N-substituted cycloalkyl and polycycloalkyl alpha-substituted Trp-Phe- and phenethylamine derivatives
申请人:WARNER-LAMBERT COMPANY
公开号:EP0405537A1
公开(公告)日:1991-01-02
Novel unnatural dipeptoids of α-substituted Trp-Phe derivatives useful as agents in the treatment of obesity, hypersecretion of gastric acid in the gut, gastrin-dependent tumors, or as antipsychotics are disclosed. Further the compounds are antianxiety agents and antiulcer agents and are agents useful for preventing the withdrawal response produced by chronic treatment or use followed by chronic treatment followed by withdrawal from nicotine, diazepam, alcohol or cocaine. Also disclosed are pharmaceutical compositions and methods of treatment using the dipeptoids as well as processes for preparing them and novel intermediates useful in their preparation. An additional feature of the invention is the use of the subject compounds to prepare pharmaceutical and diagnostic compositions.
本研究公开了α-取代的Trp-Phe衍生物的新型非天然二肽类化合物,可作为治疗肥胖症、肠道胃酸分泌过多、胃泌素依赖性肿瘤的药物或抗精神病药物。此外,这些化合物还是抗焦虑剂和抗溃疡剂,以及用于防止因长期治疗或使用尼古丁、地西泮、酒精或可卡因而产生的戒断反应的药物。本发明还公开了使用二胜肽类药物的药物组合物和治疗方法,以及制备二胜肽类药物的工艺和用于制备二胜肽类药物的新型中间体。本发明的另一个特点是使用上述化合物制备药物和诊断组合物。