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Last Updated: December 12, 2025

Claims for Patent: 8,673,893


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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):Andrea Lombardi Borgia, Maria Menichincheri, Paolo Orsini, Achille Panzeri, Ettore Perrone, Ermes Vanotti, Marcella Nesi, Chiara Marchionni
Assignee:Nerviano Medical Sciences SRL
Application Number:US13/611,679
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) wherein: X is —CH2—, —CH(OH)—, —CH(OR′)— or —C(R′R″)—, wherein: R′ is C1-C6 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, NHSO2R10, a straight or branched C1-C6 alkyl optionally substituted by a heterocyclyl, in its turn optionally substituted by a straight or branched C1-C6 alkyl or an heterocyclylalkyl, or a heterocyclyl optionally substituted by a straight or branched C1-C6 alkyl, in its turn optionally substituted by a heterocyclyl or a C1-C6 alkoxycarbonyl, or a C1-C6 dialkylamino: R4 is NR5R6, or a heterocyclyl, optionally further substituted by a straight or branched C1-C6 alkyl, heterocyclylalkyl, heterocyclyl or a C1-C6 dialkylamino; R5 and R6 are independently hydrogen, R8R9N—C2-C6 alkyl, R8O—C2-C6 alkyl, a straight or branched C1-C6 alkyl optionally further substituted by C1-C6 alkoxy, C1-C6 dialkylamino, halogen, phenyl, hydroxyl or heterocyclyl in its turn optionally substituted by alkyl, C3-C6 cycloalkyl optionally substituted by hydroxyl or trifluoro C1-C6 alkyl, heterocyclyl optionally substituted by C1-C6 alkyl in its turn optionally substituted by halogen or heterocyclyl, C1-C6 alkoxycarbonyl, C1-C6 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 C1-C6 alkyl, in its turn optionally substituted by a heterocyclyl or a C1-C6 alkoxycarbonyl, a C1-C6 dialkylamino or a heterocyclyl; R7 is straight or branched C1-C6 alkyl, optionally substituted by C1-C6 dialkylamino or heterocyclyl in its turn substituted by C1-C6 alkyl; R8 and R9 are independently an optionally further substituted straight or branched C1-C6 alkyl; R10 is an optionally further substituted straight or branched C1-C6 alkyl; R is phenyl or pyridyl optionally substituted halogen or straight or branched C1-C6 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.

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