6,7,8,9-Tetrahydro-3H-benz(e)indolamine derivatives, processes for their preparation and intermediates used therein, and pharmaceutical compositions containing the indolamine derivatives
申请人:AYERST, MCKENNA AND HARRISON INC.
公开号:EP0055043A2
公开(公告)日:1982-06-30
The invention concerns compounds of the formula
in which R1, R2 and R3 each is hydrogen or lower alkyl having 1 to 5 carbon atoms, and one of R4 and R5 is hydrogen and the other is NR6R7 wherein R6 and R7 each is hydrogen or lower alkyl having 1 to 5 carbon atoms, therapeutically acceptable acid addition salts thereof, processes for their preparation, methods of using the compounds and pharmaceutical compositions. The compounds exhibit dopamine-receptor stimulating activity in a mammal and are useful for treating hyperprolactinemia, glactorrhea, amenorrhea, impotence, Parkinsonism, diabetes, acromegaly, hypertension and other central nervous system disorders. Also disclosed are 6,7,8,9-tetra- hydro-3H-benz[e]indolamine-1,2-dione derivatives; 1,2,3,4-tetrahydronaphthalenediamine derivatives and 1,2,3,4,5,8-hexahydro-6-methoxy-naphthaleneamine derivatives which are useful as intermediates.
本发明涉及式如下的化合物
其中R1、R2和R3各自为氢或具有1至5个碳原子的低级烷基,R4和R5中的一个为氢,另一个为NR6R7(其中R6和R7各自为氢或具有1至5个碳原子的低级烷基),其治疗上可接受的酸加成盐,其制备工艺,化合物的使用方法和药物组合物。这些化合物在哺乳动物体内具有
多巴胺受体刺激活性,可用于治疗高
催乳素血症、泌乳素血症、闭经、阳痿、帕
金森氏症、糖尿病、肢端肥大症、高血压和其他中枢神经系统疾病。还公开了 6,7,8,9-四氢-3H-苯并[e]
吲哚胺-1,2-二酮衍
生物;
1,2,3,4-四氢萘二胺衍
生物和 1,2,3,4,5,8-六氢-6-甲氧基
萘胺衍
生物,这些衍
生物可用作中间体。