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ARYL-ISOXAZOLO-4-YL-OXADIAZOLE DERIVATIVES
专利权人:
发明人:
申请号:
EP06841339.2
公开号:
EP1968972B1
申请日:
2006.12.13
申请国别(地区):
EP
年份:
2012
代理人:
摘要:
The present invention is concerned with isoxazol-4-yl-oxadiazole derivatives of formula (I) wherein R1 is hydrogen, halogen, aryl, heterocyclyl, heteroaryl, cyano, lower alkyl, -(CH2)n-cycloalkyl, -(CH2)n-N(R)2, -(CH2)n-O-lower alkyl or -(CH2)n-OH n is 0,1 or 2 R is hydrogen or lower alkyl R2 is cycloalkyl, aryl, heteroaryl or heterocyclyl, which are optionally substituted by one or more substituents, selected from the group consisting of halogen, cyano, nitro, lower alkyl, lower alkoxy, lower alkoxy substituted by halogen, lower alkyl substituted by halogen, C(O)O-lower alkyl, lower alkylsulfonyl, -NRaRb, -C(O)-NRaRb, -C(O)-heterocyclyl, benzyloxy, heterocyclyl optionally substituted by hydroxy, halogen or lower alkyl, or is heteroaryl optionally substituted by lower alkyl Ra and Rb are independently hydrogen, lower alkylsulfonyl, -C(O)H, -(CH2)n-N(R)2, -(CH2)n-O-lower alkyl, -(CH2)n-S-lower alkyl, -(CH2)n-S(O)2-lower alkyl, heteroarylsulfonyl, lower alkyl, -(CH2)n-heterocyclyl, optionally substituted by lower alkyl, or is -(CH2)n-cycloalkyl, -(CH2)n-heteroaryl, -(CH2)n-OH, -(CO)-R, wherein R is lower alkyl, cycloalkyl or heteroaryl R3 is aryl or heteroaryl, which are optionally substituted by halogen or lower alkyl substituted by halogen as well as pharmaceutically acceptable acid addition salts thereof. It has been found that this class of compounds show high affinity and selectivity for GABA α5 receptor binding sites and might be useful as cognitive enhancer or for the treatment of cognitive disorders like Alzheimers disease.La présente invention concerne des dérivés d’isoxazol-4-yl-oxadiazole de formule (I) dans laquelle R1 représente un hydrogène, un halogène, un aryle, un hétérocyclyle, un hétéroaryle, un cyano, un alkyle inférieur, un -(CH2)n-cycloalkyle, -(CH2)n-N(R)2, un -(CH2)n-O-alkyle inférieur ou -(CH2)n-OH n représente 0, 1 ou 2 R représente un hydrogène ou un alkyle inférieur R2 représente un cycloalkyle, un aryle, un hétéroaryle ou un hétérocycly
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