3-(3,4-difluorophenyl)pyrrolidine | 848822-98-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯烷类
• 英文名称: 3-(3,4-difluorophenyl)pyrrolidine
• CAS: 848822-98-0
• 化学式: C₁₀H₁₁F₂N
• 分子量: 183.201
• InChiKey: KVTILWXFURUWHL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.9
• 重原子数：
  13
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  12
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  3-(3,4-difluorophenyl)pyrrolidine 在 甲酸 作用下， 反应 1.0h， 生成 3-(3,4-difluorophenyl)-1-methylpyrrolidine fumarate
  参考文献：
  名称：

  WO2008/148799

  摘要：

  公开号：
• 作为产物：
  描述：

  1-benzyl-3-(3,4-difluorophenyl)-2,5-dihydro-1H-pyrrole 、 甲酸铵 在 氮气 、 钯 、 crude product 作用下， 以 甲醇 为溶剂， 反应 2.0h， 以to give the title compound (0.3 g)的产率得到3-(3,4-difluorophenyl)pyrrolidine
  参考文献：
  名称：

  DISUBSTITUTED PHENYLPYRROLIDINES AS MODULATORS OF CORTICAL CATECHOLAMINERGIC NEUROTRANSMISSION

  摘要：

  本发明提供了一种能够增加哺乳动物大脑皮层区域多巴胺和去甲肾上腺素等儿茶酚胺类物质的细胞外水平的化合物，更具体地，本发明提供了使用3-(二取代芳基)-吡咯烷类化合物治疗中枢神经系统疾病的方法。

  公开号：

  US20100197760A1

文献信息

• Novel 1-aryl-3-azabicyclo[3.1.0]hexanes: preparation and use to treat neuropsychiatric disorders
  申请人：Skolnick Phil

  公开号：US20070082940A1

  公开（公告）日：2007-04-12

  The invention provides novel, multiply-substituted 1-aryl-3-azabicyclo[3.1.0]hexanes, and related processes and intermediates for preparing these compounds, as well as compositions and methods employing these compounds for the treatment and/or prevention of central nervous system (CNS) disorders, including depression and anxiety.

  本发明提供了新型的、多取代的1-芳基-3-氮杂双环[3.1.0]己烷，以及制备这些化合物的相关过程和中间体，以及使用这些化合物治疗和/或预防中枢神经系统（CNS）疾病，包括抑郁症和焦虑症的组合物和方法。
• Novel 1-Aryl-3-Azabicyclo[3.1.0]Hexanes: Preparation And Use To Treat Neuropsychiatric Disorders
  申请人：Skolnick Phil

  公开号：US20090233978A1

  公开（公告）日：2009-09-17

  The invention provides novel, multiply-substituted 1-aryl-3-azabicyclo[3.1.0]hexanes, and related processes and intermediates for preparing these compounds, as well as compositions and methods employing these compounds for the treatment and/or prevention of central nervous system (CNS) disorders, including depression and anxiety.

  本发明提供了新颖的多取代的1-芳基-3-氮杂双环[3.1.0]己烷，以及制备这些化合物的相关过程和中间体，以及使用这些化合物进行中枢神经系统（CNS）疾病的治疗和/或预防，包括抑郁症和焦虑症的组合物和方法。
• Novel piperidine derivative
  申请人：Ohtake Norikazu

  公开号：US20090203710A1

  公开（公告）日：2009-08-13

  Provided are a histamine-H3 receptor antagonist; and a preventive and/or a remedy for metabolic system diseases such as obesity, diabetes, hormone secretion disorder, hyperlipemia, gout, fatty liver, circulatory system diseases, for example, stenocardia, acute/congestive cardiac insufficiency, cardiac infarction, coronary arteriosclerosis, hypertension, nephropathy, sleep disorder and various diseases accompanied by sleep disorder such as idiopathic hypersomnia repetitive hypersomnia, true hypersomnia, narcolepsy, sleep periodic acromotion disorder, sleep apnea syndrome, circadian rhythm disorder, chronic fatigue syndrome, REM sleep disorder, senile insomnia, night worker sleep insanitation, idiopathic insomnia, repetitive insomnia, true insomnia, electrolyte metabolism disorder; and central and peripheral nervous system diseases such as bulimia, emotional disorder, melancholia, anxiety, epilepsy, delirium, dementia, shinzophrenia, attention deficit/hyperactivity disorder, memory disorder, Alzheimer's disease, Parkinson's disease, sleep disorder, recognition disorder, motion disorder, paresthesia, dysosmia, epilepsy, morphine resistance, narcotic dependency, alcoholic dependency. The histamine-H3 receptor antagonist comprises a piperidine derivative compound of formula (I) [wherein X 1 and X 2 independently represent a nitrogen atom or CH; Y represents a specific group; X 3 represents O s —(CH 2 ) m ; R 1 and R 2 independently resent a hydrogen atom, a halogen atom, a linear or branched lower alkyl group, a lower alkoxy group, or an acetyl group substituted with 2 or 3 fluorine atoms; s is 0 or 1; and m is an integer to make (m+s) 0 or from 1 to 4], or its pharmaceutically-acceptable salt.

