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：
IBIB2017/050748
公开号：
WO2017/144995A1
申请日:
2017.02.10
申请国别(地区):
IB
年份:
2017
代理人:
摘要：
A compound compound having the structure (I) 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=0； R0 and R are independently H, Br, CI, 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.La présente invention concerne un composé de structure (I) ou son sel pharmaceutiquement acceptable, ou un solvate pharmaceutiquement acceptable dudit composé ou sel pharmaceutiquement acceptable, A, A' et A'' étant indépendammen
