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.
本发明涉及一种新型PDE-IV抑制剂,其化学式为:##STR1## 其中:R1=氢、C1-C6烷基;R2=C3-C7烷基、C3-C7环烷基或C4-C8环烷基亚甲基,当Y为CH时;##STR2## R4=氢、OR5、NHR5、NHOH、NHNH2或##STR3## R5=氢、C1-C6烷基、C3-C8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=CH2、O、S或NH;Y=CH2、CH、O、S或NH;Q=键或CH=CH;n=0、1、2、3或4;M=O、NOH或H2;Z=氢或卤素;或其药学上可接受的盐,作为抗哮喘剂。