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：
SG11201806307Y
公开号：
SG11201806307YA
申请日:
2017.02.10
申请国别(地区):
SG
年份:
2018
代理人:
摘要：
or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate of said compound or pharmaceutically acceptable salt, wherein A, A′ and A″ are independently O, C═O, C—R′ or N—R″, where R′ and R″ may independently be H, amino, —NR7COR6, COR6, —CONR7R8, C1-C6 alkyl, or hydroxy(C1-C6 alkyl), and R″ may be present or absent, and is present where the rules of valency permit, and where not more than one of A, A′ and A″ is O or C═O； R0 and R are independently H, Br, Cl, F, or C1-C6 alkyl； R1 is H, C1-C6 alkyl, or hydroxy(C1-C6 alkyl)； R2 is selected from the group consisting of H, C1-C6 alkyl, C1-C6 alkoxy, hydroxy(C1-C6 alkyl), phenyl(C1-C6 alkyl), formyl, heteroaryl, heterocyclic, —COR6, —OCOR6, —COOR6, —NR7COR6, —CONR7R8, and —(CH2)n—W, where W is cyano, hydroxy, C3-C8 cycloalkyl, —SO2NR7R8, and —SO2—R9, where R9 is C1-C6 alkyl, C3-C8 cycloalkyl, heteroaryl, or heterocyclic； wherein each of said alkyl, cycloalkyl, heterocyclic, or heteroaryl may be unsubstituted or substituted by halo, cyano, hydroxy, or C1-C6 alkyl； X is C—R3 or N, where R3 may be H or C1-C6 alkyl； R4 and R5 are independently H, amino, C1-C6 alkyl, or hydroxy(C1-C6 alkyl)； R6, R7 and R8 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 R8 together with the atom bonded thereto form a 5- or 6-membered ring, said ring being optionally substituted by halo, hydroxy, CN, or C1-C6 alkyl； and, n is 0, 1, 2 or 3. Also provided are methods of treatment as Janus Kinase inhibitors and pharmaceutical compositions containing the compounds of the invention and combinations thereof with other therapeutic agents.
