C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 215/56 (2006.01) A61K 31/4375 (2006.01) A61K 31/47 (2006.01) A61K 31/4709 (2006.01) A61K 31/5377 (2006.01) A61K 45/06 (2006.01) A61P 31/12 (2006.01) A61P 31/18 (2006.01) A61P 43/00 (2006.01) C07D 401/06 (2006.01) C07D 409/06 (2006.01) C07D 417/06 (2006.01) C07D 471/04 (2006.01)
Patent
CA 2470365
An anti-HIV agent containing, as an active ingredient, a 4-oxoquinoline compound represented by the following formula [I] (see formula I] 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.
La présente invention concerne des composés 4-oxoquinoliniques représentés par la formule générale (I) suivante, certains de leurs sels pharmaceutiquement admis, ou des agents anti-VIH contenant ces composés. Dans cette formule générale (I), les symboles sont tels que définis dans les spécifications. L'activité d'inhibition de la VIH-intégrase de ces composés fait qu'ils conviennent particulièrement comme agents anti-VIH dans des médicaments ou des traitements prophylactiques anti-SIDA. L'association de ces composés à d'autres agents anti-VIH tels qu'un inhibiteur de protéase ou un inhibiteur de transcriptase inverse permet d'en augmenter l'efficacité anti-VIH. Du fait de leur puissance d'inhibition des intégrases, ces composés constituent des médicaments sans nocivité particulière pour l'homme, et sensiblement dépourvus d'effets secondaires.
Aramaki Hisateru
Itoh Yoshiharu
Kawakami Hiroshi
Matsuzaki Yuji
Motomura Takahisa
Japan Tobacco Inc.
Ridout & Maybee Llp
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