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2-AZETIDINEMETHANEAMINES AND 2-PYRROLIDINEMETHANEAMINES AS TAAR-LIGANDS

机译:Taar配体中的2-氮杂环丁烷甲胺和2-吡咯烷基乙胺

摘要

The present invention relates to compounds of formula (I) wherein R1is hydrogen, lower alkyl or benzyl which may be optionally substituted by halogenor lower alkoxy; R2 is hydrogen, halogen or OR, wherein R is lower alkyl,aryl or lower alkyl substituted by halogen; R3 is hydrogen or fluorine;Ar is phenyl; n is 0 or 1; o is 0, 1 or 2; and to their pharmaceutically active salts.It has been found that the compounds of formula I have a good affinity to the traceamine associated receptors (TAARs), especially for TAAR1. The compounds maybe used for the treatment of depression, anxiety disorders, bipolar disorder,attention deficit hyperactivity disorder (ADHD), stress-related disorders,psychotic disorders such as schizophrenia, neurological diseases such as Parkinson'sdisease, neurodegenerative disorders such as Alzheimer's disease, epilepsy,migraine, hypertension, substance abuse and metabolic disorders such as eatingdisorders, diabetes, diabetic complications, obesity, dyslipidemia, disordersof energy consumption and assimilation, disorders and malfunction of body temperaturehomeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.
机译:本发明涉及式(I)的化合物,其中R 1是氢,可被卤素取代的低级烷基或苄基或低级烷氧基; R2是氢,卤素或OR,其中R是低级烷基,被卤素取代的芳基或低级烷基; R3是氢或氟;Ar是苯基; n为0或1; o是0、1或2;以及它们的药物活性盐。已经发现式I化合物对痕量具有良好的亲和力。胺相关受体(TAAR),尤其是TAAR1。这些化合物可能用于治疗抑郁症,焦虑症,躁郁症,注意缺陷多动障碍(ADHD),与压力有关的障碍,精神分裂症等精神疾病,帕金森氏症等神经系统疾病疾病,神经退行性疾病(例如阿尔茨海默氏病),癫痫病,偏头痛,高血压,药物滥用和进食等代谢异常疾病,糖尿病,糖尿病并发症,肥胖症,血脂异常,疾病消耗和吸收,体温异常和功能异常稳态,睡眠和昼夜节律紊乱以及心血管疾病。

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