Amico acid derivatives cyclized at the C-terminal
    2.
    发明授权
    Amico acid derivatives cyclized at the C-terminal 失效
    氨基酸衍生物在C末端循环

    公开(公告)号:US5244915A

    公开(公告)日:1993-09-14

    申请号:US726654

    申请日:1991-07-12

    CPC分类号: C07D401/06 C07D209/20

    摘要: Novel .alpha.-substituted Trp dipeptoid derivatives cyclized at the C-terminal 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. They are agents useful for preventing the response to the withdrawal from chronic treatment with or use of nicotine, diazepam, alcohol, cocaine, caffeine, or opioids. The compounds of the invention are also useful in treating and/or preventing panic attacks. Also disclosed are pharmaceutical compositions and methods of treatment using the compounds 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 compounds in diagnostic compositions.

    摘要翻译: 在C末端环化的新型α取代Trp ep皮甙衍生物用作治疗肥胖症的药物,肠中胃酸分泌过高,胃泌素依赖性肿瘤或抗精神病药。 此外,化合物是抗焦虑剂和抗溃疡剂。 它们是可用于预防慢性治疗或使用尼古丁,地西泮,酒精,可卡因,咖啡因或阿片样物质的戒断反应的药剂。 本发明的化合物也可用于治疗和/或预防恐慌发作。 还公开了使用该化合物的药物组合物和治疗方法以及其制备方法和可用于其制备的新型中间体。 本发明的另一个特征是化合物在诊断组合物中的用途。

    Pro drugs for CCK antagonists
    4.
    发明授权
    Pro drugs for CCK antagonists 失效
    为CCK拮抗剂提供药物

    公开(公告)号:US5340825A

    公开(公告)日:1994-08-23

    申请号:US726653

    申请日:1991-07-12

    摘要: Novel pro-drugs ##STR1## the variables are as defined in the specification. New and unnatural dipeptoids of .alpha.-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 dipeptoids are antianxiety agents and antiulcer agents. They are agents useful for preventing the response to the withdrawal from chronic treatment or with use of nicotine, diazepam, alcohol, cocaine, caffeine, or opioids. The pro-drugs are also useful in treating and/or preventing panic attacks. Also disclosed are pharmaceutical compositions and methods of treatment using the pro-drugs 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 pro-drug compounds in diagnostic compositions.

    摘要翻译: 新型药物我的变量如规范中所定义。 公开了用作治疗肥胖症,胃肠胃分泌过多,胃泌素依赖性肿瘤或抗精神病药的α-取代的Trp-Phe衍生物的新的和非天然的dipeptoid。 此外,趾甲是抗焦虑剂和抗溃疡剂。 它们是用于预防慢性治疗戒断或使用尼古丁,地西泮,酒精,可卡因,咖啡因或阿片样物质的反应的药剂。 前药也可用于治疗和/或预防恐慌发作。 还公开了药物组合物和使用前药的治疗方法以及其制备方法和可用于其制备的新型中间体。 本发明的另一个特征是本发明的前药化合物在诊断组合物中的用途。