Nitrogen-containing fused ring compound and use thereof as HIV integrase inhibitor

Abstract

The present invention relates to a nitrogen-containing fused ring compound represented by the following formula [I]wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof, and an anti-HIV agent containing such compound. The compound of the present invention has an HIV integrase inhibitory activity, and is useful as an agent for the prophylaxis or treatment of AIDS, or as an anti-HIV agent. In addition, by the combined use with other anti-HIV agents such as a protease inhibitor, a reverse transcriptase inhibitor and the like, it can be a more effective anti-HIV agent. Becuae it shows integrase-specific high inhibitory activity, the compound can be a pharmaceutical agent safe on human body, which causes only a fewer side effects.

Description

TECHNICAL FIELD The present invention relates to a novel nitrogen-containing fused ring compound or a pharmaceutically acceptable salt thereof useful as an anti-HIV agent. Moreover, the present invention relates to novel use of a certain kind of nitrogen-containing fused ring compound or a pharmaceutically acceptable salt thereof as an anti-HIV agent. More specifically, the present invention relates to an anti-HIV agent containing a nitrogen-containing fused ring compound or a pharmaceutically acceptable salt thereof showing an anti-HIV action particularly based on an integrase inhibitory activity. BACKGROUND ART HIV (Human Immunodeficiency Virus (type 1)) belonging to retrovirus is a causative virus of AIDS (Acquired Immunodeficiency Syndrome). HIV targets CD4 positive cell groups such as helper T cell, macrophage and dendritic cell and destroys these immunocompetent cells to cause immunodeficiency. Accordingly, a pharmaceutical agent that eradicates HIV in a living organism or...

AI Technical Summary

Benefits of technology

The compound of the present invention can be a pharmaceutical agent effective for the prophylaxis or treatment of AIDS, as an anti-HIV agent having an HIV integrase inhibitory activity. In addition, by a combined use with other anti-HIV agents such as protease inhibitors, reverse transcriptase inhibitors and the like, the compound can be a more effective anti-HIV agent. Moreover, since the compound has an integrase-specific high inhibitory activity, it can be a pharmaceutical agent safe on the human body, which is associated with a fewer side effects.

Here, in the case of a compound wherein Ry2 is Ry2′—CX5H—CY5H— (wherein X5 and Y5 are each a lower alkyl group such as methyl group, ethyl group and the like and Ry2′ is a group such as a C1-7 alkyl group, a C3-8 cycloalkyl C1-6 alkyl group and a C6-14 aryl C1-6 alkyl group, wherein the alkyl moiety is free of CX5H—CY5H moiety), fine results are often obtained by using Ry2′—CX5═CY5—SnBu3 to give compound [8′-3] wherein Ry2 is Ry2′—CX5═CY5—, and subjecting this compound to a catalytic reduction to give compound [8′-3] wherein Ry2 is Ry2′—CX5H—CY5H—.

Problems solved by technology

However, some of these pharmaceutical agents are known to HIV cause side effects such as liver function failure, central nervous disorders (e.g., vertigo), and the like.

In addition, acquisition of resistance to a pharmaceutical agent causes a problem.

Nevertheless, an effective integrase inhibitor has not been found as yet.

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