Derivatives of pyrroloindole which are inhibitors of Hsp90, compositions containing same, and use thereof

Pyrroloindoles of formula (I) are provided 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...

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Hauptverfasser: ALASIA MARCEL, MINOUX HERVE, RUXER JEAN-MARIE
Format: Patent
Sprache:eng
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Zusammenfassung:Pyrroloindoles of formula (I) are provided 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-COCH2-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 independently a single bond, CH2, CH-alkyl, and CH-aralkyl; n=1, 2 and m=0, 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, CONH(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.