RAGHAVAN, Subharekha,STELMACH, John E.,SMITH, Cameron J.,LI, Hong,WHITEHEAD, Alan,WADDELL, Sherman T.,CHEN, Yi-Heng,MIAO, Shouwu,ORNOSKI, Olga A.,GARFUNKLE, Joie,LIAO, Xibin,CHANG, Jiang,HAN, Xiaoqing
申请号：
ES11787236
公开号：
ES2564503T3
申请日:
2011.05.24
申请国别(地区):
ES
年份:
2016
代理人:
摘要：
A compound having structural formula I: ** Formula ** or a pharmaceutically acceptable salt thereof, in which ** Formula ** is a heteroaryl selected from ** Formula ** where * indicates binding to the pyrimidinyl ring and * * indicates binding to -CH2-R2 of structural formula I； Each X1, X2, X3 and X4 is independently N or CH, provided that no more than two of X1, X2, X3 and X4 are N； Each RX and RY are independently H, C3-10 cycloalkyl or -C1-C6 alkyl； Each R1 is independently -H, halo, OR, -C1-C6 alkyl, aryl, heterocyclyl, heteroaryl, -C3-10 cycloalkyl, -CN, -NRaC (O) Rb or -C (O) NRaRb, said aryl being, heteroaryl and cycloalkyl optionally substituted with one to three substituents selected from halo, -C1-C6 alkyl, -OR, -CN and -CF3； R2 is - (CRd 2) t-C1-C6 alkyl, -C2-C6 alkenyl, -C2-C6 alkynyl, - (CRd 2) tOR, - (CRd 2) tSR, - (CRd 2) tCF3, - (CRd 2) C3-10 t-cycloalkyl, - (CRd 2) t-aryl, - (CRd 2) t-heterocyclyl or - (CRd 2) t-heteroaryl, said alkyl, cycloalkyl, aryl, heterocyclyl and heteroaryl being optionally substituted with one to three substituents selected from halo, -C1-C6 alkyl, -CF3, -CN or -OR； R3 is - (CRd 2) t-aryl, - (CRd 2) t-heteroaryl, - (CRd 2) t-heterocyclyl, - (CRd 2) C3-10 t-cycloalkyl, - (CRd 2) tCN, - ( CRd 2) tC (O) NRaRb, - (CRd 2) t-NRaC (O) Rb, - (CRd 2) tC (S) NRaRb, - (CRd 2) tC (O) ORa, - (CRd 2) t -NRaC (O) NRb, - (CRd 2) t- NRaC (O) ORa, - (CRd 2) t-NRaRb or -ORa, said aryl, heteroaryl or heterocyclyl are optionally substituted with one to three substituents selected from R5 ； R4 is -C1-C6 alkyl, C3-10 cycloalkyl, halo or CF3； Each R5 is independently halo, OR, CN, - (CRd 2) tCF3, S (O) pRc, - (CRd 2) C3-10 t-cycloalkyl or -C1-C6 alkyl, said alkyl and cycloalkyl being optionally substituted with one to three substituents selected from halo or OR； Each R6 is independently halo, -C1-C6 alkyl, OR, CN, CF3, aryl or heteroaryl, wherein said alkyl, aryl or heteroaryl are optionally substituted with halo, C1-C6 alkyl or CF3； Each R is ind
