Tricyclic pyrrolo derivatives, process for their preparation and their use as kinase inhibitors

摘要

The present invention relates to tricyclic pyrrolo derivatives of Formula (I), 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.;

主权项

1. 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 —NHR″ and —N(OR′″)R″ 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; 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 group selected from —NR′—, —O— and —S—, 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 a group selected from —(CH2)2—, —CH—CH—, —C(CH3)2—CH2— and —CH2—C(CH3)2; or a pharmaceutically acceptable salt thereof, with the proviso that the following compounds are excluded: 2-amino-9-methyl-6,9-dihydro-5H-pyrrolo[3,2-h]quinazoline-7-carboxamide, 2-amino-8-phenyl-9H-pyrrolo[3,2-h]quinazoline-7-carboxamide, 2-amino-9-methyl-8-phenyl-9H-pyrrolo[3,2-h]quinazoline-7-carboxamide and 2-amino-9-methyl-8-phenyl-6,9-dihydro-5H-pyrrolo[3,2-h]quinazoline-7-carboxamide.