申请人:American Home Products Corporation
公开号:US05459151A1
公开(公告)日:1995-10-17
This invention relates to novel PDE-IV inhibitors having the formula: ##STR1## where: R.sup.1 =H, C.sub.1 -C.sub.6 alkyl; R.sup.2 =C.sub.3 -C.sub.7 alkyl, C.sub.3 -C.sub.7 cycloalkyl or C.sub.4 -C.sub.8 cycloalkylidene when Y is CH; ##STR2## R.sup.4 =H, OR.sup.5, NHR.sup.5, NHOH, NHNH.sub.2 or ##STR3## R.sup.5 =H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.8 cycloalkyl, aryl, substituted aryl, aralkyl, substituted aralkyl or ##STR4## W=N or CH; X=CH.sub.2, O, S, or NH; Y=CH.sub.2, CH, O, S, or NH; Q=a bond or CH.dbd.CH; n=0, 1, 2, 3 or 4; M=O, NOH or H.sub.2 ; Z=H or halogen; or a pharmaceutically acceptable salt thereof, as antiasthmatic agents.
本发明涉及具有以下式子的新型PDE-IV抑制剂:##STR1## 其中:R.sup.1 =氢,C.sub.1-C.sub.6烷基;R.sup.2 =C.sub.3-C.sub.7烷基,C.sub.3-C.sub.7环烷基或C.sub.4-C.sub.8环烷基亚甲基,当Y为CH时;##STR2## R.sup.4 =氢,OR.sup.5,NHR.sup.5,NHOH,NHNH.sub.2或##STR3## R.sup.5 =氢,C.sub.1-C.sub.6烷基,C.sub.3-C.sub.8环烷基,芳基,取代芳基,芳基烷基,取代芳基烷基或##STR4## W=N或CH;X=CH.sub.2,O,S或NH;Y=CH.sub.2,CH,O,S或NH;Q=键或CH.dbd.CH;n=0,1,2,3或4;M=O,NOH或H.sub.2;Z=氢或卤素;或其药学上可接受的盐,作为抗哮喘剂。