Japan Tobacco Inc.

Shinichi Kiyonari

Wataru Watanabe

Yuji Matsuzaki

Shuichi Wamaki

Kazunobu Yamataka

Hiroshi Kawakami

Takashi Matsuda

Hisashi Shinkai

Susumu Miyazaki

Mitsuru Takahashi

Satoshi Okuda

Motohide Satoh

Susumu Katoh

Hisateru Aramaki

Satoru Kobayashi

Hirotaka Isoshima

Kaoru Adachi

Naohito Yamada

Akemi Nagao

Provision of a compound having an anti-HIV activity, particularly an integrase inhibitory activity. A 4-oxoquinoline compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof: wherein each symbol is as defined in the specification. The present invention also relates to a pharmaceutical composition containing the 4-oxoquinoline compound or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier; an integrase inhibitor, an antiviral agent, anti-HIV agent, and the like, which contains the 4-oxoquinoline compound or a pharmaceutically acceptable salt thereof as an active ingredient; an anti-HIV composition containing the 4-oxoquinoline compound or a pharmaceutically acceptable salt thereof, and one or more other kinds of anti-HIV activity substances as active ingredients; an anti-HIV agent containing the 4-oxoquinoline compound or a pharmaceutically acceptable salt thereof as an active ingredient, which is used for a multiple drug therapy with other anti-HIV agent(s), and the like.

4-oxoquinoline compound and use thereof as HIV integrase inhibitor

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. Because 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.

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

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Osaka, Japan

Shinichi Kiyonari