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Pyrazole [, 1,5-a] derivatives as JAK inhibitors
专利权人:
Pfizer Inc.
发明人:
HAYWARD, Matthew Merrill,BROWN, Matthew Frank,WRIGHT, Stephen Wayne,FENSOME, Andrew,XING, Li Huang,DERMENCI, Alpay,GERSTENBERGER, Brian Stephen,OWEN, Dafydd Rhys,YANG, Xiaojing
申请号:
MA43668
公开号:
MA43668B1
申请日:
2017.02.10
申请国别(地区):
MA
年份:
2020
代理人:
摘要:
The invention relates to structural compounds(R and R can be independently h, amino, nr7cor6, cor6, cor7 R8, C1-C6 alkyl or hydroxyl group ("C1-C6 alkyl"),However, R may or may not exist, and exist in the place allowed by Valencia rules, and no more than one a, a and a or O or C group = O;R0 and R are independent of H, Br, Cl, f or C1 to C6 alkyl groups;R1 is an H, C1-C6 alkyl group, or a hydroxyl group ("C1-C6 alkyl");R2 was selected from group H, c1-c6alkyl, c1-c6alkoxy, hydroxyl ("c1-c6alkyl"),Phenyl (- C1-C6 alkyl)1. Formyl, heteroaryl, heterocyclic, - cor6, - ocor6, - coor6, - coor6, - conr7r8, and - (CH2)1. Each of the above alkyl, cycloalkyl, heterocyclic or heteroaryl groups may not be substituted or substituted by C1-C6 of halogenated, cyano, hydroxyl or alkyl groups;X is a c-r3 or N group, where R3 may be an H or C1-C6 alkyl group;R4 and R5 are independent of H, amino, C1-C6 alkyl or hydroxyl group ("C1-C6 alkyl");R6, R7 and R8 are h, c1-c6alkyl, C1-C4 alkoxy ("C1-C6 alkyl"), respectively,Or C3 to C8 cycloalkanes, the C1 to C6 alkyl groups are selectively substituted by halogenated, CN or hydroxyl groups;where?R7 and R8, together with their related atoms, form a cycle of 5 or 6 chains, which are selectively replaced by halogen, hydroxyl group, CN or alkyl group (C1-C6).And, N, values 0, 1, 2 or 3. Methods for treating Janus kinase inhibitors and pharmaceutical compositions containing the compounds of the invention and combinations with other therapeutic agents are also disclosed.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 indépendamment o, c=o, c-r' ou n-r'', où r' et r'' peuvent indépendamment être h, un groupe amino, -nr7cor6, cor6, -conr7r8, un groupe alkyle en c1 à c6, ou un groupe hydroxy(alkyle en c1 à c6), et r'' peut être présent ou absent, et est présent où les règles de valence
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