FENSOME, Andrew,GOPALSAMY, Ariamala,GERSTENBERGER, Brian S.,EFREMOV, Ivan Viktorovich,WAN, Zhao-Kui,PIERCE, Betsy,TELLIEZ, Jean-Baptiste,TRUJILLO, John I,ZHANG, Liying,XING, Li,SAIAH, Eddine
申请号：
EP15766627
公开号：
EP3183247B9
申请日:
2015.08.07
申请国别(地区):
EP
年份:
2018
代理人:
摘要：
A compound having the structure: or a pharmaceutically acceptable salt thereof, wherein X is N or CR, where R is hydrogen, deuterium, C1-C4 alkyl, C1-C4 alkoxy, C3-C6 cycloalkyl, aryl, heteroaryl, aryl(C1-C6 alkyl), CN, amino, alkylamino, dialkylamino, CF3, or hydroxyl A is selected from the group consisting of a bond, C&boxHO, &mdashSO2&mdash, &mdash(C&boxHO)NR0&mdash, and &mdash(CRaRb)q&mdash, where R0 is H or C1-C4 alkyl, and Ra and Rb are independently hydrogen, deuterium, C1-C6 alkyl, C3-C6 cycloalkyl, aryl, aryl(C1-C6 alkyl), heteroaryl, (C1-C6 alkyl)heteroaryl, etc. A&prime is selected from the group consisting of a bond, C&boxHO, &mdashSO2&mdash, &mdash(C&boxHO)NR0&prime, &mdashNR0&prime(C&boxHO)&mdash, and &mdash(CRa&primeRb&prime)q&mdash, where R0&prime is H or C1-C4 alkyl, and Ra&prime and Rb&prime are independently hydrogen, deuterium, C1-C6 alkyl, C3-C6 cycloalkyl, aryl, aryl(C1-C6 alkyl), heteroaryl, (C1-C6 alkyl)heteroaryl, heteroaryl(C1-C6 alkyl), and heterocyclic(C1-C6 alkyl) Z is &mdash(CH2)h&mdash or a bond, where one or more methylene units are optionally substituted by one or more C1-C3 alkyl, CN, OH, methoxy, or halo, and where said alkyl may be substituted by one or more fluorine atoms R1 and R1&prime are independently selected from the group consisting of hydrogen, deuterium, C1-C4 alkyl, C3-C6 cycloalkyl, aryl, heteroaryl, aryl(C1-C6 alkyl), CN, etc., wherein said alkyl, aryl, cycloalkyl, heterocyclic, or heteroaryl is further optionally substituted with one or more substituents selected from the group consisting of C1-C6 alkyl, halo, CN, C1-C4 alkylamino, C3-C6 cycloalkyl, etc. R2 is selected from the group consisting of hydrogen, deuterium, C1-C6 alkyl, C3-C6 cycloalkyl, halo, and cyano, where said alkyl may be substituted by one or more fluorine atoms R3 is selected from the group consisting of hydrogen, deuterium, and amino R4 is monocyclic or bicyclic aryl or monocyclic or bicyclic heteroaryl wherein said aryl or heteroaryl is optionall
