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A novel anti-HIV drug and its preparation method and application

A pharmacy and compound technology, applied in the field of new anti-HIV drugs and their preparation and use, can solve problems such as cross-drug resistance

Active Publication Date: 2022-04-19
HC SYNTHETIC PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Reverse transcriptase inhibitors and protease inhibitors are clinically used as anti-HIV drugs, however, drugs with the same mechanism of action often show cross-resistance or have only additional activity

Method used

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  • A novel anti-HIV drug and its preparation method and application
  • A novel anti-HIV drug and its preparation method and application
  • A novel anti-HIV drug and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Embodiment 1: the preparation of compound 1

[0033] The reaction equation is as follows:

[0034]

[0035] Under a carbon monoxide atmosphere, a mixture of 33.5 g of compound 1-1, 34.8 ml of diisopropylethylamine, 14.3 mL of compound 2-1 and 4.62 g of tetrakis (triphenylphosphine) palladium dimethyl sulfoxide Stir at 90°C for 5.5 hours. After cooling, the precipitate was filtered and washed with 50 ml of water. Then wash with 500ml of isopropanol, dissolve the solid with ethyl acetate, and wash the organic layer with 335ml of water. The aqueous layer was separated, and 300ml of 0.5N hydrochloric acid was added to the aqueous layer. The aqueous layer was extracted with 300 ml of ethyl acetate. The organic layers were combined and concentrated. To the residue was added 150 ml of isopropanol, cooled to 20°C and filtered, the resulting solid was dissolved in ethanol (100 mL) and treated with 1N sodium hydroxide (aq). The resulting suspension was stirred at room te...

Embodiment 2

[0036] Embodiment 2: the preparation of compound 2

[0037] The reaction equation is as follows:

[0038]

[0039] The preparation method is the same as in Example 1.

Embodiment 3

[0040] Embodiment 3: the preparation of compound 3

[0041] The reaction equation is as follows:

[0042]

[0043] The preparation method is the same as in Example 1.

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PUM

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Abstract

The present invention relates to a novel anti-HIV drug and its clinical application. The novel anti-HIV drug of the present invention has the structure shown in the following formula (I). The present invention also includes the compound represented by formula (I) or hydrate, solvate, co-crystal, pharmaceutically acceptable salt, and its preparation method. The pharmaceutical composition of the compound is used in medicine, especially for the treatment of acquired immunodeficiency syndrome. (I).

Description

technical field [0001] The present invention relates to a novel anti-HIV drug and its non-toxic pharmaceutically acceptable salt, preparation method, pharmaceutical composition containing them and clinical application, especially for the treatment of acquired immunodeficiency syndrome. Background technique [0002] Among viruses, human immunodeficiency virus (HIV), a retrovirus, is known to cause acquired immunodeficiency syndrome (AIDS). Therapeutic agents for AIDS are mainly selected from a group of reverse transcriptase inhibitors (eg, AZT, 3TC) and protease inhibitors (eg, indinavir), but they have been shown to be associated with side effects such as kidney disease and emergence of drug-resistant viruses . Therefore, the development of anti-HIV drugs having other mechanisms of action is desired. [0003] On the other hand, it has been reported that combination therapy can effectively treat AIDS due to the frequent emergence of drug-resistant mutants. Reverse transcri...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D498/14C07F9/6561A61K31/5365A61K31/675A61P31/18
CPCC07D498/14C07F9/6561
Inventor 张起愿刘晓鹏戚苏民
Owner HC SYNTHETIC PHARMA CO LTD
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