发明名称 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.
申请公布号 US2014378481(A1) 申请公布日期 2014.12.25
申请号 US201414318149 申请日期 2014.06.27
申请人 Bifulco, JR. Neil;Brooijmans Natasja;Hodous Brian L.;Kim Joseph L.;Miduturu Chandrasekhar V. 发明人 Bifulco, JR. Neil;Brooijmans Natasja;Hodous Brian L.;Kim Joseph L.;Miduturu Chandrasekhar V.
分类号 C07D239/84;A61K31/4375;A61K31/519;A61K31/517;C07D471/04 主分类号 C07D239/84
代理机构 代理人
主权项 1. A method of treating a cancer selected from breast cancer, ovarian cancer, lung cancer, liver cancer, and a sarcoma in a subject, the method comprising administering an effective amount of a compound of Formula I or 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; and Warhead is selected from the group consisting ofwherein X is halo, or triflate; and each of Ra, Rb, and Rc is, independently, H, substituted or unsubstituted C1-4 alkyl, substituted or unsubstituted C1-4 cycloalkyl, or cyano, to thereby treat the cancer.
地址 Sudbury MA US