Indole derivatives with antiviral activity

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 209/12 (2006.01) A61K 31/40 (2006.01) A61K 31/41 (2006.01) A61K 31/415 (2006.01) A61K 31/44 (2006.01) A61K 31/535 (2006.01) C07D 209/18 (2006.01) C07D 209/20 (2006.01) C07D 209/22 (2006.01) C07D 401/04 (2006.01) C07D 403/06 (2006.01) C07D 409/06 (2006.01) C07D 409/14 (2006.01) C07D 417/06 (2006.01)

Patent

CA 2326166

Compounds represented by formula (I), wherein R1 represents hydrogen, lower alkyl, optionally substituted arylsulfonyl, etc.; R2 represents hydrogen, lower alkyl, optionally substituted aralkyl, etc.; R3, R4, R5, and R6 each independently represents hydrogen, halogeno, lower trihaloalkyl, etc.; X represents hydroxy or optionally substituted amino; and Y represents COOR (R is hydrogen or an ester residue), optionally substituted aryl, or optionally substituted heteroaryl. They have an integrase inhibitory activity and are useful as an anti-HIV agent.

Composés représentés par la formule (I) dans laquelle R?1¿ représente hydrogène, alkyle inférieur, arylsulfonyle éventuellement substitué; R?2¿ représente hydrogène, alkyle inférieur, aralkyle éventuellement substitué; R?3¿, R?4¿; R?5¿ et R?6¿ représentent chacun indépendamment hydrogène, halogéno, trihaloalkyle inférieur; X représente hydroxy ou amino éventuellement substitué; Y représente COOR (R représentant hydrogène ou un résidu d'ester), aryle éventuellement substitué ou hétéroaryle éventuellement substitué. Ces composés exercent une activité d'inhibition d'intégrase et sont utiles en tant qu'agent anti-VIH.

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