N-(3-bromopropyl)-2,2-diphenylacetamide | 644974-20-9

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: N-(3-bromopropyl)-2,2-diphenylacetamide
• CAS: 644974-20-9
• 化学式: C₁₇H₁₈BrNO
• 分子量: 332.24
• InChiKey: CPSBMUMHXPUMKC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.9
• 重原子数：
  20
• 可旋转键数：
  6
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.24
• 拓扑面积：
  29.1
• 氢给体数：
  1
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  4-苄基哌啶 、 N-(3-bromopropyl)-2,2-diphenylacetamide 在 三乙胺 作用下， 以 二甲基亚砜 为溶剂， 以53%的产率得到N-(3-(4-benzylpiperidin-1-yl)propyl)-2,2-diphenylacetamide
  参考文献：
  名称：

  1，4-二取代哌嗪和哌啶作为三重再摄取抑制剂的设计，合成和体外活性。

  摘要：

  单胺转运蛋白调节着单胺神经递质的浓度，这对于重要的生理过程至关重要，其功能障碍会导致多种中枢神经系统疾病。目前，单胺转运蛋白似乎是这些疾病管理中的潜在靶标。在这项研究中，同源性和生物立体异构技术已被用于设计新的1,4-二取代哌嗪和哌啶。这些衍生物被合成并评估为潜在的三重再摄取抑制剂，用于研究结构-活性关系。最先进的化合物1-（4-（5-苯甲酰基-1H-四唑-1-基）丁基）-4-（3-苯丙基）哌嗪（2i）在体外测试中能够抑制单胺神经递质的再摄取（对于5-HT，IC50 = 158.7nM，对于NE，IC50 = 99nM，对于DA，IC50 = 97.5nM）。

  DOI：

  10.1016/j.bmc.2017.02.051
• 作为产物：
  描述：

  2,2-二苯基乙酸 在 氯化亚砜 、 三乙胺 作用下， 以 四氢呋喃 、 二氯甲烷 、 甲苯 、 苯 为溶剂， 生成 N-(3-bromopropyl)-2,2-diphenylacetamide
  参考文献：
  名称：

  1，4-二取代哌嗪和哌啶作为三重再摄取抑制剂的设计，合成和体外活性。

  摘要：

  单胺转运蛋白调节着单胺神经递质的浓度，这对于重要的生理过程至关重要，其功能障碍会导致多种中枢神经系统疾病。目前，单胺转运蛋白似乎是这些疾病管理中的潜在靶标。在这项研究中，同源性和生物立体异构技术已被用于设计新的1,4-二取代哌嗪和哌啶。这些衍生物被合成并评估为潜在的三重再摄取抑制剂，用于研究结构-活性关系。最先进的化合物1-（4-（5-苯甲酰基-1H-四唑-1-基）丁基）-4-（3-苯丙基）哌嗪（2i）在体外测试中能够抑制单胺神经递质的再摄取（对于5-HT，IC50 = 158.7nM，对于NE，IC50 = 99nM，对于DA，IC50 = 97.5nM）。

  DOI：

  10.1016/j.bmc.2017.02.051

文献信息

• Substituted alkyl amido piperidines
  申请人：Synaptic Pharmaceutical Corporation

  公开号：US20040186103A1

  公开（公告）日：2004-09-23

  This invention is directed to compounds which are selective antagonists for melanin concentrating hormone-1 (MCH1) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of the compound of this invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of reducing the body mass of a subject which comprises administering to the subject an amount of a compound of the invention effective to reduce the body mass of the subject. This invention further provides a method of treating a subject suffering from depression and/or anxiety which comprises administering to the subject an amount of a compound of the invention effective to treat the subject's depression and/or anxiety.

  这项发明涉及选择性拮抗黑色素浓缩激素-1（MCH1）受体的化合物。该发明提供了一种包括该发明化合物的治疗有效量和药学上可接受的载体的药物组合物。该发明提供了一种由结合本发明化合物的治疗有效量和药学上可接受的载体制成的药物组合物。该发明还提供了一种制备药物组合物的方法，包括结合本发明化合物的治疗有效量和药学上可接受的载体。该发明还提供了一种减少受试者体重的方法，包括向受试者施用本发明化合物的有效量以减少受试者的体重。该发明还提供了一种治疗患有抑郁症和/或焦虑症的受试者的方法，包括向受试者施用本发明化合物的有效量以治疗受试者的抑郁症和/或焦虑症。
• 신규한 1,4-치환된 피페라진 또는 피페리딘 화합물 및 이를 포함하는 약학적 조성물
  申请人：INDUSTRY FOUNDATION OF CHONNAM NATIONAL UNIVERSITY 전남대학교산학협력단(220040365775) BRN ▼409-82-11942

  公开号：KR101819472B1

  公开（公告）日：2018-01-17

  본 발명은 하기 화학식 1의 화합물 또는 이의 약제학적으로 허용 가능한 염에 관한 것이다: [화학식 1] 상기 화학식 1에서, R 및 R는 서로 독립적으로 수소, 할로겐,탄소수 1 내지 4인 알킬기, 탄소수 1 내지 4인 알콕시기, 또는 트리플루오로메틸이고; R는 직접 결합, 탄소수 1 내지 4인 알킬기, 또는 탄소수 2 내지 4인 알케닐이고; R는 치환 또는 비치환된 탄소수 6 내지 10인 아릴기, 또는 치환 또는 비치환된 탄소수 6 내지 10인 헤테로아릴기이고, 상기 R의 치환된 아릴기 및 헤테로아릴기는 서로 독립적으로 할로겐, 탄소수 1 내지 4인 알킬기, 또는 탄소수 1 내지 4인 알콕시기로 치환된 것이고; X는 C 또는 N이고; Y는 O, CONH, NHCO 또는 이고; n은 0 내지 4의 정수인 것이다.

