2-PHENYLAMINO-4- (5-PYRAZOLYLAMINO) -PYRAMIDINE DERIVATIVES AS KINASE INHIBITORS, IN PARTICULAR, SRC KINASE INHIBITORS

摘要

The invention provides novel substituted 2,4-diaminopyrimidine compounds (I). In formula (I), the variables are as follows. Y1 represents H or C 1-4 alkyl. Y2 represents CF3, C1-6 alkyl; C3-6 cycloalkyl; or phenyl optionally substituted with halogen, C1-4 alkyl, or C1-4 alkoxy. The subscript n is 0, 1, or 2. X represents halogen or C1-4 alkyl, p is 0, 1, or 2. Z represents halogen, C1-4 alkyl, or C1-4 alkoxy; and q is 0, 1, or 2. L represents a chemical bond; C1-4 alkylene; O; O(C1-4 alkylene); CH(C1-6 alkoxy); S(O)0-2; S(O)0-2(C1-4 alkylene); (C1-4 alkylene)S(O)0-2; NH(C1-4 alkylene); C(O); or C(O)-(C1-4 alkylene). D represents pyridinyl; imidazolyl; thiazolyl; pyrrolyl; thienyl; pyrazolyl; furyl; thiadiazolyl; oxazolyl; or benzimidazolyl. The pyridinyl and benzimidazolyl groups D each may be optionally substituted by up to three substituents independently selected from C1-4 alkyl, OH, C1-4 alkoxy, CN, NR1R2, C(O)NR1R2, halogen, and CO2(C1-6 alkyl), in which R1 and R2 are independently selected from H, C1-4 alkyl, and C3-6 cycloalkyl. Alternatively, R1 and R2 may be joined to form a 5-6 membered saturated heterocycle (II) in which Q represents O, S(O)0-2, N-Y1, or C(Y1)2, pharmaceutical compositions containing them, a method of making them, and methods of using them for treatment of cell proliferative diseases such as cancer, and non-malignant cell proliferative diseases, as well as osteoporosis and inflammatory diseases.