Knust, Henner,Buettelmann, Bernd,Thomas, Andrew,Han, Bo
申请号：
AU2006331437
公开号：
AU2006331437B2
申请日:
2006.12.14
申请国别(地区):
AU
年份:
2012
代理人:
摘要：
The present invention is concerned with aryl-isoxazol-4-yl-imidazole derivativesof formula (I), wherein R to R are each independently hydrogenor halogen； R is hydrogen, lower alkyl, cycloalkyl, -(CH)-O-loweralkyl or lower alkyl substituted by hydroxy； R is -(CH)-arylor -(CH)-heteroaryl which are optionally substitutedby one or more substituents selected from the group consisting of halogen, cyano,nitro, lower alkyl, lower alkoxy, lower alkylsulfanyl, lower alkyl substitutedby halogen, -C(O)-lower alkyl, -C(O)-O-lower alkyl, -NH-C(O)-O-lower alkylor -C(O)-NH-R', wherein R' is lower alkynyl or lower alkyl substitutedby halogen, or is -(CH)-cycloalkyl, -(CH)-heterocyclyl,-(CH)-heteroaryl or -(CH)-aryl,optionally substituted by halogen； R is hydrogen, -C(O)H, -(CH)-O-loweralkyl, -C(O)O-lower alkyl, lower alkyl substituted by hydroxy or halogen, oris cycloalkyl, aryl, or is -(CH)-O-CH-aryl,optionally substituted by halogen or lower alkyl, or is -(CH)-O-CH-heteroaryl,optionally substituted by halogen, lower alkyl or lower alkyl substituted byhalogen, or is -(CH)-NH-(CH)-heterocyclyl；n is 0, 1, 2 or 3 m is 0 or 1； o is 1, 2 or 3； as well as with pharmaceutically acceptableacid addition salts thereof. It has been found that this class of compounds showhigh affinity and selectivity for GABA A α5 receptor binding sites andmight be useful as cognitive enhancer or for the treatment of cognitive disorderslike Alzheimer's disease.
