ALKYNYL SUBSTITUTED PYRIMIDINYL-PYRROLES ACTIVE AS KINASES INHIBITORS

摘要

The present invention relates to alkynyl substituted pyrimidinyl-pyrrole compounds which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular Jak and/or Src family kinases. 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: one selected from R1 and R2 is hydrogen and the other is ethynyl-R7, wherein: R7 is hydrogen, trialkylsylyl or an optionally substituted group selected from straight or branched C1-C6 alkyl, C3-C7 cycloalkyl, cycloalkyl-alkyl, aryl, aryl-alkyl, heterocyclyl and heterocyclyl-alkyl; R3 and R4 are independently 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-C7 cycloalkyl, cycloalkyl-alkyl, aryl, arylalkyl, heterocyclyl and heterocyclyl-alkyl, or R3 and R4, taken together with the nitrogen atom to which they are bonded, may form an optionally substituted 5 to 7 membered heterocyclyl group optionally containing one additional heteroatom selected from N, O and S; R5 is an optionally substituted aryl; R6 is hydrogen, an optionally substituted straight or branched C1-C6 alkyl or NR8R9, wherein: R8 and R9 are independently hydrogen or an optionally substituted group selected from straight or branched C1-C6 alkyl, C3-C7 cycloalkyl, cycloalkyl-alkyl, heterocyclyl and heterocyclyl-alkyl, or R8 and R9, taken together with the nitrogen atom to which they are bonded, may form an optionally substituted 5 to 7 membered heterocyclyl group optionally containing one additional heteroatom selected from N, O and S; or a pharmaceutically acceptable salt thereof.