Han, Bo,Buettelmann, Bernd,Knust, Henner,Thomas, Andrew,Koblet, Andreas
申请号：
AU2006328602
公开号：
AU2006328602B2
申请日:
2006.12.13
申请国别(地区):
AU
年份:
2012
代理人:
摘要：
The present invention is concerned with isoxazol-4-yl-oxadiazole derivativesof formula (I) wherein R is hydrogen, halogen, aryl, heterocyclyl,heteroaryl, cyano, lower alkyl, -(CH)-cycloalkyl,-(CH)-N(R), -(CH)-O-loweralkyl or -(CH)-OH； n is 0,1 or 2 R is hydrogen or lower alkyl；R is cycloalkyl, aryl, heteroaryl or heterocyclyl, which are optionallysubstituted by one or more substituents, selected from the group consistingof halogen, cyano, nitro, lower alkyl, lower alkoxy, lower alkoxy substitutedby halogen, lower alkyl substituted by halogen, C(O)O-lower alkyl, lower alkylsulfonyl,-NRR, -C(O)-NRR, -C(O)-heterocyclyl,benzyloxy, heterocyclyl optionally substituted by hydroxy, halogen or loweralkyl, or is heteroaryl optionally substituted by lower alkyl； Rand R are independently hydrogen, lower alkylsulfonyl, -C(O)H,-(CH)-N(R), -(CH)-O-loweralkyl, -(CH)-S-lower alkyl, -(CH)-S(O)-loweralkyl, heteroarylsulfonyl, lower alkyl, -(CH2)n-heterocyclyl, optionallysubstituted by lower alkyl, or is -(CH)-cycloalkyl,-(CH)-heteroaryl, -(CH)-OH,-(CO)-R', wherein R' is lower alkyl, cycloalkyl or heteroaryl； Ris aryl or heteroaryl, which are optionally substituted by halogen or lower alkylsubstituted by halogen； as well as pharmaceutically acceptable acid additionsalts thereof. It has been found that this class of compounds show high affinityand selectivity for GABA α5 receptor binding sites and might be usefulas cognitive enhancer or for the treatment of cognitive disorders like Alzheimer'sdisease.
