Claims for Patent: 8,673,893

Summary for Patent: 8,673,893

Title:	Substituted indazole derivatives active as kinase inhibitors
Abstract:	Substituted indazole 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 deregulated protein kinase activity, like cancer.
Inventor(s):	Lombardi Borgia; Andrea (Paullo, IT), Menichincheri; Maria (Milan, IT), Orsini; Paolo (Legnano, IT), Panzeri; Achille (Merate, IT), Perrone; Ettore (Boffalora Sopra Ticino, IT), Vanotti; Ermes (Milan, IT), Nesi; Marcella (Saronno, IT), Marchionni; Chiara (Milan, IT)
Assignee:	Nerviano Medical Sciences S.r.l. (Neviano (MI), IT)
Application Number:	13/611,679
Patent Claims:	1. A method for treating a disease, the disease selected from the group consisting of ovarian cancer, lung cancer, colon cancer and lymphoma, which comprises administering to a mammal in need thereof an effective amount of a compound of formula (I) ##STR00133## wherein: X is --CH.sub.2--, --CH(OH)--, --CH(OR')-- or --C(R'R'')--, wherein: R' is C.sub.1-C.sub.6 alkyl and R'' is hydrogen; Ar is phenyl, pyrazolyl or pyridyl optionally substituted with one or more substituents independently selected from halogen, nitro, COR4, OR7, NR5R6, NHSO.sub.2R10, a straight or branched C.sub.1-C.sub.6 alkyl optionally substituted by a heterocyclyl, in its turn optionally substituted by a straight or branched C.sub.1-C.sub.6 alkyl or an heterocyclylalkyl, or a heterocyclyl optionally substituted by a straight or branched C.sub.1-C.sub.6 alkyl, in its turn optionally substituted by a heterocyclyl or a C.sub.1-C.sub.6 alkoxycarbonyl, or a C.sub.1-C.sub.6 dialkylamino: R4 is NR5R6, or a heterocyclyl, optionally further substituted by a straight or branched C.sub.1-C.sub.6 alkyl, heterocyclylalkyl, heterocyclyl or a C.sub.1-C.sub.6 dialkylamino; R5 and R6 are independently hydrogen, R8R9N--C.sub.2-C.sub.6 alkyl, R8O--C.sub.2-C.sub.6 alkyl, a straight or branched C.sub.1-C.sub.6 alkyl optionally further substituted by C.sub.1-C.sub.6 alkoxy, C.sub.1-C.sub.6 dialkylamino, halogen, phenyl, hydroxyl or heterocyclyl in its turn optionally substituted by alkyl, C.sub.3-C.sub.6 cycloalkyl optionally substituted by hydroxyl or trifluoro C.sub.1-C.sub.6 alkyl, heterocyclyl optionally substituted by C.sub.1-C.sub.6 alkyl in its turn optionally substituted by halogen or heterocyclyl, C.sub.1-C.sub.6 alkoxycarbonyl, C.sub.1-C.sub.6 dialkylamino, heterocyclyl, or phenyl, or R5 and R6, taken together with the nitrogen atom to which they are bonded, may form a heterocyclyl group optionally substituted by a straight or branched C.sub.1-C.sub.6 alkyl, in its turn optionally substituted by a heterocyclyl or a C.sub.1-C.sub.6 alkoxycarbonyl, a C.sub.1-C.sub.6 dialkylamino or a heterocyclyl; R7 is straight or branched C.sub.1-C.sub.6 alkyl, optionally substituted by C.sub.1-C.sub.6 dialkylamino or heterocyclyl in its turn substituted by C.sub.1-C.sub.6 alkyl; R8 and R9 are independently an optionally further substituted straight or branched C.sub.1-C.sub.6 alkyl; R10 is an optionally further substituted straight or branched C.sub.1-C.sub.6 alkyl; R is phenyl or pyridyl optionally substituted halogen or straight or branched C.sub.1-C.sub.6 alkyl; R1, R2 and R3 are hydrogen; or optical isomers, tautomers or pharmaceutically acceptable salt thereof. 2. The method according to claim 1 which provides tumor angiogenesis and metastasis inhibition. 3. The method according to claim 1 further comprising subjecting the mammal in need thereof to a radiation therapy or chemotherapy regimen in combination with at least one cytostatic or cytotoxic agent. 4. The method according to claim 1 wherein the mammal in need thereof is a human.