Derivative of pyridine and (4,3-d) pyrimidine-1(2H)-base phenyl acetamide and application thereof

A technology of phenylacetamide and derivatives, applied in the field of derivatives of compounds, can solve problems such as poor metabolism, small toxic and side effects, and achieve the effects of less side effects, small dosage, and elimination of bad metabolism problems.

Inactive Publication Date: 2014-05-28
ZHENJIANG SAN AN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The purpose of the present invention is to overcome the defects in the prior art, and to provide derivatives of pyrido(4,3-d)pyrimidin-1(2H)-ylphenylacetamide and applications thereof, the derivatives have good pharmaceutical activity , At the same time, it can solve the problem of poor metabolism of drugs, and the toxic and side effects in the course of medication are small

Method used

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  • Derivative of pyridine and (4,3-d) pyrimidine-1(2H)-base phenyl acetamide and application thereof
  • Derivative of pyridine and (4,3-d) pyrimidine-1(2H)-base phenyl acetamide and application thereof
  • Derivative of pyridine and (4,3-d) pyrimidine-1(2H)-base phenyl acetamide and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Preparation of N-[3-[3-cyclopropyl-5-[(2-fluoro-4-iodophenyl)amino]-3,4,6,7-tetrahydro-6,8-dimethyl-2 ,4,7-Trioxo-pyrido[4,3-d]pyrimidin-1(2H)-yl}phenyl)acetamide-1,1,1-d3.

[0022] The synthesis of derivatives described in the present invention comprises reduction and acetylation 2 steps:

[0023] The preparation steps are as follows:

[0024] (1) Reduction steps

[0025] Preparation of [3-cyclopropyl-5-[(2-fluoro-4-iodophenyl)amino]-6,8-dimethyl-1-(3-aminophenyl)-pyrido[4,3- d] pyrimidine-2,4,7(1H,3H,6H)-trione 1-2, the reaction equation is as follows:

[0026]

[0027] Under anhydrous, oxygen-free and argon protection, 3.78 grams of [3-cyclopropyl-5-[(2-fluoro-4-iodophenyl)amino]-6,8- Dimethyl-1-(3-nitrophenyl)-pyrido[4,3-d]pyrimidine-2,4,7(1H,3H,6H)-trione 1-1 and 40 ml of dichloromethane . 3.27 grams of sodium bisulfite and 2 milliliters of water were added under stirring at room temperature, and the reaction was stirred for 3-5 hours at a reaction tempera...

Embodiment 2

[0033] Preparation of N-[3-[3-cyclopropyl-5-[(2-fluoro-4-iodophenyl)amino]-3,4,6,7-tetrahydro-6,8-dimethyl-2 , 4,7-trioxo-pyrido[4,3-d]pyrimidin-1(2H)-yl}phenyl)acetamide-1-d1.

[0034]

[0035] The preparation method is the same as in Example 1, and the acetic acid-d3 anhydride in the embodiment 1 is replaced by acetic acid-d2 anhydride.

Embodiment 3

[0037] Preparation of N-[3-[3-cyclopropyl-5-[(2-fluoro-4-iodophenyl)amino]-3,4,6,7-tetrahydro-6,8-dimethyl-2 ,4,7-Trioxo-pyrido[4,3-d]pyrimidin-1(2H)-yl}phenyl)acetamide-1,1-d2.

[0038]

[0039] The preparation method is the same as in Example 1, and the acetic acid-d3 anhydride in the embodiment 1 is replaced by acetic acid-d1 anhydride.

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PUM

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Abstract

The invention discloses a derivative of pyridine and (4,3-d) pyrimidine-1(2H)-base phenyl acetamide and an application thereof. The derivative has good pharmaceutical activity, can greatly prolong the half-life periods of drugs, prolongs the retention time of drugs in the human body, and meanwhile increases the drug concentration in the blood. Therefore, a better curative effect is achieved. As the half-life periods of drugs are greatly prolonged, the drugs can keep activity concentration for a longer time in the blood. Under the cure condition with dose limiting, the curative effect can be kept and the recommended dosage of drugs can be reduced at the same time, therefore the bad metabolism of drugs is eliminated, the drug toxicity is reduced, and the toxic and side effects in the drug using process are small.

Description

technical field [0001] The invention relates to a compound derivative and its application, belonging to the technical field of medicine. Background technique [0002] Melanoma is a malignant tumor with a high degree of malignancy, also known as malignant melanoma. Most of them originate in the skin, and can also originate in the eyes, nasal cavity, etc., and can metastasize in the early stage. The most common metastatic sites are the lung and brain. Melanoma is the leading cause of death among skin diseases. The National Cancer Institute estimates that as many as 76,690 Americans will be diagnosed with melanoma in 2013 and 9,480 will die from the disease. On May 29, 2013, the US Food and Drug Administration (FDA) approved a new drug for the treatment of patients with metastatic melanoma and inoperable melanoma, and the use of this new drug can also be used to diagnose the patient suitability for treatment. The chemical name of this new drug is: N-[3-[3-cyclopropyl-5-[(2-f...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D471/04A61P35/04A61P35/00
CPCC07D471/04
Inventor 陈兴海
Owner ZHENJIANG SAN AN PHARMA
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