Pyrazolo-quinazolines

摘要

The present invention relates to pyrazolo-quinazolines, characterized by an ortho-substituted-arylamino, heterocyclylamino- or C3-C7 cycloalkylamino residue at 8 position and an aryl, heterocyclyl or C3-C7 cycloalkyl as substituent of a carboxamide at 3 position of the molecule framework. The compounds of this invention modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular MPS1/TTK. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds.

主权项

1. A compound of formula (I): wherein: R1 is an ortho-substituted-aryl group or a heterocyclyl or C3-C7 cycloalkyl group; R2 is hydrogen atom or a straight or branched C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C7 cycloalkyl or heterocyclyl group; R3 is aryl; R4 is hydrogen atom, hydroxyl or C1-C6 alkyl group, which group may be optionally cyclized together with one of the atom of the group which R3 may represent so as to form a fused C4-C7 cyclic group; R5 and R6: are each independently hydrogen atom, C1-C6 alkyl, or are optionally cyclized together with the carbon atom to which they are bonded so as to form a C3-C7 cycloalkyl group; wherein the groups ortho-substituted-aryl, aryl, heterocyclyl, C3-C7 cycloalkyl, C4-C7 cycloalkyl, C1-C6 alkyl, C2-C6 alkenyl and C2-C6 alkynyl may be optionally (further) substituted; and the pharmaceutically acceptable salts thereof.