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Pyridine condensed ring compound and its preparation method and use

Technology of a compound, pyridine, applied in the field of medicine

Active Publication Date: 2018-02-09
INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Although the existing drugs alone or in combination can effectively inhibit the replication of the virus in the body, the common problem is drug resistance

Method used

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  • Pyridine condensed ring compound and its preparation method and use
  • Pyridine condensed ring compound and its preparation method and use
  • Pyridine condensed ring compound and its preparation method and use

Examples

Experimental program
Comparison scheme
Effect test

preparation Embodiment 1

[0191] Preparation Example 1 2-(4-cyanoanilino)-3-nitro-4-amino-6-chloro-pyridine (IV-1)

[0192]

[0193] 2,6-dichloro-3-nitro-4-aminopyridine (II-1, 416mg, 2.0mmol) and p-cyanoaniline (III-1, 472mg, 4.0mmol), solvent-free reaction, react overnight at 100°C, add Dissolve DMF, introduce into water with pH=3.0, stir for 10 minutes, filter with suction, filter the solid, stir in aqueous sodium bicarbonate solution for 15 minutes, filter with suction, wash with water, dry, separate and purify with medium pressure column (dichloromethane, ethyl acetate is eluent) to obtain 491.3 mg of a yellow solid with a yield of 85%.

preparation Embodiment 2

[0194] Preparation Example 2 2-(4-cyanoanilino)-3-nitro-4-amino-5-bromo-6-chloro-pyridine (IV-2)

[0195]

[0196] Using 4-amino-3-nitro-2,6-dichloro-5-bromopyridine as raw material, the preparation method is the same as IV-1, and the yield is 90%.

preparation Embodiment 3

[0197] Preparation Example 3 2-(4-cyanoanilino)-3-nitro-4-amino-5,6-dichloropyridine (IV-3)

[0198]

[0199] Using 4-amino-3-nitro-2,5,6-trichloropyridine as raw material, the preparation method is the same as IV-1, and the yield is 92.75%.

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Abstract

The invention relates to a pyridine condensed nucleus compound and a preparing method and application thereof, in particular to a compound as shown in formula I in the description or pharmaceutical salt thereof, a pharmaceutical composition thereof, and the application thereof to preparation of drugs for preventing and / or treating diseases relevant to HIV infection. The compound is novel in structure, has high anti-HIV activity, can effectively resist the drug resistance of HIV virus strain, and is a non-nucleoside HIV reverse transcriptase inhibitor with great application potential.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a pyridine condensed ring compound and a preparation method and application thereof. As a non-nucleoside HIV reverse transcriptase inhibitor, the compound can be used for preventing or treating diseases related to HIV infection. Background technique [0002] AIDS virus (ie human immunodeficiency virus, Human Immunodeficiency Virus, HIV) is a kind of RNA virus, and the surface of this virus is a layer of double lipid membrane. Two single-stranded RNAs and some important enzymes (such as reverse transcriptase, proteolytic enzyme, integrase) and structural proteins (p24, p17, p7, etc.) are wrapped in the membrane. There are two important glycoproteins GP120 and GP41 on the membrane surface of the virus. GP120 is on the outside of the membrane, and GP41 straddles the double lipid membrane and forms a complex with GP120. Their main function is to recognize and attack cells with CD4 surface r...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D471/04A61K31/437A61K31/4375A61K31/4985A61K31/496A61P31/18
CPCC07D471/04
Inventor 秦炳杰谢蓝陈清和姜世勃
Owner INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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