BROWN, MATTHEW FRANK,DERMENCI, ALPAY,FENSOME, ANDREW,GERSTENBERGER, BRIAN STEPHEN,HAYWARD, MATTHEW MERRILL,OWEN, DAFYDD RHYS,WRIGHT, STEPHEN WAYNE,XING, LI HUANG,YANG, XIAOJING
申请号：
CA2958490
公开号：
CA2958490A1
申请日:
2017.02.21
申请国别(地区):
CA
年份:
2017
代理人:
摘要：
A compound having the structure:or a pharmaceutically acceptable salt thereof, or a pharmaceuticallyacceptable solvate of saidcompound or pharmaceutically acceptable salt, wherein. A, A' and A" areindependently O, C-R' or N-R", where R' and R" may independently be H, amino, -NR7COR6, COR6, -CONR7R8,C1-C6 alkyl, orhydroxy(C1-C6 alkyl)-, and R" may be present or absent, and is present wherethe rules of valencypermit, and where not more than one of A, A' and A" is O； R0 and R areindependently H, Br, CI, F, orC1-C6 alkyl, R1 is H, Cl-C6 alkyl, or hydroxy(C1-C6 alkyl)-； R2 is selectedfrom the group consisting ofH, C1-C6 alkyl-, C1-C6 alkoxy-, hydroxy(C1-C6 alkyl)-, phenyl(C1-C6 alkyl)-,formyl, heteroaryl,heterocyclic, -COR6, -OCOR6, -COOR6, -NR7COR6, CONR7R6, and -(CH2),-,-W, whereW is cyano,hydroxy, C3-C8 cycloalkyl, -SO2NR7R8, and -S02-R9, where R9 is C1-C6 alkyl, C3-C8 cycloalkyl,heteroaryl, or heterocyclic； wherein each of said alkyl, cycloalkyl,heterocyclic, or heteroaryl may beunsubstituted or substituted by halo, cyano, hydroxy, or C1-C6 alkyl, X is C-R3 or N, where R3 may beH or C1-C6 alkyl； R4 and R5 are independently H, amino, C1-C6 alkyl, orhydroxy(C1-C6 alkyl)-； R6, R7and R5 are each independently H, C1-C6 alkyl, C1-C4 alkoxy(C1-C6 alkyl) or C3-C8 cycloalkyl, said C1-C6 alkyl is optionally substituted by halo, CN or hydroxy, or, R7 and R8together with the atom bondedthereto form a 5- or 6-membered ring, said ring being optionally substitutedby halo, hydroxy, CN, orC1-C6 alkyl； and, n is 0, 1, 2 or 3. Also provided is a use of a compound ofthe invention as a TYK2inhibitor.
