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Applications of pyrimidine compounds in preparation of medicines for promoting small intestine peristalsis

A technology of small intestinal peristalsis and pyrimidine, which is applied in the field of medicine and achieves the effect of good development and application prospects

Inactive Publication Date: 2018-03-02
南京多宝生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The pyrimidine compound 2-anilino-4-pyrrolidinyl-6-(5-(4-methyl-1-piperazinyl)-2-pyridyl)aminopyrido[3,4-d ] pyrimidine, CN107245075A discloses 2-anilino-4-pyrrolidinyl-6-(5-(4-methyl-1-piperazinyl)-2-pyridyl) aminopyrido[3,4-d] The preparation method of pyrimidine, there is no 2-anilino-4-pyrrolidinyl-6-(5-(4-methyl-1-piperazinyl)-2-pyridyl)aminopyrido[3,4- d] Related reports on pyrimidine promoting intestinal peristalsis

Method used

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  • Applications of pyrimidine compounds in preparation of medicines for promoting small intestine peristalsis
  • Applications of pyrimidine compounds in preparation of medicines for promoting small intestine peristalsis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] Embodiment 1: The compound 2-anilino-4-pyrrolidinyl-6-(5-(4-methyl-1-piperazinyl)-2-pyridyl)aminopyrido[3,4 -d] Preparation of pyrimidine tablets:

[0016] Prepare 2-phenylamino-4-pyrrolidinyl-6-(5-(4-methyl-1-piperazinyl)-2-pyridyl)aminopyrido[3,4 according to the method disclosed in Example 1 of CN107245075A -d] pyrimidine, take 20 grams of compound 2-anilino-4-pyrrolidinyl-6-(5-(4-methyl-1-piperazinyl)-2-pyridyl)aminopyrido[3,4 -d] pyrimidine, add 180 grams of conventional adjuvants for preparing tablets, mix evenly, and make 1000 tablets with a conventional tablet press.

Embodiment 2

[0017] Example 2: The compound 2-anilino-4-pyrrolidinyl-6-(5-(4-methyl-1-piperazinyl)-2-pyridyl)aminopyrido[3,4 -d] the preparation of pyrimidine capsules:

[0018] Prepare 2-phenylamino-4-pyrrolidinyl-6-(5-(4-methyl-1-piperazinyl)-2-pyridyl)aminopyrido[3,4 according to the method disclosed in Example 1 of CN107245075A -d] pyrimidine, take 20 grams of compound 2-anilino-4-pyrrolidinyl-6-(5-(4-methyl-1-piperazinyl)-2-pyridyl)aminopyrido[3,4 -d] pyrimidine, add conventional auxiliary materials for preparing capsules such as 180 grams of starch, mix well, and make 1000 capsules.

[0019] The following pharmacodynamic experiments will further illustrate its drug activity.

experiment example

[0020] Experimental example: Evaluation of the compound 2-anilino-4-pyrrolidinyl-6-(5-(4-methyl-1-piperazinyl)-2-pyridyl)aminopyrido[3,4 -d] Effect of pyrimidine on propulsive motility of the small intestine

[0021] 1. Method: Get 30 Kunming mice, 20 ± 5g, half male and half male, and divide them into 3 groups randomly according to sex and body weight, i.e. blank group, 2-phenylamino-4-pyrrolidinyl-6-(5-( 4-Methyl-1-piperazinyl)-2-pyridyl)aminopyrido[3,4-d]pyrimidine (0.06mg / 10g, 0.24mg / 10g) two dose groups. 10 per group, 2-anilino-4-pyrrolidinyl-6-(5-(4-methyl-1-piperazinyl)-2-pyridyl)aminopyrido[3,4-d]pyrimidine Suspension was made with 5% charcoal powder and 10% gum arabic, and the blank group was directly suspended with charcoal powder and gum arabic without adding drugs, and both were prepared with normal saline. The mice were fasted for 24 hours before the experiment. Mice were intragastrically administered 0.2ml / 10g and killed 30 minutes after administration. Take ...

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Abstract

The invention relates to applications of 2-phenylamino-4-pyrrolidyl-6-(5-(4-methyl-1-piperazinyl)-2-pyridyl)aminopyridino-[3,4-d]pyrimidine in preparation of medicines for promoting small intestine peristalsis. The pharmacological experiment shows that 2-phenylamino-4-pyrrolidyl-6-(5-(4-methyl-1-piperazinyl)-2-pyridyl)aminopyridino-[3,4-d]pyrimidine has a relatively good effect of promoting smallintestine peristalsis, has the outstanding substantive characteristics, and obviously has remarkable progress in preparation of the medicines for promoting small intestine peristalsis.

Description

technical field [0001] The invention belongs to the field of medicine, in particular to a new pharmaceutical application of pyrimidine compounds, especially 2-anilino-4-pyrrolidinyl-6-(5-(4-methyl-1-piperazinyl)-2 Application of -pyridyl)aminopyrido[3,4-d]pyrimidine in the preparation of drugs for promoting small intestinal peristalsis. Background technique [0002] Intestinal peristalsis refers to the movement of peristalsis similar to worms, especially the wave-like contraction of the intestines. Rough food with more fiber but low nutrition can stimulate intestinal peristalsis. Fibrous food A coarse, indigestible plant substance composed mainly of polysaccharides (such as cellulose), which stimulates bowel movements when eaten. Slow movement can cause constipation. [0003] The pyrimidine compound 2-anilino-4-pyrrolidinyl-6-(5-(4-methyl-1-piperazinyl)-2-pyridyl)aminopyrido[3,4-d ] pyrimidine, CN107245075A discloses 2-anilino-4-pyrrolidinyl-6-(5-(4-methyl-1-piperazinyl)-...

Claims

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Application Information

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IPC IPC(8): A61K31/519A61P1/14A61P1/00
CPCA61K31/519
Inventor 徐艳
Owner 南京多宝生物科技有限公司
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