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Pharmaceutical uses of 4,5-disubstituted-2-pyrrolidone compounds

A technology of pyrrolidone and compound, applied in the field of drug application, can solve the problems of forgetfulness, bone marrow suppression, toxic and side effects, etc.

Inactive Publication Date: 2016-01-27
THE KEY LAB OF CHEM FOR NATURAL PROD OF GUIZHOU PROVINCE & CHINESE ACADEMY OF SCI +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The clinical application of these drugs prolongs the lives of AIDS patients, but it is also accompanied by serious side effects, such as bone marrow suppression, amnesia and the occurrence of drug resistance

Method used

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  • Pharmaceutical uses of 4,5-disubstituted-2-pyrrolidone compounds
  • Pharmaceutical uses of 4,5-disubstituted-2-pyrrolidone compounds
  • Pharmaceutical uses of 4,5-disubstituted-2-pyrrolidone compounds

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Example 1: Preparation of 4,5-disubstituted-2-pyrrolidone compound (i.e. general formula I):

[0040] Wherein the preparation of trans 4-phenyl-5-o-chlorobenzyl-2-pyrrolidone is according to invention patent ZL97123419.1 (synthetic process of d1-trans-4-phenyl-5-o-chlorobenzylpyrrolidone-2) The disclosed method, the synthetic route is as follows:

[0041]

[0042] (1) Synthesis of 2-o-chlorophenylnitroethylene (intermediate Ⅳ)

[0043] Method A: 8g of o-chlorobenzaldehyde (0.057mol) and nitromethane (5.2g, 0.086mol) are mixed in 25ml of methanol, 10% KOH aqueous solution is added dropwise under stirring at 0-5°C to adjust the pH of the reaction solution to 8-9, continue to react for 2 hours (check the reaction process by TLC), add dropwise 10% KOH aqueous solution to adjust the pH to greater than 10, and react for 30 minutes, quickly pour the reaction solution into ice water with concentrated hydrochloric acid, stir for 30 minutes, add A certain amount of saturated...

Embodiment 2

[0052] Example 2: Take (dl)-trans-4-phenyl-5-o-chlorobenzyl-2-pyrrolidone, grind it through an 80-mesh sieve, add appropriate amount of starch, dextrin, and lactose and mix evenly , granulated, dried, granulated, and divided into capsule shells to obtain capsules. The preparation is orally administered twice a day, and the dose of each dose is 5-100 mg based on the raw material drug.

Embodiment 3

[0053] Example 3: Take 4-phenyl-5-benzyl-2-pyrrolidone, crush it and pass through an 80-mesh sieve, add appropriate amount of starch, dextrin, and lactose, mix evenly by equal multiplication method, granulate, dry, and granulate. The granules are compressed into tablets. The preparation is orally administered twice a day, and the dose of each dose is 5-100 mg based on the raw material drug.

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Abstract

The invention discloses application of a 4, 5-disubstituted-2-pyrrolidone compound in preparation of anti-AIDS drugs and preparation of reverse transcriptase inhibitor drugs. Test on the anti-HIV-1 activity of the compound provided by the invention by an international general experimental method finds that the compound has good anti-HIV-1 activity, small toxic and side effect, and has good new drug development prospects.

Description

technical field [0001] The invention relates to the medicinal application of 4,5-disubstituted-2-pyrrolidone compound, in particular the application as a reverse transcriptase inhibitor in the preparation of anti-AIDS drugs, and belongs to the technical field of pharmaceutical application. Background technique [0002] AIDS (Acquiredimmuno-deficiency Syndrome, AIDS) is an acquired immune deficiency syndrome, and it is one of the incurable diseases that threaten human health in the world today. The pathogen that causes AIDS is Human Immunodeficiency Virus (HIV). HIV has two subtypes, HIV-1 and HIV-2, and several mutant strains. The development of anti-AIDS drugs mainly focuses on HIV reverse transcriptase (RT) inhibitors, protein synthetase inhibitors, reverse transcription promoter inhibitors, etc., and reverse transcriptase inhibitors (such as AZT, DDC, DDI, D4T, etc.) and protease inhibitory drugs (such as Ritonavir, Indinavir, Nelfinavir, Sequanavir, etc.). The clinical...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/4015A61P31/18
Inventor 杨小生郑永唐郝小江汪冶
Owner THE KEY LAB OF CHEM FOR NATURAL PROD OF GUIZHOU PROVINCE & CHINESE ACADEMY OF SCI
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