BROWN, MATTHEW FRANK,布朗 马休,布朗 馬休,DERMENCI, ALPAY,德门西 阿尔佩,德門西 阿爾佩,FENSOME, ANDREW,费森 安德鲁,費森 安德魯,GERSTENBERGER, BRIAN STEPHEN,格坦柏格 布莱恩,格坦柏格 布萊恩,HAYWARD, MATTHEW MERRILL,海瓦 马修,海瓦 馬修,OWEN, DAFYDD RHYS,欧文 ,布朗 马休,布朗 馬休,德门西 阿尔佩,德門西 阿爾佩,费森 安德鲁,費森 安德魯,格坦柏格 布莱恩,格坦柏格 布萊恩,海瓦 马修,海瓦 馬修,欧文
申请号：
TW106105777
公开号：
TW201741313A
申请日:
2017.02.21
申请国别(地区):
TW
年份:
2017
代理人:
摘要：
A compound compound having the structure: 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.本發明係有關一種具有下列結構之化合物：或其藥學上可接受的鹽、或該化合物或藥學上可接受的鹽之藥學上可接受的溶劑合物，其中A、A’和A”獨立地為O、C=O、C-R’或N-R”，其中R’和R”可獨立地為H、胺基、-NR7COR6、-COR6、-CONR7R8、C1-C6烷基、或羥基(C1-C6烷基)，且R”可存在或不存在，且當存在時符合價數原則，及A、A’和A”中不超過一者是O或C=O；R0和R獨立地為H、Br、Cl、F、或C1-C6烷基；R1是H、C1-C6烷基、或
