The present invention relates to compounds of the formula ##STR1## wherein X is --O-- or --CH.sub.2 --; Y is --C(O)--, --(CH.sub.2).sub.n -- or --N(CH.sub.3)--; n is 1 or 2 or X and Y taken together are --CH.dbd.CH-- Z is --NH--, --CH.sub.2 --, --O-- or .dbd.CH--; A.sup.1 is a group ##STR2## B is --(CH.sub.2).sub.m --; m is 0, 1 or 2; R.sup.1 and R.sup.2 are each independently hydrogen or lower alkyl; R.sup.3 is hydrogen or halogen; R.sup.4 is hydrogen or hydroxy and the dotted line is (--CH.sub.2 --CH.sub.2 --).sub.n, and n' is 0 or 1 and to pharmaceutically acceptable acid addition salts thereof. The compounds of the present invention are antagonists of the OFQ receptor. Consequently they will be useful in the treatment of memory and attention deficits, psychiatric, neurological and physiological disorders, especially, but not limited to, amelioration of symptoms of anxiety and stress disorders, depression, memory loss due to Alzheimer's disease or other dementias, epilepsy and convulsions, acute and/or chronic pain conditions, symptoms of addictive drug withdrawal, control of water balance, Na.sup.+ excretion and arterial blood pressure disorders and metabolic disorders such as obesity.
本发明涉及以下式的化合物:##STR1##
其中,X为--O--或--CH.sub.2--; Y为--C(O)--、--(CH.sub.2).sub.n--或--N(CH.sub.3)--;n为1或2,或X和Y共同为--CH.dbd.CH--; Z为--NH--、--CH.sub.2--、--O--或.dbd.CH--; A.sup.1为##STR2## B为--(CH.sub.2).sub.m--;m为0、1或2;R.sup.1和R.sup.2各自独立地为氢或较低的烷基;R.sup.3为氢或卤素;R.sup.4为氢或羟基,虚线为(--CH.sub.2--CH.sub.2--).sub.n,n'为0或1,以及其药学上可接受的酸加盐。本发明的化合物是OFQ受体的拮抗剂。因此,它们将在治疗记忆和注意力缺陷、精神、神经和生理障碍,特别是缓解焦虑和压力障碍症状、抑郁症、由阿尔茨海默病或其他痴呆症引起的记忆丧失、癫痫和惊厥、急性和/或慢性疼痛症状、成瘾药物戒断症状、控制
水平衡、Na.sup.+排泄和动脉血压障碍以及代谢障碍如肥胖症方面有用。