INHIBITORS OF THE FIBROBLAST GROWTH FACTOR RECEPTOR

摘要

Described herein are inhibitors of FGFR, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions to inhibit the activity of tyrosine kinases.

主权项

1. A compound of Formula I, or a pharmaceutically acceptable salt thereof:wherein:
Ring A is a 3-8 membered aryl, heteroaryl, heterocyclic or alicyclic group; X is CH or N; Y is CH or N—R4 where R4 is H or C1-6 alkyl; L is —[C(R5)(R6)]q—, where each of R5 and R6 is, independently, H or C1-6 alkyl; wherein q is 0-4; each of R1 and R3 is, independently, halo, cyano, optionally substituted C1-6 alkoxy, hydroxy, oxo, amino, amido, alkyl urea, optionally substituted C1-6 alkyl, optionally substituted C1-6 heterocyclyl; two R2 are halo and two R2 are C1-6 alkoxy; m is 0-3; n is 4; p is 0-2; andWarhead is selected from:wherein X is a leaving group selected from halo and triflate; and each of Ra, Rb, and Rc is, independently, H; substituted or unsubstituted C1-4 alkyl; or substituted or unsubstituted C1-4 cycloalkyl.