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US 8,138,217 B2Granted
1H-thieno[2,3-c]pyrazole derivatives useful as kinase inhibitors
AssigneeNerviano Medical Sciences S.R.L.
InventorsDaniele Fancelli, Paola Vianello, Mario Varasi, Simona Bindi, Sergio Vioglio, Dania Tesei
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Abstract
Thieno[2,3-c]pyrazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.
Claims20
A compound of formula (I)
- wherein
- R is an optionally substituted aryl or heteroaryl group;
- R1 and R2 represent, the same or different and independently from each other, a hydrogen atom, a straight or branched C1-C3 alkyl or a group —CONH2 or —CH2NR′R″ or, taken together with the carbon atom to which they are bonded, R1 and R2 may form a C3-C6 cycloalkyl group;
- with the proviso that at least one of R1 and R2 is other than a hydrogen atom;
- R′ and R″ represent, the same or different and independently from each other, a hydrogen atom or a straight or branched C1-C3 alkyl group or, taken together with the nitrogen atom to which they are bonded, R′ and R″ may form a heterocyclic ring of formula
- wherein R′″ is a hydrogen atom or a straight or branched C1-C3 alkyl group;
- R3 is a hydrogen or halogen atom or a group selected from hydroxy, cyano, straight or branched C1-C3 alkyl or C1-C3 alkoxy;
- or stereoisomers, tautomers, and pharmaceutically acceptable salts thereof with the proviso that the compound not have one of R1 and R2 be a hydrogen atom, the other one of R1 and R2 be a C1-C3 alkyl and R be a 4-(1-methyl-piperazin-4-yl)phenyl.
5 more elements
Dependencies are inferred from the claim text.