发明名称 Antifungal 5,6-dihydro-4-[(difluoroethyl)phenyl]-4<i>H</i>-pyrrolo[1,2-α][1,4]benzodiazepine and 4-(difluoroethyl)phenyl-6<i>H</i>-pyrrolo[1,2-α][1,4]benzodiazepine derivatives
摘要 The present invention concerns novel compounds of Formula (I):; wherein R1, R2, R3, R4, R5 and R6 have the meaning defined in the claims. The compounds according to the present invention are active mainly against dermatophytes and systemic fungal infections. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
申请公布号 US9637490(B2) 申请公布日期 2017.05.02
申请号 US201113702361 申请日期 2011.06.01
申请人 Janssen Pharmaceutica NV 发明人 Meerpoel Lieven;Maes Louis Jules Roger Marie;de Wit Kelly
分类号 C07D487/12;A61K31/55;C07D487/04 主分类号 C07D487/12
代理机构 代理人 Dodd Thomas J.
主权项 1. A compound of Formula (I) or a stereoisomeric form thereof, wherein R1 is hydrogen, chloro or fluoro; R2 is hydrogen, chloro, fluoro or methyl; R3 and R4 are hydrogen; or R3 and R4 taken together form a bond; R5 is 1,1-difluoroethyl, and R6 is hydrogen or fluoro; or R5 is hydrogen or fluoro, and R6 is 1,1-difluoroethyl; or a pharmaceutically acceptable addition salt or a solvate thereof.
地址 Beerse BE