3-(4-(3-nitrophenyl)-3,6-dihydro-1(2h)-pyridinyl)-1-propanamine | 387827-16-9

• 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: 3-(4-(3-nitrophenyl)-3,6-dihydro-1(2h)-pyridinyl)-1-propanamine
• 英文别名: 3-[4-(3-nitrophenyl)-3,6-dihydro-2H-pyridin-1-yl]propan-1-amine
• CAS: 387827-16-9
• 化学式: C₁₄H₁₉N₃O₂
• 分子量: 261.324
• InChiKey: WVQBYISNQZTXHD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.4
• 重原子数：
  19
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.43
• 拓扑面积：
  75.1
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  3-(4-(3-nitrophenyl)-3,6-dihydro-1(2h)-pyridinyl)-1-propanamine 、 (S)-4-(3,4-difluorophenyl)-1,2,3,4-tetrahydro-6-(methoxymethyl)-2-oxo-5-pyrimidinecarboxylic acid 在 N-甲基吗啉 、 1,2-二氯乙烷 作用下， 以 二氯甲烷 为溶剂， 生成 (4R)-4-(3,4-difluorophenyl)-6-(methoxymethyl)-N-[3-(4-(3-nitrophenyl)-3,6-dihydro-1(2h)-pyridinyl)propyl]-2-oxo-1,2,3,4-tetrahydro-5-pyrimidinecarboxamide
  参考文献：
  名称：

  DNA encoding a human melanin concentrating hormone receptor (MCH1) and uses thereof

  摘要：

  这项发明提供了编码人类MCH1受体的孤立核酸，纯化的人类MCH1受体，包括编码人类MCH1受体的孤立核酸的载体，包含这种载体的细胞，针对人类MCH1受体的抗体，用于检测编码人类MCH1受体的核酸探针，互补于编码人类MCH1受体独特序列的反义寡核苷酸，表达编码正常或突变人类MCH1受体的转基因非人类动物，孤立人类MCH1受体的分离方法，治疗与人类MCH1受体活性相关的异常的方法，以及确定化合物与哺乳动物MCH1受体结合的方法。这项发明提供了一种修改受试者摄食行为的方法，包括向受试者投与足以减少受试者体重和/或减少受试者食物摄入量的MCH1拮抗剂的量。这项发明还提供了一种治疗患有抑郁和/或焦虑的受试者的方法，包括向受试者投与足以治疗受试者抑郁和/或焦虑的MCH1拮抗剂的量。

  公开号：

  US20030082623A1
• 作为产物：
  描述：

  tert-butyl 3-(4-(3-nitrophenyl)-3,6-dihydro-1(2H)-pyridinyl)propylcarbamate 在 盐酸 作用下， 以 1,4-二氧六环 、 水 为溶剂， 以97%的产率得到3-(4-(3-nitrophenyl)-3,6-dihydro-1(2h)-pyridinyl)-1-propanamine
  参考文献：
  名称：

  DNA encoding a human melanin concentrating hormone receptor (MCH1) and uses thereof

  摘要：

  该发明提供了编码人类MCH1受体的孤立核酸，纯化的人类MCH1受体，含有编码人类MCH1受体的孤立核酸的载体，含有这种载体的细胞，针对人类MCH1受体的抗体，用于检测编码人类MCH1受体的核酸探针，与编码人类MCH1受体的核酸的独特序列互补的反义寡核苷酸，表达编码正常或突变人类MCH1受体的转基因非人类动物，分离人类MCH1受体的方法，治疗与人类MCH1受体活性相关的异常的方法，以及确定化合物与哺乳动物MCH1受体结合的方法。该发明还提供了一种治疗患有尿失禁的受试者的方法，包括向受试者投予足以治疗受试者尿失禁的MCH1拮抗剂。

  公开号：

  US20040038855A1

文献信息

• Substituted anilinic piperidines as MCH selective antagonists
  申请人：Synaptic Pharmaceutical Corporation

  公开号：US06727264B1

  公开（公告）日：2004-04-27

  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 therepeutically 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.

  这项发明涉及对黑素集中激素-1（MCH1）受体具有选择性的拮抗剂化合物。发明提供了一种药物组合物，包括治疗有效量的本发明化合物和药用可接受载体。本发明还提供了一种通过结合本发明的治疗有效量的化合物和药用可接受载体来制造的药物组合物。本发明进一步提供了一种制造药物组合物的方法，包括结合治疗有效量的本发明化合物和药用可接受载体。
• Selective melanin concentrating hormone-1 (MCH1) receptor antagonists and uses thereof
  申请人：——

  公开号：US20030069261A1

  公开（公告）日：2003-04-10

  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 modifying feeding behavior of a subject which comprises administering to the subject an amount of a compound of the invention effective to decrease the consumption of food by the subject. This invention further provides a method of treating a feeding disorder in a subject which comprises administering to the subject an amount of a compound of the invention effective to decrease the consumption of food by the subject. In an embodiment of the invention, the feeding disorder is bulimia, bulimia nervosa or obesity.

  这项发明涉及选择性拮抗黑素浓集激素-1（MCH1）受体的化合物。该发明提供了一种包括所述化合物的治疗有效量和药学可接受载体的药物组合物。该发明提供了一种通过结合本发明化合物的治疗有效量和药学可接受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，包括结合本发明化合物的治疗有效量和药学可接受载体。该发明还提供了一种修改受试者进食行为的方法，包括向受试者投与本发明化合物的有效量以减少受试者的食物摄入量。该发明还提供了一种治疗受试者进食障碍的方法，包括向受试者投与本发明化合物的有效量以减少受试者的食物摄入量。在该发明实施方式中，进食障碍可以是暴食症、暴食症神经质或肥胖症。
• [EN] SELECTIVE MELANIN CONCENTRATING HORMONE-1 (MCH1) RECEPTOR ANTAGONISTS AND USES THEREOF<br/>[FR] ANTAGONISTES SELECTIFS DES RECEPTEURS (MCH1) D'HORMONE-1 DE CONCENTRATION DE LA MELANINE ET UTILISATION DE CEUX-CI
  申请人：SYNAPTIC PHARMARCEUTICAL CORP

  公开号：WO2002006245A1

  公开（公告）日：2002-01-24

  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 modifying feeding behavior of a subject which comprises administering to the subject an amount of a compound of the invention effective to decrease the consumption of food by the subject. This invention further provides a method of treating a feeding disorder in a subject which comprises administering to the subject an amount of a compound of the invention effective to decrease the consumption of food by the subject. In an embodiment of the invention, the feeding disorder is bulimia, bulimia nervosa or obesity.

  本发明涉及选择性拮抗黑色素浓集激素-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药组合物，其由本发明的化合物的治疗有效量和药学上可接受的载体组合而成。本发明还提供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组合。本发明还提供了一种修改受试者进食行为的方法，包括向受试者施用本发明的化合物的有效量，以减少受试者的食物摄入量。本发明还提供了一种治疗受试者进食障碍的方法，包括向受试者施用本发明的化合物的有效量，以减少受试者的食物摄入量。在本发明的实施方式中，进食障碍是贪食症、神经性贪食症或肥胖症。
• SELECTIVE MELANIN CONCENTRATING HORMONE-1 (MCH1) RECEPTOR ANTAGONISTS AND USES THEREOF
  申请人：Synaptic Pharmaceutical Corporation

  公开号：EP1299362A1

  公开（公告）日：2003-04-09
• EP1299362A4
  申请人：——

  公开号：EP1299362A4

  公开（公告）日：2004-11-03