4-cyclohexyl-5-methyl-4,5-dihydro-1,3-oxazol-2-ylamine | 1257614-00-8

• 分子结构分类: 有机化合物 - 有机杂环化合物
• 英文名称: 4-cyclohexyl-5-methyl-4,5-dihydro-1,3-oxazol-2-ylamine
• 英文别名: 4-cyclohexyl-5-methyl-4,5-dihydro-oxazol-2-ylamine；4-Cyclohexyl-5-methyl-4,5-dihydro-1,3-oxazol-2-amine
• CAS: 1257614-00-8
• 化学式: C₁₀H₁₈N₂O
• 分子量: 182.266
• InChiKey: UKMBFDLEKQMQSD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.1
• 重原子数：
  13
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.9
• 拓扑面积：
  47.6
• 氢给体数：
  1
• 氢受体数：
  2

文献信息

• [EN] 2-AMINOOXAZOLINES AS TAAR1 LIGANDS<br/>[FR] 2-AMINOOXAZOLINES UTILISÉES COMME LIGANDS DE TAAR1
  申请人：HOFFMANN LA ROCHE

  公开号：WO2010139707A1

  公开（公告）日：2010-12-09

  The invention relates to compounds of formula (I) wherein R1 is halogen; R2 is lower alkyl or lower alkyl substituted by halogen; R2' is hydrogen, lower alkyl or lower alkyl substituted by halogen; X is a bond, -CH2-, -CH2CH2- or -CH2CH2CH2-; Y is phenyl or cyclohexyl; and n is 0, 1 or 2; or to a pharmaceutically suitable acid addition salt thereof. The compounds of formula I are active on the TAAR1 receptor and are therefore suitable for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress-related disorders, psychotic disorders, schizophrenia, neurological diseases, Parkinson's disease, neurodegenerative disorders, Alzheimer's disease, epilepsy, migraine, substance abuse and metabolic disorders, eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.

  该发明涉及以下式（I）的化合物，其中R1是卤素；R2是较低的烷基或被卤素取代的较低烷基；R2'是氢、较低的烷基或被卤素取代的较低烷基；X是键、-CH2-、- -或- -；Y是苯基或环己基；n为0、1或2；或其药学上适用的酸盐。式I的化合物对TAAR1受体具有活性，因此适用于治疗抑郁症、焦虑症、双相情感障碍、注意力缺陷多动障碍、与压力有关的障碍、精神障碍、精神分裂症、神经系统疾病、帕金森病、神经退行性疾病、阿尔茨海默病、癫痫、偏头痛、物质滥用和代谢障碍、饮食障碍、糖尿病、糖尿病并发症、肥胖症、血脂异常、能量消耗和吸收障碍、体温稳态障碍和功能障碍、睡眠和昼夜节律障碍，以及心血管疾病的治疗。
• 2-AMINOOXAZOLINES AS TAAR1 LIGANDS
  申请人：Décoret Guillaume

  公开号：US20100311798A1

  公开（公告）日：2010-12-09

  The invention relates to compounds of formula wherein R 1 , R 2 , R 2′ , X, Y, andn are as defined in the specification or to a pharmaceutically suitable acid addition salt thereof. The compounds of formula I are active on the TAAR1 receptor and are therefore suitable for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress-related disorders, psychotic disorders, schizophrenia, neurological diseases, Parkinson's disease, neurodegenerative disorders, Alzheimer's disease, epilepsy, migraine, substance abuse and metabolic disorders, eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.

  本发明涉及式I的化合物，其中R1、R2、R2'、X、Y和n的定义如规范中所述，或其药学上适宜的酸盐。式I的化合物在TAAR1受体上具有活性，因此适用于治疗抑郁症、焦虑症、双相障碍、注意力缺陷多动障碍、与压力相关的障碍、精神障碍、精神分裂症、神经系统疾病、帕金森病、神经退行性疾病、阿尔茨海默病、癫痫、偏头痛、物质滥用和代谢性疾病、进食障碍、糖尿病、糖尿病并发症、肥胖症、血脂异常、能量消耗和吸收障碍、体温稳态失调、睡眠和昼夜节律障碍以及心血管疾病的治疗。
• TRACE AMINE ASSOCIATED RECEPTOR 1 AGONISTS AND PARTIAL AGONISTS FOR PAIN TREATMENT
  申请人：Purdue Pharma LP

  公开号：EP3463359A1

  公开（公告）日：2019-04-10
• [EN] TRACE AMINE ASSOCIATED RECEPTOR 1 AGONISTS AND PARTIAL AGONISTS FOR PAIN TREATMENT<br/>[FR] AGONISTES DU RÉCEPTEUR 1 ASSOCIÉ À UNE AMINE À L'ÉTAT DE TRACE ET AGONISTES PARTIELS POUR LE TRAITEMENT DE LA DOULEUR
  申请人：PURDUE PHARMA LP

  公开号：WO2017210616A1

  公开（公告）日：2017-12-07

  This application relates to using trace amine associated receptor 1 (TAAR1) agonists and/or partial agonists for treating or preventing pain, especially neuropathic pain.