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首页> 外国专利> New indole derivatives are melatonin receptor binders useful to treat e.g. sleep disturbance, stress, anxiety, depression, cardiovascular diseases, digestive system disorders, schizophrenia, panic attack, obesity and insomnia

New indole derivatives are melatonin receptor binders useful to treat e.g. sleep disturbance, stress, anxiety, depression, cardiovascular diseases, digestive system disorders, schizophrenia, panic attack, obesity and insomnia

机译：新的吲哚衍生物是可用于治疗例如美沙酮的褪黑激素受体粘合剂。睡眠障碍，压力，焦虑，抑郁，心血管疾病，消化系统疾病，精神分裂症，惊恐发作，肥胖和失眠

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Indole derivatives (I), their enantiomers, diastereomers and their acid/base addition salts are new. Indole derivatives of formula (I), their enantiomers, diastereomers and their acid/base addition salts are new. R 11-6C alkyl, 3-8C cycloalkyl or 3-8C cycloalkyl-1-6C alkyl, preferably methyl; R 21-6C alkyl, preferably methyl, ethyl or propyl; and n : 1-6, preferably 2. An independent claim is included for the preparation of (I). [Image] ACTIVITY : Hypnotic; Tranquilizer; Antidepressant; Cardiovascular-Gen; Gastrointestinal-Gen; Neuroleptic; Anorectic; Anticonvulsant; Antidiabetic; Antiparkinsonian; Nootropic; Antimigraine; Neuroprotective; Endocrine-Gen; Contraceptive; Immunomodulator; Cytostatic. MECHANISM OF ACTION : Melatonin receptor binder. The affinity of (I) to bind with melatonin receptors MT1 and MT2 was tested using 2-[ 1 2 5I]-iodomelatonin as reference radioligand. The results showed that (I) exhibited an inhibition constant value of less than 1 mu M.
机译：吲哚衍生物（I），其对映异构体，非对映异构体及其酸/碱加成盐是新的。式（I）的吲哚衍生物，其对映异构体，非对映异构体及其酸/碱加成盐是新的。 R 11-6C烷基，3-8C环烷基或3-8C环烷基-1-6C烷基，优选甲基; R 21-6C烷基，优选甲基，乙基或丙基; n：1-6，优选2。制备（I）包括独立权利要求。 [图像]活动：催眠;镇静剂;抗抑郁药心血管基因胃肠源;抗精神病药;厌食的;抗惊厥药;抗糖尿病反帕金森病;促智;抗偏头痛;具有神经保护作用;内分泌基因避孕药免疫调节剂止细胞的。作用机理：褪黑激素受体结合剂。使用2- [1> 2> 5> I]-碘降钙素作为参考放射性配体，测试（I）与褪黑激素受体MT1和MT2结合的亲和力。结果表明（I）显示出小于1μM的抑制常数。

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