  该专利涉及化学式1中的化合物或其药理学上可接受的盐：[化学式1] 在上述化学式1中，R和R分别独立地表示氢，卤素，1至4个碳原子的烷基，1至4个碳原子的氧烷基，或三氟甲基；R直接连接，表示1至4个碳原子的烷基，或表示2至4个碳原子的烯基；R代表取代或未取代的含6至10个碳原子的芳基，或取代或未取代的含6至10个碳原子的杂环芳基，R的取代芳基和杂环芳基可以独立地被卤素，1至4个碳原子的烷基，或1至4个碳原子的氧烷基取代；X为C或N；Y为O，CONH，NHCO或；n为0到4之间的整数。
• [EN] SPIROCYCLIC PIPERIDINES AS MCH1 ANTAGONISTS AND USES THEREOF<br/>[FR] PIPERIDINES SPIROCYCLIQUES UTILISEES COMME ANTAGONISTES DES MCH1 ET UTILISATIONS ASSOCIEES
  申请人：SYNAPTIC PHARMA CORP

  公开号：WO2004004714A1

  公开（公告）日：2004-01-15

  This invention is directed to compounds which are selective antagonists for melanin concentrating hormone-1 (MCH1) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of the compound of this invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of reducing the body mass of a subject which comprises administering to the subject an amount of a compound of the invention effective to reduce the body mass of the subject. This invention further provides a method of treating a subject suffering from depression and/or anxiety which comprises administering to the subject an amount of a compound of the invention effective to treat the subject=s depression and/or anxiety. This invention further provides a method of treating a subject suffering from a urinary disorder.

  这项发明涉及选择性拮抗黑色素浓缩激素-1（MCH1）受体的化合物。该发明提供了一种药物组合物，包括本发明的化合物的治疗有效量和药学上可接受的载体。该发明提供了一种通过结合本发明的化合物的治疗有效量和药学上可接受的载体制备的药物组合物。该发明还提供了一种制备药物组合物的方法，包括结合本发明的化合物的治疗有效量和药学上可接受的载体。该发明还提供了一种减少受试者体重的方法，包括向受试者投与本发明化合物的有效量以减少受试者体重。该发明还提供了一种治疗患有抑郁症和/或焦虑症的受试者的方法，包括向受试者投与本发明化合物的有效量以治疗受试者的抑郁症和/或焦虑症。该发明还提供了一种治疗患有尿液失调的受试者的方法。
• Spirocvclic piperidines as mch1 antagonists and uses thereof
  申请人：Marzabadi R Mohammad

  公开号：US20060173027A1

  公开（公告）日：2006-08-03

  This invention is directed to compounds which are selective antagonists for melanin concentrating hormone-1 (MCH1) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of the compound of this invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of reducing the body mass of a subject which comprises administering to the subject an amount of a compound of the invention effective to reduce the body mass of the subject. This invention further provides a method of treating a subject suffering from depression and/or anxiety which comprises administering to the subject an amount of a compound of the invention effective to treat the subject=s depression and/or anxiety. This invention further provides a method of treating a subject suffering from a urinary disorder.

  本发明涉及选择性拮抗黑色素浓集素-1（MCH1）受体的化合物。本发明提供一种制药组合物，包括本发明的化合物的治疗有效量和药学上可接受的载体。本发明提供了一种制备制药组合物的方法，包括将本发明的化合物的治疗有效量和药学上可接受的载体结合。本发明还提供了一种减轻受试者体重的方法，包括向受试者施用本发明的化合物的有效量以减轻受试者的体重。本发明还提供了一种治疗患有抑郁症和/或焦虑症的受试者的方法，包括向受试者施用本发明的化合物的有效量以治疗受试者的抑郁症和/或焦虑症。本发明还提供了一种治疗患有泌尿系统疾病的受试者的方法。
• SUBSTITUTED ALKYL AMIDO PIPERIDINES
  申请人：Marzabadi R. Mohammad

  公开号：US20060041139A9

  公开（公告）日：2006-02-23

  This invention is directed to compounds which are selective antagonists for melanin concentrating hormone-1 (MCH1) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of the compound of this invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of reducing the body mass of a subject which comprises administering to the subject an amount of a compound of the invention effective to reduce the body mass of the subject. This invention further provides a method of treating a subject suffering from depression and/or anxiety which comprises administering to the subject an amount of a compound of the invention effective to treat the subject's depression and/or anxiety.

  本发明涉及一种选择性抗黑色素浓缩激素-1（MCH1）受体的化合物。本发明提供一种制药组合物，包括本发明化合物的治疗有效量和药学上可接受的载体。本发明提供一种由本发明化合物的治疗有效量和药学上可接受的载体组合而成的制药组合物。本发明还提供一种制备制药组合物的方法，包括将本发明化合物的治疗有效量和药学上可接受的载体组合。本发明还提供一种减轻受试者体重的方法，包括向受试者给予本发明化合物的有效量以减轻受试者的体重。本发明还提供一种治疗患有抑郁和/或焦虑症的受试者的方法，包括向受试者给予本发明化合物的有效量以治疗受试者的抑郁和/或焦虑症。