New pyrazole substituted pyridine compound, useful as an inhibiting agent for a reaction catalyzed by a kinase e.g. focal adhesion kinase

摘要

Pyrazole substituted pyridine compound (I) is new. Pyrazole substituted pyridine compound of formula (I) is new. A, Ar1 : aryl, heteroaryl or cycloalkyl (all optionally substituted); L : CO, NH, CO-NH, NH-CO, NH-SO, NH-SO2, SO2NH, NH-CH2, CH2-NH, CH2-CO-NH, NH-CO-CH2, NH-CH2-CO, CO-CH2-NH, NH-CO-NH, NH-CS-NH, NH-CO-O or O-CO-NH; X, Y1 : NR, NO or C(R5); R5, R6 : H, halo, R2, CN, O(R2), OC(O)(R2), OC(O)NR(R2)(R3), OS(O2)(R2), NR(R2)(R3), N=C(R2)(R3), N(R2)C(O)(R3), N(R2)C(O)O(R3), N(R4)C(O)N(R2)(R3), N(R4)C(S)N(R2)(R3), N(R2)S(O2)(R3), C(O)(R2), C(O)O(R2), C(O)NR(R2)(R3), C(=N (R3))(R2), C(=N (OR3))(R2), S(R2), S(O)(R2), S(O2)(R2), S(O2)O(R2) or S(O2)NR(R2)(R3); and R2-R4 : H, alkyl, alkylene, alkynyl, (hetero)aryl, cycloalkyl or heterocyclyl (all optionally substituted). Provided that R2 and R3 are present on one of R5 and R6 at the same time and can be dependent between them to form a cycle. [Image] ACTIVITY : Cytostatic. MECHANISM OF ACTION : Kinase inhibitor. The ability of (I) to inhibit focal adhesion kinase was tested in vitro. The results showed that (I) has a median inhibitory concentration value of 264 nm.