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PEPTIDES THAT PERFORM THE ROLE OF OXYTOCINE AGONISTS

机译:履行催产素激动剂作用的肽

摘要

The invention relates to compounds of the formula where R is hydrogen, lower alkyl or cycloalkyl; R is hydrogen or R and R may form together with the N atom and C atom to which they are attached a pyrrolidine ring, optionally substituted with one or two F atoms or a hydroxyl group, or may form an azetidine or piperazine ring; R is hydrogen, lower alkyl, lower alkyl substituted by a hydroxyl group, - (CH) C (O) NH, benzyl, phenyl, —CH-five-membered aromatic heterocyclic group, CH-indolyl, —CH-cycloalkyl, cycloalkyl or - (CH) -S-lower alkyl; Is hydrogen or lower alkyl; or X is —C (O) —CHR — CHR — C (O) —NH — CH—, R / R is hydrogen, or one of R or R is an amino group; o means 0 or 1; or to their pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and / or its optical isomers. The present compounds have been found to be oxytocin receptor agonists for the treatment of autism, stress, including post-traumatic stress disorder, anxiety, including anxiety disorders and depression, schizophrenia, mental disorders and memory loss, alcohol withdrawal, drug dependence, and also for the treatment of Pradora syndrome Willy.
机译:本发明涉及下式的化合物,其中R是氢,低级烷基或环烷基; R是氢或R和R可以与它们所连接的N原子和C原子一起形成吡咯烷环,并任选地被一个或两个F原子或羟基取代,或者可以形成氮杂环丁烷或哌嗪环; R为氢,低级烷基,被羟基取代的低级烷基,-(CH)C(O)NH,苄基,苯基,-CH 5元芳族杂环基,CH-吲哚基,-CH-环烷基,环烷基或-(CH)-S-低级烷基;是氢或低级烷基;或X为-C(O)-CHR-CHR-C(O)-NH-CH-,R / R为氢,或R或R之一为氨基;或o表示0或1;或其药学上可接受的酸加成盐,外消旋混合物,或其对应的对映异构体和/或其旋光异构体。已经发现本发明的化合物是催产素受体激动剂,用于治疗自闭症,压力(包括创伤后应激障碍),焦虑症(包括焦虑症和抑郁症),精神分裂症,精神障碍和记忆力减退,戒酒,药物依赖性,以及用于治疗普拉多拉综合症威利。

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