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.
Claims16
A method for treating a cancer, the method comprising administering to a mammal in need thereof an effective amount of a compound represented by the following formula:
- 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;
- and
- R1 is tert-butyl;
- or a pharmaceutically acceptable salt thereof.
A compound represented by the following formula:
- 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;
- and
- R1 is tert-butyl;
- or a pharmaceutically acceptable salt thereof.
A compound:
- N-[5-(2,2-dimethylpropanoyl)-6,6-dimethyl-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl]-4-fluorobenzamide;
- or a pharmaceutically acceptable salt thereof.
A library of two or more compounds of the following formula:
- 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;
- and
- R1 is tert-butyl;
- or pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.