Azaindoles

C - Chemistry – Metallurgy – 07 – D

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C07D 471/04 (2006.01) A61K 31/437 (2006.01) A61K 31/4985 (2006.01) A61P 11/06 (2006.01) A61P 17/06 (2006.01) A61P 29/00 (2006.01) C07D 209/00 (2006.01) C07D 221/00 (2006.01) C07D 241/00 (2006.01) C07D 471/00 (2006.01) C07D 487/00 (2006.01) C07D 487/04 (2006.01) C07D 519/00 (2006.01)

Patent

CA 2395593

The invention is directed to compositions containing physiologically active compounds of general formula (I) wherein R1 is aryl or heteroaryl; R2 represents hydrogen, acyl, cyano, halo, lower alkenyl or lower alkyl optionally substituted by a substituent selected from cyano, heteroaryl, heterocycloalkyl, -Z1R8,-C(=O)-NY3Y4,-CO2R8,-NY3Y4,-N(R6)-C(=O)-R7, -N(R6)- C(=O)-NY3Y4,-N(R6)-C(=O)-OR7, -N(R6)-SO2-R7,-N(R6)-SO2-NY3Y4 and one or more halogen atoms; R3 represents hydrogen, aryl, cyano, halo, heteroaryl, lower alkyl, -C(=O)-OR5 or -C(=O)-NY3Y; and X1 represents N, CH, C-halo, C-CN, C-R7, C-NY3Y4, C-OH, C-Z2R7, C-C(=O)-OR5, C-C(=O)-NY3Y4, C-N(R8)-C(=O)-R7, C-SO2- NY3Y4, C-N(R8)-SO2-R7, C-alkenyl, C-alkynyl or C-NO2; and their produgs, and pharmaceutically acceptable salts and solvates of such compounds and their produgs, as well as to novel compounds within the scope of fomula (I). Such compounds and compositions have valuable pharmaceutical properties, in particular the ability to inhibit protein kinases.

L'invention concerne des compositions renfermant des composés physiologiquement actifs de la formule générale (I), dans laquelle R?1¿ représente un aryle ou un hétéroaryle, R?2¿ représente un hydrogène, un acyle, un cyano, un halo, un alcényle inférieur ou un alkyle inférieur éventuellement substitué par un substituant sélectionné parmi un cyano, un hétéroaryle, un hétérocycloalkyle, -Z?1¿R?8¿,-C(=O)-NY?3¿Y?4¿,-CO¿2?R?8¿,-NY?3¿Y?4¿,-N(R?6¿)-C(=O)-R?7¿ -N(R?6¿)-C(=O)-NY?3¿Y?4¿,-N(R?6¿)-C(=O)-OR?7¿, -N(R?6¿)-SO¿2?-R?7¿,-N(R?6¿)-SO¿2?-NY?3¿Y?4¿ et un ou plusieurs atomes d'halogènes, R?3¿ représente un hydrogène, un aryle, un cyano, un halo, un hétéroaryle, un alkyle inférieur, -C(=O)-OR?5¿ ou -C(=O)-NY?3¿Y, et X?1¿ représente N, CH, C-halo, C-CN, C-R?7¿, C-NY?3¿Y?4¿, C-OH, C-Z?2¿R?7¿, C-C(=O)-OR?5¿, C-C(=O)-NY?3¿Y?4¿, C-N(R?8¿)-C(=O)-R?7¿, C-SO¿2?-NY?3¿Y?4¿, C-N(R?8¿)-SO¿2?-R?7¿, C-alcényle, C-alcynyle ou C-NO¿2?, leurs promédicaments, des sels et des solvats pharmaceutiquement acceptables de ces composés et leurs promédicaments, ainsi que de nouveaux composés dans le champ d'application de la formule générale (I). Ces composés et compositions présentent des propriétés pharmaceutiques intéressantes, en particulier celle d'inhiber les protéines kinases.

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