Heteroaromatic derivatives having an inhibitory activity...

Details Heteroaromatic derivatives having an inhibitory activity... Heteroaromatic derivatives having an inhibitory activity...

C - Chemistry, Metallurgy

07

D

C07D 207/333 (2006.01) A61K 31/341 (2006.01) A61K 31/381 (2006.01) A61K 31/40 (2006.01) A61K 31/4025 (2006.01) A61K 31/415 (2006.01) A61K 31/4155 (2006.01) A61K 31/4178 (2006.01) A61K 31/4184 (2006.01) A61K 31/4196 (2006.01) A61K 31/422 (2006.01) A61K 31/4245 (2006.01) A61K 31/426 (2006.01) A61K 31/427 (2006.01) A61K 31/433 (2006.01) A61K 31/443 (2006.01) A61K 31/4439 (2006.01) A61K 31/4709 (2006.01) A61K 31/4725 (2006.01) A61K 31/497 (2006.01) A61K 31/506 (2006.01) A61P 31/12 (2006.01) A61P 31/18 (2006.01)

Patent

CA 2353961

Compounds represented by general formula (I), tautomers of the same, prodrugs of both, or pharmaceutically acceptable salts or hydrates of them, which exhibit integrase inhibiting activities: wherein X is hydroxyl, protected hydroxyl or optionally substituted amino; Y is COORA (wherein RA is hydrogen or an ester residue), CONRBRC (wherein RB and RC are each independently hydrogen or an amide residue), optionally substituted aryl or optionally substituted heteroaryl; and A1 is optionally substituted heteroaryl, with the proviso that the cases wherein either or both of Y and A1 are optionally substituted indol-3-yl are excepted.

L'invention concerne des composés représentés par la formule générale (I), des tautomères de ceux-ci, des promédicaments des composés et tautomères de ceux-ci, de même que des sels ou hydrates, acceptables sur le plan pharmacologique, et démontrant tous des activités inhibitrices de l'intégrase. Dans cette formule, X représente hydroxyle, hydroxyle protégé ou amino éventuellement substitué, Y représente COOR?A¿ (où R?A¿ représente hydrogène ou un reste ester), CONR?B¿R?C¿ (où R?B¿ et R?C¿ représentent chacun indépendamment hydrogène ou un reste amide), aryle, ou hétéroaryle, éventuellement substitués, et A?1¿ représente hétéroaryle éventuellement substitué, à condition que soit Y, soit A?1¿, soit les deux ne puissent être éventuellement substitués par indol-3-yle.

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