  提供了一种组织胺H3受体拮抗剂和一种预防和/或治疗代谢系统疾病的药物，例如肥胖症、糖尿病、激素分泌障碍、高脂血症、痛风、脂肪肝、循环系统疾病（例如心绞痛、急性/充血性心力衰竭、心肌梗塞、冠状动脉粥样硬化、高血压、肾病、睡眠障碍以及伴随睡眠障碍的各种疾病，如特发性嗜睡、反复嗜睡、真性嗜睡、嗜睡性周期性运动障碍、睡眠呼吸暂停综合征、生物钟节律障碍、慢性疲劳综合征、REM睡眠障碍、老年性失眠、夜班工人睡眠不洁、特发性失眠、反复失眠、真性失眠、电解质代谢障碍）；以及中枢和周围神经系统疾病，如暴食症、情绪障碍、忧郁症、焦虑症、癫痫、谵妄、痴呆、精神分裂症、注意力缺陷/多动障碍、记忆障碍、阿尔茨海默病、帕金森病、睡眠障碍、认知障碍、运动障碍、感觉异常、嗅觉异常、癫痫、吗啡耐受、麻醉药依赖和酒精依赖。 组织胺H3受体拮抗剂包括式（I）的哌啶衍生物化合物（其中X1和X2独立地表示氮原子或CH；Y表示特定的基团；X3表示Os-（CH2）m；R1和R2独立地表示氢原子、卤素原子、线性或支链低碳基、低碳氧基或乙酰基，被2或3个氟原子取代；s为0或1；m是一个整数，使（m+s）为0或1到4），或其药学上可接受的盐。
• NOVEL PIPERIDINE DERIVATIVE
  申请人：BANYU PHARMACEUTICAL CO., LTD.

  公开号：EP1669350A1

  公开（公告）日：2006-06-14

  Provided are a histamine-H3 receptor antagonist; and a preventive and/or a remedy for metabolic system diseases such as obesity, diabetes, hormone secretion disorder, hyperlipemia, gout, fatty liver; circulatory system diseases, for example, stenocardia, acute/congestive cardiac insufficiency, cardiac infarction, coronary arteriosclerosis, hypertension, nephropathy, sleep disorder and various diseases accompanied by sleep disorder such as idiopathic hypersomnnia, repetitive hypetsomnnia, true hypersomnnia, narcolepsy, sleep periodic acromotion disorder, sleep apnea syndrome, circadian rhythm disorder, chronic fatigue syndrome, REM sleep disorder, senile insomnia, night worker sleep insanitation, idiopathic imsomnia, repetitive insomnia, true insomnia, electrolyte metabolism disorder; and central and peripheral nervous system diseases such as bulimia, emotional disorder, melancholia, anxiety, epilepsy, delirium, dementia, shinzophrenia, attention deficit/hyperactivity disorder, memory disorder, Alzheimer's disease, Parkinson's disease, sleep disorder, recognition disorder, motion disorder, paresthesia, dysosmia, epilepsy, morphine resistance, narcotic dependency, alcoholic dependency. The histamine-H3 receptor antagonist comprises a piperidine derivative compound of formula (I) [wherein X1 and X2 independently represent a nitrogen atom or CH; Y represents a specific goup; X3 represents Os-(CH2)m; R1 and R2 independently represent a hydrogen atom, a halogen atom, a linear or branched lower alkyl group, a lower alkoxy group, or an acetyl group substitued with 2 or 3 fluorine atoms; s is 0 or 1; and m is an integer to make (m+s) 0 or from 1 to 4], or its pharmaceutically-acceptable salt.

  本发明提供了一种组胺-H3 受体拮抗剂；以及一种预防和/或治疗代谢系统疾病的药物，例如肥胖症、糖尿病、激素分泌紊乱、高脂血症、痛风、脂肪肝；循环系统疾病，如心血管狭窄、急性/充血性心功能不全、心肌梗塞、冠状动脉硬化、高血压、肾病、睡眠障碍和伴有睡眠障碍的各种疾病，如特发性嗜睡症、重复性嗜睡症、真性嗜睡症、嗜睡症、睡眠周期性运动障碍、睡眠呼吸暂停综合征、昼夜节律紊乱、慢性疲劳综合征、快速眼动睡眠障碍、老年性失眠症、夜班工人睡眠失调症、特发性失眠症、重复性失眠症、真性失眠症、电解质代谢紊乱；以及中枢和周围神经系统疾病，如贪食症、情感障碍、忧郁症、焦虑症、癫痫、谵妄、痴呆、新精神分裂症、注意力缺陷/多动障碍、记忆障碍、阿尔茨海默病、帕金森病、睡眠障碍、识别障碍、运动障碍、麻痹、嗅觉障碍、癫痫、吗啡抵抗、麻醉品依赖、酒精依赖。组胺-H3 受体拮抗剂包括式（I）的哌啶衍生物化合物[其中 X1 和 X2 独立地代表氮原子或 CH；Y 代表特定基团；X3 代表 Os-(CH2)m；R1和R2独立地代表氢原子、卤素原子、直链或支链低级烷基、低级烷氧基或被2或3个氟原子取代的乙酰基；s为0或1；m为整数，使(m+s)为0或1至4]，或其药学上可接受的盐。
• Blood-brain barrier-penetrant dopamine-β-hydroxylase inhibitors
  申请人：BIAL—PORTELA & Cᵃ, S.A.

  公开号：US10975083B2

  公开（公告）日：2021-04-13

  This invention relates to: (a) compounds of formula (I) (with R1 to R5, n and A as defined herein) and pharmaceutically acceptable salts or solvates thereof that are useful as dopamine-β-hydroxylase inhibitors; (b) pharmaceutical compositions comprising such compounds, salts or solvates; (c) the use of such compounds, salts or solvates in therapy; (d) therapeutic methods of treatment using such compounds, salts or solvates; and (e) processes and intermediates useful for the synthesis of such compounds.

  本发明涉及：(a) 可用作多巴胺-β-羟化酶抑制剂的式 (I) 化合物（其中 R1 至 R5、n 和 A 如本文所定义）及其药学上可接受的盐或溶液；(b) 包含此类化合物、盐或溶液的药物组合物；(c) 此类化合物、盐或溶液在治疗中的用途；(d) 使用此类化合物、盐或溶液的治疗方法；以及 (e) 用于合成此类化合物的工艺和中间体。