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|Title:||4-oxoquinoline compound and use thereof as HIV integrase inhibitor|
|Abstract:||An anti-HIV agent containing, as an active ingredient, a 4-oxoquinoline compound represented by the following formula [I] ##STR00001## wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof. The compound of the present invention has HIV integrase inhibitory action and is useful as an anti-HIV agent for the prophylaxis or therapy of AIDS. Moreover, by a combined use with other anti-HIV agents such as protease inhibitors, reverse transcriptase inhibitors and the like, the compound can become a more effective anti-HIV agent. Since the compound has high inhibitory activity specific for integrases, it can provide a safe pharmaceutical agent with a fewer side effects for human.|
|Inventor(s):||Satoh; Motohide (Takatsuki, JP), Kawakami; Hiroshi (Takatsuki, JP), Itoh; Yoshiharu (Takatsuki, JP), Shinkai; Hisashi (Takatsuki, JP), Motomura; Takahisa (Takatsuki, JP), Aramaki; Hisateru (Takatsuki, JP), Matsuzaki; Yuji (Takatsuki, JP), Watanabe; Wataru (Takatsuki, JP), Wamaki; Shuichi (Takatsuki, JP)|
|Assignee:||Japan Tobacco Inc. (Tokyo, JP)|
|Filing Date:||Jun 05, 2006|
|Claims:||1. A compound selected from the group of formulas (a)-(d): ##STR00346## or a stereoisomer thereof, or a tautomer thereof, or a pharmaceutically acceptable salt thereof. |
2. A pharmaceutical composition comprising a compound according to claim 1, or a stereoisomer thereof, or a tautomer thereof, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.
3. A method for the treatment of an HIV infectious disease comprising administering to a mammal the compound of claim 1, or a stereoisomer thereof, or a tautomer thereof, or a pharmaceutically acceptable salt thereof.
4. A compound of the formula: ##STR00347##
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