发明名称 NOVEL PYRAZOL DERIVATIVES
摘要 The invention relates to a compound of formula (I);;wherein A1 to A3 and R1 to R3 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
申请公布号 US2017035769(A1) 申请公布日期 2017.02.09
申请号 US201615332398 申请日期 2016.10.24
申请人 Hoffmann-La Roche Inc. 发明人 GRETHER UWE;KIMBARA ATSUSHI;NETTEKOVEN MATTHIAS;RICKLIN FABIENNE;ROEVER STEPHAN;ROGERS-EVANS MARK;SCHULZ-GASCH TANJA
分类号 A61K31/519 主分类号 A61K31/519
代理机构 代理人
主权项 1. A method for the treatment of pain, atherosclerosis, age-related macular degeneration, diabetic retinopathy, glaucoma, retinal vein occlusion, retinopathy of prematurity, ocular ischemic syndrome, geographic atrophy, diabetes mellitus, inflammation, inflammatory bowel disease, ischemia-reperfusion injury, acute liver failure, liver fibrosis, lung fibrosis, kidney fibrosis, systemic fibrosis, acute allograft rejection, chronic allograft nephropathy, diabetic nephropathy, glomerulonephropathy, cardiomyopathy, heart failure, myocardial ischemia, myocardial infarction, systemic sclerosis, thermal injury, burning, hypertrophic scars, keloids, gingivitis pyrexia, liver cirrhosis or tumors, regulation of bone mass, amyotrophic lateral sclerosis, multiple sclerosis, Alzheimer's disease, Parkinson'sdisease, stroke, transient ischemic attack or uveitis, which method comprises administering to a patient in need thereof an effective amount of a compound of formula (I) wherein A1 is CH or N; A2 is CH or N; A3 is —(CH2)n— or —CH2C(O)—; R1 is alkyl, cycloalkyl, alkoxy or halogen; R2 is substituted pyrrolidinyl or substituted dihydropyrrolyl, wherein substituted pyrrolidinyl and substituted dihydropyrrolyl are pyrrolidinyl and dihydropyrrolyl substituted with one or two substituents independently selected from halogen, hydroxyl, hydroxyalkyl, alkoxyalkyl and alkylfurazanylalkoxy; R3 is phenyl, substituted phenyl, substituted furazanyl, pyridinyl, substituted pyridinyl, dioxothietanyl, tetrahydrofuranyl, substituted tetrazolyl or substituted triazolyl, wherein substituted phenyl, substituted furazanyl, substituted pyridinyl and substituted triazolyl are phenyl, pyridinyl and triazolyl substituted with one or two substituents independently selected from alkyl, alkoxy, halogen, haloalkyl, alkylsulfonyl and cycloalkyl, and wherein substituted tetrazolyl and substituted furazanyl are tetrazolyl and furazanyl substituted with one substituent selected from alkyl, alkoxy, halogen, haloalkyl, alkylsulfonyl and cycloalkyl; n is 0, 1 or 2; provided that A1 and A2 are not both CH at the same time; or a pharmaceutically acceptable salt or ester thereof.
地址 Little Falls NJ US