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Intergrase inhibitor

A compound, alkyl technology, applied in the field of inhibitors that inhibit HIV replication, HIV treatment, and integrase allosteric inhibitors, which can solve the problems of crystal form stability, solubility lipophilicity, CYP inhibition liver microsome stability and plasma stability sexual insufficiency

Inactive Publication Date: 2013-08-21
世方科技(杭州)有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

More specifically, these problems with existing drugs may include deficiencies in crystal form stability, solubility, lipophilicity, CYP inhibition, hepatic microsomal stability, and plasma stability

Method used

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Examples

Experimental program
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Effect test

Embodiment 1

[0186] Example 1 discloses a method for synthesizing a compound of formula (I).

[0187]

[0188]Condensation of methyl-2-aminobenzoate derivative (1a) with ethyl-3-ethoxy-2-enoate affords the imine, which then undergoes cyclization to yield quinoline 1b. A variety of reaction conditions can be employed to affect this condensation cyclization reaction. After that with SOCl 2 or POCl 3 Workup was performed to convert the phenol in 1b to the chloride. The chlorine in 1c is then replaced by an addition elimination reaction with the appropriate amine (benzylamine in Scheme 1) with heating in a suitable solvent.

[0189] The ester group in 1d is then reduced to the alcohol group using a suitable reducing agent such as, but not limited to, DIBAL. Reduction of the ester in 1d can also be carried out using other reducing conditions. Then use a method suitable for the oxidation of ethanol to acetaldehyde, such as DMSO oxidation conditions (such as SO 3 -pyridine), or with Mn...

Embodiment 2

[0192] Another synthetic method of 2C4 amine-substituted quinoline.

[0193]

[0194] Another method for the synthesis of compounds of formula (I) disclosed in Example 2. Condensation of methyl-2-aminobenzoate derivative (2a) with ethyl-3-ethoxy-2-enoate affords the imine, which then undergoes cyclization to yield quinoline 2b. Various reaction conditions can be used to influence this condensation cyclization reaction according to the relevant methods in this technical field. After that with SOCl 2 or POCl 3 Workup was performed to convert the phenol in 2b to chloride. The chlorine in 2c is then converted to iodine using NaI in a suitable solvent such as acetonitrile or acetone to give 2d. The ester group in 2d is then reduced to the alcohol group using a suitable reducing agent such as, but not limited to, DIBAL. The ester in 2d can also be reduced using other conditions suitable for ester reduction. Then use a method suitable for oxidation of alcohol groups to aceta...

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Abstract

The invention relates to an intergrase inhibitor, and discloses compounds for treating or preventing HIV infection or other virus infections. The compounds can be used as an HIV replication inhibitor, and can be used together with other treatment medicines, especially other antiviral medicines. The invention concretely discloses the compounds for inhibiting HIV replication, medicines containing the compounds, and methods for treating retroviral infection, such as HIV infection through using the compounds, and also discloses an intergrase allosteric inhibitor.

Description

technical field [0001] The present invention discloses compounds useful for treating human immunodeficiency virus (HIV) infection. The invention particularly discloses inhibitors for inhibiting HIV replication, medicines containing such compounds and methods for treating HIV with these compounds. More specifically, the present invention discloses integrase allosteric inhibitors. Background technique [0002] Acquired immunodeficiency syndrome (AIDS) is caused by a retrovirus, the human immunodeficiency virus (HIV). There are two types of HIV virus, HIV-1 and HIV-2, HIV-2 causes less severe disease than HIV-1. The genetic material of retroviruses is RNA (ribonucleic acid), which consists of two separate strands of RNA. Along with the RNA is reverse transcriptase (polymerase and ribonuclease activity), integrase, a protease, and several other proteins. [0003] Compounds that inhibit HIV replication are effective agents for the treatment of HIV and similar diseases. Drugs...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D215/42C07D215/14A61K31/47A61K31/4706A61K45/00A61P31/18
Inventor 吴劲梓古德木德森·克里斯金
Owner 世方科技(杭州)有限公司
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