6,7-dihydroimidazo[1,5-a]pyrazin-8(5H)-one derivatives as protein kinase modulators

摘要

There are provided 3,5-disubstituted derivatives of 6,7-dihydroimidazo[1,5-a]pyrazin-8(5H)-one compounds of formula (I) or a pharmaceutically acceptable salt thereof as defined in the present specification, which modulate the activity of protein kinases. The compounds are therefore useful in treating diseases caused by dysregulated protein kinase activity. In particular, such diseases to be treated with a compound of formula (I) of the present invention is one caused by and/or associated with disregulated protein kinase activity selected from the group consisting of cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders. The present invention also relates to processes for preparing the compounds of formula (I), combinatorial libraries thereof, pharmaceutical compositions comprising them, and methods of treating diseases utilizing pharmaceutical compositions comprising a compound of formula (I).;

主权项

1. A compound of the formula (I): wherein: R1 is —NR3R4 or —OR3; R2 is a hydrogen atom or an optionally substituted group selected from straight or branched C1-C6 alkyl, aryl, heteroaryl, aryl C1-C6 alkyl and heteroaryl C1-C6 alkyl; R3 and R4, the same or different, are each independently hydrogen atom or an optionally substituted group selected from straight or branched C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C6 cycloalkyl, cycloalkyl C1-C6 alkyl, heterocyclyl, heterocyclyl C1-C6 alkyl, aryl, aryl C1-C6 alkyl, heteroaryl and heteroaryl C1-C6 alkyl, or R3 and R4, taken together with the nitrogen atom to which they are bonded, may form an optionally substituted 3 to 7 membered heterocyclyl or heteroaryl ring, optionally containing one additional heteroatom or heteroatomic group selected from S, O, N and NH; or a pharmaceutically acceptable salt thereof, wherein the optionally substituted group of R2, R3 and R4 is substituted in any of its free positions by 1 to 6 groups, selected from the groups consisting of: halogen, nitro, oxo groups (═O), carboxy, cyano, C1-C6 alkyl, polyfluorinated alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C6 cycloalkyl, heterocyclyl, aryl, heteroaryl; amino groups and derivatives thereof; carbonylamino groups and derivatives thereof; hydroxy groups and derivatives thereof; carbonyl groups and derivatives thereof; and sulfurated derivatives, wherein when R1 is —NR3R4, only one of R3 and R4 are hydrogen and when R1 is —OR3, R3 is not hydrogen.