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US 8,557,845 B2Granted
Substituted pyrrolo-pyrazole derivatives as kinase inhibitors
AssigneeNerviano Medical Sciences S.R.L.
InventorsMaria Gabriella Brasca, Raffaella Amici, Daniele Fancelli, Marcella Nesi, Paolo Orsini, Fabrizio Orzi, Patrick Roussel, Anna Vulpetti, Paolo Pevarello
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Abstract
Compounds represented by formula (Ia) or (Ib) and wherein R and R1 are as defined in the description, and pharmaceutically acceptable salts thereof, are disclosed; the said compounds are useful in the treatment of cell cycle proliferative disorders, e.g. cancer, associated with an altered cell cycle dependent kinase activity.
Claims10
A compound represented by formula (Ib)
- wherein
- R is a group —CORa, —CONHRa or —CONRaRb wherein Ra and Rb are, each independently, hydrogen or an optionally substituted group selected from straight or branched C1-C6 alkyl, C3-C6 cycloalkyl, aryl, arylalkyl, heterocyclyl or heterocyclylalkyl or;
- together with the nitrogen atom to which they are bonded, Ra and Rb may form an optionally substituted 5 or 6 membered heterocycle optionally containing one additional heteroatom or heteroatomic group selected among N, NH, O or S;
- R1 is
- wherein, the formula (IIa), the cycle represents a 5 to 7 membered heterocyclic ring wherein X, directly linked to the rest of the molecule, represents a carbon or nitrogen atom;
- Y is a carbon, nitrogen, oxygen or sulfur atom or it is an NH group, provided that at least one of X and Y is other than a carbon atom;
- Rc is, independently from each other and in any one of the free positions of the heterocyclic ring of formula (IIa), a halogen atom or hydroxy group or it is an optionally substituted group selected from straight or branched C1-C6 alkyl, C3-C6 cycloalkyl, aryl, arylalkyl, heterocyclyl, heterocyclylalkyl, amino, aminocarbonyl, carboxy, oxo (═O), alkoxycarbonyl, alkylcarbonyl or arylcarbonyl;
- and n is 0 or an integer from 1 to 4;
- or a pharmaceutically acceptable salt thereof.
6 more elements
A library of two or more compounds of formula (Ib)
- wherein
- R is a group —CORa, —CONHRa or —CONRaRb wherein Ra and Rb are, each independently, hydrogen or an optionally substituted group selected from straight or branched C1-C6 alkyl, C3-C6 cycloalkyl, aryl, arylalkyl, heterocyclyl or heterocyclylalkyl or;
- together with the nitrogen atom to which they are bonded, Ra and Rb may form an optionally substituted 5 or 6 membered heterocycle optionally containing one additional heteroatom or heteroatomic group selected among N, NH, O or S;
- RI is
- a group of formula (IIa):
- wherein, in formula (IIa), the cycle represents a 5 to 7 membered heterocyclic ring wherein X, directly linked to the rest of the molecule, represents a carbon or nitrogen atom;
- Y is a carbon, nitrogen, oxygen or sulfur atom or it is an NH group, provided that at least one of X and Y is other than a carbon atom;
- Rc is, independently from each other and in any one of the free positions of the heterocyclic ring of formula (IIa), a halogen atom or hydroxy group or it is an optionally substituted group selected from straight or branched C1-C6 alkyl, C3-C6 cycloalkyl, aryl, arylalkyl, heterocyclyl, heterocyclylalkyl, amino, aminocarbonyl, carboxy, xoxo (═O), alkoxycarbonyl, alkylcarbonyl or arylcarbonyl;
- and n is 0 or an integer from 1 to 4;
- or a pharmaceutically acceptable salt thereof.
7 more elements
Dependencies are inferred from the claim text.