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US 9,309,253 B2Granted
Tricyclic pyrrolo derivatives, process for their preparation and their use as kinase inhibitors
AssigneeNerviano Medical Sciences S.R.L.
InventorsMarina Caldarelli, Mauro Angiolini, Italo Beria, Maria Gabriella Brasca, Francesco Casuscelli, Roberto D'Alessio, Andrea Lombardi Borgia
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Abstract
The present invention relates to tricyclic pyrrolo derivatives which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity. 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.
Claims13
A compound of formula (I):
- wherein
- R1 is hydrogen, halogen or an optionally substituted group selected from amino, straight or branched C1-C6 alkyl, C3-C7 cycloalkyl, cycloalkyl-alkyl, aryl, arylalkyl, heterocyclyl and heterocyclylalkyl;
- R2 is a group selected from —NR″R′″, —N(OR′″)R″ and OR″, wherein R″ and R′″ are, each independently, hydrogen or an optionally substituted group selected from straight or branched C1-C6 alkyl, C3-C7 cycloalkyl, cycloalkyl-alkyl, aryl, arylalkyl, heterocyclyl and heterocyclylalkyl or, together with the nitrogen atom to which they are bonded, R″ and R′″ may form a 5 to 6 membered heteroaryl or heterocyclyl group, optionally containing one additional heteroatom selected among N, O and S;
- R3 is hydrogen or optionally substituted group selected from straight or branched C1-C6 alkyl, C3-C7 cycloalkyl, cycloalkyl-alkyl, aryl, arylalkyl, heterocyclyl and heterocyclylalkyl;
- R4 is hydrogen or an optionally substituted group selected from straight or branched C1-C6 alkyl, C3-C7 cycloalkyl, cycloalkyl-alkyl, aryl, arylalkyl, heterocyclyl and heterocyclylalkyl;
- X is a single bond or a divalent radical selected from —NR′—, —CONR′—, —NH—CO—NH—, —O—, —S—, —SO2— and —OSO2—, wherein R′ is hydrogen or an optionally substituted group selected from straight or branched C1-C6 alkyl, C3-C7 cycloalkyl, cycloalkyl-alkyl, aryl, arylalkyl, heterocyclyl and heterocyclylalkyl or, together with the nitrogen atom to which they are bound, R1 and R′ may form a 5 to 6 membered heteroaryl or heterocyclyl group optionally containing one additional heteroatom selected from N, O and S;
- A is —(CH2)3—;
- or a pharmaceutically acceptable salt thereof.
5 more elements
Dependencies are inferred from the claim text.