Substituted indoles as central nervous system agents

Claim 1

A compound of Formula I: ##STR46## wherein R is ##STR47## wherein R 4 is aryl, unsubstituted or substituted by one to four substituents selected from lower alkyl, lower alkoxy, lower thioalkoxy, hydroxy, lower acyloxy, amino, ##STR48## wherein R 5 is lower alkyl, halogen, or trifluoromethyl, 2-k 3-, or 4-pyridinyl, unsubstituted or substituted by halogen, lower alkyl, hydroxy, lower acyloxy, lower alkoxy, amino, or ##STR49## wherein R 5 is as defined above, 2-, 4-, or 5-pyrimidinyl, unsubstituted or substituted by halogen, lower alkyl, hydroxy, lower acyloxy, lower alkoxy, amino, or ##STR50## wherein R 5 is as defined above, 2-pyrazinyl, unsubstituted or substituted by halogen, lower alkyl, hydroxy, lower acyloxy, lower alkoxy, amino, or ##STR51## wherein R 5 is as defined above, 2- or 3-furanyl, unsubstituted or substituted by halogen, lower alkyl, hydroxy, lower acyloxy, lower alkoxy, amino, or ##STR52## wherein R 5 is as defined above, 2-, or 3-thienyl, unsubstituted or substituted by halogen, lower alkyl, hydroxy, lower acyloxy, lower alkoxy, amino, or ##STR53## wherein R 5 is as defined above, 2-, 4-, or 5-imidazolyl, unsubstituted or substituted by halogen, lower alkyl, hydroxy, lower acyloxy, lower alkoxy, amino, or ##STR54## wherein R 5 is as defined above, 2-, 4-, or 5-thiazolyl, unsubstituted or substituted by halogen, lower alkyl, hydroxy, lower acyloxy, lower alkoxy, amino, or ##STR55## wherein R 5 is as defined above, or 2-, 3-, 4-, 5-, 6-, or 7-indolyl, unsubstituted or substituted by halogen, lower alkyl, hydroxy, lower acyloxy, lower alkoxy, amino, or ##STR56## wherein R 5 is as defined above; R 1 is hydrogen, --CN, or --CO 2 H; R 2 is hydrogen, lower alkyl, or cycloalkyl; R 3 is hydrogen, halogen, hydroxyl, lower alkoxy, lower alkyl, ##STR57## wherein R 6 is hydrogen or lower alkyl, ##STR58## wherein R 7 is hydrogen, lower alkyl, cycloalkyl, or aryl, unsubstituted or substituted by one to four substituents selected from lower alkyl, lower alkoxy, lower thioalkoxy, hydroxy, lower acyloxy, amino, ##STR59## wherein R 5 is as defined above, halogen, or trifluoromethyl, ##STR60## wherein R 8 is lower alkyl, cycloalkyl or aryl, unsubstituted or substituted by one to four substituents selected from lower alkyl, lower alkoxy, lower thioalkoxy, hydroxy, lower acyloxy, amino, ##STR61## wherein R 5 is as defined above, halogen, or trifluoromethyl, or --NH 2 ; n is zero or an integer of 1, 2, or 3; is a single or double bond; and corresponding geometric isomers thereof; or a pharmaceutically acceptable acid or base addition salt thereof.