TASLER STEFAN,BAUMGARTNER ROLAND,SAEB WAEL,CHEVRIER CARINE,LEBAN JOHANN
申请号：
NZ61359212
公开号：
NZ613592A
申请日:
2012.01.27
申请国别(地区):
NZ
年份:
2015
代理人:
摘要：
The present disclosure relates to pyrazolyl isoxazole compounds of the general formula (I), and the pharmaceutically acceptable salt or solvate thereof, as anti-inflammatory and immunomodulatory agents. These compounds act as inhibitors of IL17 and IFN-gamma. The conditions that may be treated by the present compounds include: psoriasis, psoriatric arthritis, autoimmune thyroiditis, Grave&rsquos disease, rheumatoid arthritis, vitiligo, Crohn&rsquos disease, ulcerative colitis, inflammatory bowel disease, ankylosing spondylitis, diabetes type I, multiple sclerosis, celiac disease, systemic lupus erythematosus, uveitis, Behcet disease, atopic dermatitis, Lichen planus, Sjogren&rsquos syndrome, spinal disc herniation, acne, Graft-versus-Host-Reaction, Host-versus-Graft-Reaction and osteoarthritis. Compounds of the disclosure include: methyl 3-(2-chloro-6-fluorophenyl)-5-(1-(2-fluorophenyl)-5-(trifluoromethyl)-1H-pyrazol-4-yl)isoxazole-4-carboxylate, (3-(2-chloro-6-fluorophenyl)-5-(1-(2-fluorophenyl )-5-(trifluoromethyl)-1H-pyrazol-4-yl)isoxazol-4-yl)(piperidin-1-yl)methanone, (3-(2-chloro-6-fluorophenyl)-5-(1-(3-fluorophenyl)-5-( trifluoromethyl)-1H-pyrazol-4-yl)isoxazol-4-yl)(isoxazolidin-2-yl)methanone, S-methyl 3-(2-chloro-6-fluorophenyl)-5-(1-(3-fluorophenyl)-5-(trifluoromethyl)-1H-pyrazol-4-yl)isoxazole-4-carbothioate, and (Z)-methyl N-(3-(2-chloro-6-fluorophenyl)-5-(1-(3 -fluorophenyl)-5-(trifluoromethyl)-1H-pyrazol-4-yl)isoxazol-4-yl)-2,2,2-trifluoroacetimidate.
