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US 2014/0228351 A1Published application
Substituted indazole derivatives active as kinase inhibitors
AssigneeNerviano Medical Sciences S.R.L.
InventorsAndrea Lombardi Borgia, Maria Menichincheri, Paolo Orsini, Achille Panzeri, Ettore Perrone, Ermes Vanotti, Marcella Nesi, Chiara Marchionni
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Abstract
Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a deregulated protein kinase activity, like cancer.
Claims2
A compound of formula (I):
- wherein:
- X is —CH2—, —CH(OH)—, —CH(OR′)— or —C(R′R″)—, wherein:
- R′ is C1-C6 alkyl and R″ is hydrogen or C1-C6 alkyl;
- Ar is aryl or heteroaryl optionally substituted with one or more substituents independently selected from halogen, C2-C6 alkenyl, C2-C6 alkynyl, cyano, nitro, NHCOR4, COR4, NR5R6, NR5COR4, OR7, SR7, SOR10, SO2R10, NHSOR10, NHSO2R10, R8R9N—C1-C6 alkyl, R8O—C1-C6 alkyl, an optionally further substituted straight or branched C1-C6 alkyl, C3-C6 cycloalkyl, heterocyclyl, aryl and heteroaryl, wherein:
- R4 is hydrogen, C2-C6 alkenyl, C2-C6 alkynyl, NR5R6, OR7, SR7, R8R9N—C1-C6 alkyl, R8O—C1-C6 alkyl, an optionally further substituted straight or branched C1-C6 alkyl, C3-C6 cycloalkyl, heterocyclyl, aryl or heteroaryl;
- R5 and R6 are independently hydrogen, C2-C6 alkenyl, C2-C6 alkynyl, R8R9N—C2-C6 alkyl, R8O—C2-C6 alkyl, an optionally further substituted straight or branched C1-C6 alkyl, C3-C6 cycloalkyl, heterocyclyl, aryl or heteroaryl, or R5 and R6, taken together with the nitrogen atom to which they are bonded, may form an optionally substituted heterocyclyl group;
- R7 is hydrogen, C2-C6 alkenyl, C2-C6 alkynyl, COR4, SOR10, SO2R10, R8R9N—C2-C6 alkyl, R8O—C2-C6 alkyl, an optionally further substituted straight or branched C1-C6 alkyl, C3-C6 cycloalkyl, heterocyclyl, aryl or heteroaryl, wherein R4 is as defined above;
- R8 and R9 are independently hydrogen, C2-C6 alkenyl, C2-C6 alkynyl, COR4, an optionally further substituted straight or branched C1-C6 alkyl, C3-C6 cycloalkyl, heterocyclyl, aryl or heteroaryl, or R8 and R9, taken together with the nitrogen atom to which they are bonded, may form an optionally substituted heterocyclyl group, wherein R4 is as defined above;
- R10 is hydrogen, C2-C6 alkenyl, C2-C6 alkynyl, NR5R6, OR7, R8R9N—C1-C6 alkyl, R8O—C1-C6 alkyl, an optionally further substituted straight or branched C1-C6 alkyl, C3-C6 cycloalkyl, heterocyclyl, aryl or heteroaryl, wherein R5, R6, R7, R8 and R9 are as defined above;
- R is an optionally substituted straight or branched C1-C6 alkyl, C3-C6 cycloalkyl, heterocyclyl, aryl or heteroaryl;
- R1, R2 and R3 are independently hydrogen, halogen, nitro, an optionally substituted straight or branched C1-C6 alkyl, NR5R6, or OR7, wherein R5, R6 and R7 are as defined above;
- or isomers, tautomers, prodrugs or pharmaceutically acceptable salt thereof.
9 more elements
Dependencies are inferred from the claim text.