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US 10,478,423 B2Granted
Substituted indazole derivatives active as kinase inhibitiors
AssigneeNerviano Medical Sciences S.R.L.
InventorsAndrea Lombardi Borgia, Marina Ciomei, Daniele Donati, Marcella Nesi
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Abstract
The present invention relates to substituted indazole compounds which modulate the activity of protein kinases and are therefore useful in treating diseases caused by degulated protein kinase activity, like cancer. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such these compounds or the pharmaceutical compositions containing them.
Claims14
A compound of formula (I):
- wherein:
- Ar is a group selected from
- wherein:
- R1 is A, NR6R7, OR8, SOnR9, COR10, nitro, cyano or an optionally substituted group selected from C3-C6 cycloalkyl and heteroaryl;
- R2, R3, R4 and R5 are independently hydrogen, halogen, nitro, cyano, SOnR9, COR10, NR11R12, OR13 or an optionally substituted group selected from straight or branched C1-C6 alkyl, straight or branched C2-C6 alkenyl, straight or branched C2-C6 alkynyl, C3-C6 cycloalkyl and heterocyclyl wherein:
- A is a straight or branched C1-C6 alkyl substituted with a group selected from an optionally substituted heterocyclyl, an optionally substituted heteroaryl, SOnR9, COR10, NR11R12 and OR13;
- R6 is hydrogen or an optionally substituted group selected from straight or branched C1-C6 alkyl, straight or branched C2-C6 alkenyl, straight or branched C2-C6 alkynyl, C3-C6 cycloalkyl, heterocyclyl, aryl and heteroaryl;
- R7 is hydrogen, SOnR9, COR10, a substituted straight or branched C1-C6 alkyl or an optionally substituted group selected from straight or branched C2-C6 alkenyl, straight or branched C2-C6 alkynyl, C3-C6 cycloalkyl, heterocyclyl, aryl and heteroaryl or
- R6 and R7, taken together with the nitrogen atom to which they are bound, may form an optionally substituted heterocyclyl group;
- R8 is hydrogen, A, COR10 or an optionally substituted group selected from straight or branched C2-C6 alkenyl, straight or branched C2-C6 alkynyl, C3-C6 cycloalkyl, heterocyclyl, aryl and heteroaryl, wherein A is as defined above;
- R9 is NR11R12 or an optionally substituted group selected from straight or branched C1-C6 alkyl, straight or branched C2-C6 alkenyl, straight or branched C2-C6 alkynyl, C3-C6 cycloalkyl, heterocyclyl, aryl and heteroaryl;
- R10 is hydrogen, NR11R12, OR13 or an optionally substituted group selected from straight or branched C1-C6 alkyl, straight or branched C2-C6 alkenyl, straight or branched C2-C6 alkynyl, C3-C6 cycloalkyl, heterocyclyl, aryl and heteroaryl;
- R11 and R12 are independently hydrogen, SOnR9, COR10 or an optionally substituted group selected from straight or branched C1-C6 alkyl, straight or branched C2-C6 alkenyl, straight or branched C2-C6 alkynyl, C3-C6 cycloalkyl, heterocyclyl, aryl and heteroaryl, wherein R9 and R10 are as defined above, or
- R11 and R12, taken together with the nitrogen atom to which they are bound, may form an optionally substituted heterocyclyl group;
- R13 is hydrogen, COR10 or an optionally substituted group selected from straight or branched C1-C6 alkyl, straight or branched C2-C6 alkenyl, straight or branched C2-C6 alkynyl, C3-C6 cycloalkyl, heterocyclyl, aryl and heteroaryl, wherein R10 is as defined above;
- n is 0, 1 or 2;
- X is an optionally substituted straight or branched C1-C6 alkyl;
- Y is oxygen;
- Z is an optionally substituted straight or branched C1-C6 alkyl;
- Ar′ is an optionally substituted aryl or an optionally substituted heteroaryl;
- or a pharmaceutically acceptable salt thereof.
18 more elements
Dependencies are inferred from the claim text.