申请人:Hoffmann-La Roche Inc.
公开号:US05318967A1
公开(公告)日:1994-06-07
The invention relates to cis-2,3,3a,4,5,9b-Hexahydro-1H-benzo[b]indole derivatives of the formula ##STR1## wherein R.sup.1 is a residue of the formula --O--CO--NR.sup.4 R.sup.5, R.sup.2 is lower alkyl, lower cycloalkyl or lower alkyl substituted by lower cycloalkyl, aryl, aroyl, aroylamino, amino or by a cyclic amino, amide or imide group, R.sup.3 is hydrogen or lower alkyl, R.sup.4 is lower alkyl and R.sup.5 is hydrogen or lower alkyl, the corresponding trans isomers or cis-trans isomeric mixtures and pharmaceutically acceptable salts thereof. These compounds and salts are especially suitable for the treatment or prophylaxis of cognitive disorders and senile dementia particularly, Alzheimer's disease, and for the improvement of memory capacity.
本发明涉及式为##STR1##的cis-2,3,3a,4,5,9b-六氢-1H-苯并[b]吲哚衍生物,其中R.sup.1是公式--O--CO--NR.sup.4 R.sup.5的残基,R.sup.2是较低的烷基,较低的环烷基或较低的烷基,其被较低的环烷基,芳基,芳基酰基,芳基氨基,氨基或环状氨基,酰胺或酰亚胺基所取代,R.sup.3是氢或较低的烷基,R.sup.4是较低的烷基,R.sup.5是氢或较低的烷基,对应的顺式异构体或顺反异构体混合物及其药学上可接受的盐。这些化合物和盐特别适用于治疗或预防认知障碍和老年性痴呆症,尤其是阿尔茨海默病,并用于提高记忆能力。