • N-piperidino-1-(2,4-dichlorophenyl)-4-methyl-5-(4-chlorophenyl)pyrazole-3-formamide organic salts and their pharmaceutical compositions
  • N-piperidino-1-(2,4-dichlorophenyl)-4-methyl-5-(4-chlorophenyl)pyrazole-3-formamide organic salts and their pharmaceutical compositions
  • N-piperidino-1-(2,4-dichlorophenyl)-4-methyl-5-(4-chlorophenyl)pyrazole-3-formamide organic salts and their pharmaceutical compositions

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] Example 1: N-piperidine-1-(2,4-dichlorophenyl)-4-methyl-5-(4-chlorophenyl)pyrazole-3-carboxamide nicotinate

[0045] Dissolve 4.64g (0.01mol) of N-piperidine-1-(2,4-dichlorophenyl)-4-methyl-5-(4-chlorophenyl)pyrazole-3-carboxamide in acetone 46.4 ml, stir, add a solution of niacin 1.23g (0.01mol) and acetone 6.15ml, stir at room temperature for 24 hours, cool in the refrigerator, and fully crystallize. Suction filtration, the solid was filtered out, and the solid was washed with a small amount of cold acetone and dried in vacuo to constant weight to obtain N-piperidine-1-(2,4-dichlorophenyl)-4-methyl-5-(4-chlorophenyl) Phenyl)pyrazole-3-carboxamide nicotinate.

[0046] C

Embodiment 2

[0047] Example 2: N-piperidine-1-(2,4-dichlorophenyl)-4-methyl-5-(4-chlorophenyl)pyrazole-3-carboxamide lactate

[0048]Dissolve 4.64g (0.01mol) of N-piperidine-1-(2,4-dichlorophenyl)-4-methyl-5-(4-chlorophenyl)pyrazole-3-carboxamide in acetone 46.4 ml, stir, add 0.90 g (0.01 mol) of lactic acid, stir at room temperature for 24 hours, cool in the refrigerator, and fully crystallize. Suction filtration, the solid was filtered out, and the solid was washed with a small amount of cold acetone and dried in vacuo to constant weight to obtain N-piperidine-1-(2,4-dichlorophenyl)-4-methyl-5-(4-chlorophenyl) Phenyl)pyrazole-3-carboxamide lactate.

[0049] C

Embodiment 3

[0050] Example 3: N-piperidine-1-(2,4-dichlorophenyl)-4-methyl-5-(4-chlorophenyl)pyrazole-3-carboxamide pyrrolidonate

[0051] Dissolve 4.64g (0.01mol) of N-piperidine-1-(2,4-dichlorophenyl)-4-methyl-5-(4-chlorophenyl)pyrazole-3-carboxamide in acetone 46.4 ml, stir, add 1.29g (0.01mol) of pyrrolidone acid / 6.45ml of acetone, stir at room temperature for 24 hours, cool in the refrigerator, and fully crystallize. Suction filtration, the solid was filtered out, and the solid was washed with a small amount of cold acetone and dried in vacuo to constant weight to obtain N-piperidine-1-(2,4-dichlorophenyl)-4-methyl-5-(4-chlorophenyl) Phenyl)pyrazole-3-carboxamide pyrrolidonate.

[0052] C

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Abstract

The invention relates to a N-piperidino-1-(2,4-dichlorophenyl)-4-methyl-5-(4-chlorophenyl)pyrazole-3-formamide organic salts and their pharmaceutical compositions, wherein the organic acids coordinated by the organic acid salts are all edible or in existence in human body, thus no side effects are resulted to the human body, and higher level of safety can be achieved.

Description

technical field [0001] The present invention relates to a kind of N-piperidinyl-1-(2,4-dichlorophenyl)-4-methyl-5-(4-chlorophenyl)pyrazole-3-carboxamide organic acid salt and its pharmaceutical composition. Background technique [0002] Structural Formula I [0003] The compound of structural formula I, the international general name rimonabant is the first cannabinoid (CB1) receptor blocker (EP656354), which blocks the core of the central appetite regulation system by blocking endogenous cannabinoid-like substances. It can not only quantitatively regulate the consumption of calories, but also reduce the appetite for fatty food and sugar-added food. It is a weight-loss drug that is safer than previous weight-loss drugs. The compound of structural formula I has a good improvement effect on controlling cholesterol and other heart disease risk factors while losing weight. [0004] Research also shows (CN01804713.0) that the smoking cessation effect of the compound of struc...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D231/14
Inventor 金鑫
Owner 江西圣佳格医药技术研究有限公司
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