Novel derivatives of pyrroloindole inhibitors of hsp90,...

Details Novel derivatives of pyrroloindole inhibitors of hsp90,... Novel derivatives of pyrroloindole inhibitors of hsp90,...

C - Chemistry, Metallurgy

07

D

C07D 487/04 (2006.01) A61K 31/437 (2006.01) C07D 207/323 (2006.01) C07D 209/40 (2006.01) C07D 233/64 (2006.01) C07D 471/04 (2006.01)

Patent

CA 2727626

The invention relates to novel products of formula (I) wherein Het is an aromatic or partially unsaturated, monocyclic or bicyclic heterocycle containing between 1 and 4 heteroatoms N, O or S, optionally substituted by R1 or R'1 which are the same or different; R is X-(A-B)n-CONH2, X-(A-B)n-O-CONH2, X-(A-B)n-NH-CONH2, X-(CH2)m- heterocycloalkyl, X-(CH2)m-aryl and X-(CH2)m-heteroaryl wherein X is -O-C(O), -NH-C(O), NH-CS, -NH-CO-CH2-O-; -NH-CO-CH2-S-CH2-CO-NH-; -NH-CO-(CH2)2- SO2-; and -NH-CO-CH2-N(CH3)-CO-; A and B are the same or different and are each a single bond, CH2, CH-alkyl, and CH-aralkyl, n = 1,2 and m = O, 1; R1 and/or R'1 are H, halogen, CF3, nitro, cyano, alkyle, hydroxy, mercapto, amino, alkylamino, dialkylamino, alkoxy, alkylthio, and carboxy, free or esterified by an alkyl, carboxamide, CO-NH(alkyl), CON(alkyl)2, NH-CO-alkyl, sulfonamide, NH- SO2-alkyl, S(O)2-NHalkyl, and S(O2)-N(alkyl)2 group, all of said alkyl, alcoxy and alkylthio groups being optionally substituted themselves, said products being in all isomer forms and salts, as medicaments.

L'invention concerne les nouveaux produits de formule (I) : avec Het représente un hétérocycle aromatique ou partiellement insataré, mono ou bicyclique, contenant de 1 à 4 hétéroatomes N, O ou S, éventuellement substitué par R1 ou R'1 identiques ou différents; R représente X-(A-B)n-CONH2, X-(A-B)n-O-CONH2, X-(A-B)n-NH-CONH2, X-(CH2)m- hétérocycloalkyle, X--(CH2)m-aryle et X-(CH2)m-hétéroaryle avec X représente -O-C(O), -NH-C(O), NH-CS, -NH-CO-CH2-O-; -NH-CO-CH2-S--CH2-CO-NH-; -NH-CO-(CH2)2- SO2-; -NH-CO-CH2-N(CH3)-CO-; A et B identiques ou différents représentent indépendamment une simple liaison, CH2, CH-alkyle, CH-aralkyle, n = 1,2 et m = O, 1; R1 et/ou R'1 représentent H, halogène, CF3, nitro, cyano, alkyle, hydroxy, mercapto, amino, alkylamino, dialkylamino, alkoxy, alkylthio, carboxy libre ou estérifié par un radical alkyle, carboxamide, CO-NH(alkyl), CON(alkyl)2, NH-CO-alkyl, sulfonamide, NH- SO2-alkyl, S(O)2-NHalkyl, S(O2)--N(alkyl)2, tous ces radicaux alkyle, alcoxy et alkylthio étant eux- mêmes éventuellement substitués; ces produits étant sous toutes les formes isomères et les sels, à titre de médicaments.

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