申请人:Sterling Winthrop Inc.
公开号:US05290796A1
公开(公告)日:1994-03-01
The invention is related to compounds, being useful in treating psychosis, of the formula: ##STR1## wherein R.sup.1 is lower-alkyl, or phenyl-lower-alkyl; R.sup.2, R.sup.3 and R.sup.4 are the same or different lower-alkyl; n is zero or one; R.sup.5 is hydrogen, lower-alkyl, C.sub.3 -C.sub.7 -monocyclic cycloalkyl, lower-alkoxy, phenyl, phenyl-lower-alkyl, phenyl-lower-alkyl in which the phenyl ring is substituted in the 2, 3, or 4-position by one to two, the same or different, halogen substituents, or R.sup.5 is a 5-membered aromatic monocyclic heterocycle selected from the group consisting of thienyl, furanyl and isoxazolyl; R.sup.6 is hydrogen or lower-alkyl; or when n is zero, R.sup.5 and R.sup.6 together are --(CH.sub.2).sub.m -- wherein m is an integer from four to six; with the proviso that when R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are methyl, n is zero and R.sup.6 is hydrogen or methyl, R.sup.5 cannot be hydrogen; further provided that when n is zero, R.sup.5 cannot be lower-alkoxy, phenyl, or a 5-membered aromatic monocyclic heterocycle, or a pharmaceutically acceptable acid-addition salt thereof.
该发明涉及一类化合物,其公式为:##STR1##其中R.sup.1为低烷基或苯基-低烷基;R.sup.2,R.sup.3和R.sup.4为相同或不同的低烷基;n为零或一;R.sup.5为氢、低烷基、C.sub.3-C.sub.7-单环萜烷基、低烷氧基、苯基、苯基-低烷基、苯基-低烷基,其中苯环在2、3或4位上被一个到两个相同或不同的卤素取代,或R.sup.5是从噻吩基、呋喃基和异噁唑基组成的5-成员芳香单环杂环;R.sup.6为氢或低烷基;或当n为零时,R.sup.5和R.sup.6一起为--(CH.sub.2).sub.m--,其中m为四到六的整数;但是如果R.sup.1,R.sup.2,R.sup.3和R.sup.4为甲基,n为零且R.sup.6为氢或甲基,则R.sup.5不能是氢;进一步地,当n为零时,R.sup.5不能是低烷氧基、苯基或5-成员芳香单环杂环,或其药学上可接受的酸加成盐。