SUBSTITUTED 3,4-DIHYDROPYRROLO[1,2-a]PYRAZIN-1(2H)-ONE DERIVATIVES AS KINASES INHIBITORS

摘要

The present invention relates to substituted 3,4-dihydropyrrolo[1,2-a]pyrazin-1(2H)-one 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 compounds or the pharmaceutical compositions containing them.

主权项

1. A compound of formula (I): wherein R1 is NR5R6 wherein R5 and R6 are each independently hydrogen, an optionally substituted group selected from straight or branched C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C7 cycloalkyl, cycloalkyl-alkyl, aryl, arylalkyl, heterocyclyl and heterocyclylalkyl; or R5 and R6 together with the nitrogen atom to which they are bound, form a 5 to 7 membered heterocyclyl group optionally containing one additional heteroatom selected from N, O and S; R2 is aryl, arylalkyl, heterocyclyl or heterocyclylalkyl; R3 and R4 are each independently hydrogen, halogen, cyano, or an optionally substituted group selected from straight or branched C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C7 cycloalkyl, cycloalkyl-alkyl, aryl, arylalkyl, heterocyclyl and heterocyclylalkyl; and a pharmaceutically acceptable salt thereof, provided that when R3 and R4 are hydrogen, R5 is a group of formula wherein R7 is an optionally substituted group selected from straight or branched C1-C6 alkyl, C3-C7 cycloalkyl, and cycloalkyl-alkyl; and Y is N—R′ or CH—NR′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, cycloalkylalkyl, heterocyclyl and heterocyclylalkyl.