COE Jotham Wadswort,DEHNHARDT Christoph Martin,JONES Peter,SABNIS Yogesh Anil,STROHBACH Joseph Walter,WAKENHUT Florian Michel,WHITLOCK Gavin Alistair
申请号：
MD20160121
公开号：
MD20160121A2
申请日:
2015.04.30
申请国别(地区):
MD
年份:
2017
代理人:
摘要：
The invention relates to a compound having the structure (I):(I)or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate of said compound or pharmaceutically acceptable salt, wherein A and A′ are independently C or N, where C may be unsubstituted or substituted by halo or C1-C6 alkyl； R and R0 are independently selected from the group consisting of H, C1-C6 alkyl, hydroxy(C1-C6 alkyl), phenyl(C1-C6 alkyl), and -(CH2)n-W, where W is C3-C8 cycloalkyl, phenyl, naphthyl, 5- or 6-membered heteroaryl or heterocycle containing 1...3 N, S and/or O atoms, -SO2-R′, -NHSO2-R′, -NR″SO2-R′ and SR′, where R′ and R″ are independently C1-C6 alkyl or C3-C8 cycloalkyl, etc.； wherein each of said alkyl, cycloalkyl, heterocycle, phenyl, naphthyl or heteroaryl may be unsubstituted or substituted by phenyl, heteroaryl, etc.； or, R and R0 and the N atom to which they are bonded together form a monocyclic or bicyclic heterocyclic ring which may be unsubstituted or substituted by (a) halo, hydroxy, heteroaryl, C1-C6 alkyl, C1-C6 alcoxy, etc.； or (b) -(CH2)n-W, where W is C3-C8 cycloalkyl, phenyl, etc.； R1 is H, halo or cyano； R2 and R2′ are independently H, C1-C6 alkyl, cyano, C1-C6 alcoxy, C1-C6 alkylthio, or C3-C8 cycloalkyl where alkyl, alcoxy, or cycloalkyl is optionally substituted by one or more fluorine atoms； X is a bond, -CO-, -CONH-, -SO2-, -SONH-, or -(CH2)m-； R3 is H, C1-C4 alkyl, phenyl, naphthyl, 5- or 6-membered heteroaryl or heterocycle containing 1…3 N atoms, a 5-membered heteroaryl or heterocycle, etc., or (c) 2 O or S atoms and 0…2 N atoms； wherein each of said phenyl, naphthyl, heteroaryl or heterocycle is optionally substituted by alkyl, 1 substituent -Y-R4 and/or 1…4 substituents each independently selected from R5； with the proviso that when X is -CO- or -SO2-, R3 is not H； Y is a bond, -(CH2)m- or -O-； R4 is (a) H, C1-C6 alkyl, C3-C8 cycloalkyl, halo, oxo, -OR6, -NR7R8, -SR6, -SOR9, -SO2R9, -COR6, -OCOR6, -COOR6, -NR6COR6, -CONR7R8, etc
