4-(3-氨基苯基)-5,6-二氢吡啶-1(2H)-羧酸叔丁酯 | 387827-18-1

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: 4-(3-氨基苯基)-5,6-二氢吡啶-1(2H)-羧酸叔丁酯
• 英文名称: tert-butyl 4-[3-(amino)phenyl]-1,2,3,6-tetrahydro-1-pyridinecarboxylate
• 英文别名: tert-butyl 4-(3-aminophenyl)-3,6-dihydropyridine-1(2H)-carboxylate；TERT-BUTYL 4-(3-AMINOPHENYL)-3,6-DIHYDRO-1(2H)-PYRIDINE CARBOXYLATE；tert-butyl 4-(3-aminophenyl)-3,6-dihydro-1(2H)-pyridinecarboxylate；tert-Butyl 4-(3-aminophenyl)-5,6-dihydropyridine-1(2H)-carboxylate；tert-butyl 4-(3-aminophenyl)-3,6-dihydro-2H-pyridine-1-carboxylate
• CAS: 387827-18-1
• 化学式: C₁₆H₂₂N₂O₂
• 分子量: 274.363
• InChiKey: HPSJZYBXANBFJH-UHFFFAOYSA-N

物化性质

• 沸点：
  424.7±45.0 °C(Predicted)
• 密度：
  1.131±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  20
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.44
• 拓扑面积：
  55.6
• 氢给体数：
  1
• 氢受体数：
  3

安全信息

• 危险性防范说明：
  P261,P305+P351+P338
• 危险性描述：
  H302,H315,H319,H335

反应信息

• 作为反应物：
  描述：

  4-(3-氨基苯基)-5,6-二氢吡啶-1(2H)-羧酸叔丁酯 在 吗啉 、 吡啶 、 4-二甲氨基吡啶 、 四(三苯基膦)钯 、 palladium on activated charcoal 、 氢气 、 potassium carbonate 、 N,N'-二环己基碳二亚胺 、 三氟乙酸 作用下， 以 乙腈 为溶剂， 反应 37.0h， 生成 FE@SNAP
  参考文献：
  名称：

  用于正电子发射断层扫描的黑色素浓缩激素受体 1 (MCHR1) 示踪剂 [¹¹C]SNAP-7941 和 [¹⁸F]FE@SNAP 的前体和参考化合物的合成。

  摘要：

  MCH 受体已被揭示为正电子发射断层扫描成像中非常感兴趣的目标。该受体的同名底物黑色素浓缩激素 (MCH) 是一种环肽激素，主要位于下丘脑，主要影响能量和体重调节以及水平衡和记忆。因此，人们认为它在肥胖的病理生理学中起重要作用，肥胖是当今世界范围内的一个大问题。基于选择性和高亲和力 MCH 受体 1 拮抗剂 SNAP-7941，开发了一系列新型 SNAP 衍生物，为新型 PET 放射性示踪剂 [(11)C]SNAP-7941 和[(18)F]FE@SNAP。

  DOI：

  10.3390/molecules181012119
• 作为产物：
  描述：

  tert-butyl 4-hydroxy-5,6-dihydropyridine-1(2H)-carboxylate 在 potassium carbonate 、 三苯基膦 、 palladium dichloride 作用下， 生成 4-(3-氨基苯基)-5,6-二氢吡啶-1(2H)-羧酸叔丁酯
  参考文献：
  名称：

  用于正电子发射断层扫描的黑色素浓缩激素受体 1 (MCHR1) 示踪剂 [¹¹C]SNAP-7941 和 [¹⁸F]FE@SNAP 的前体和参考化合物的合成。

  摘要：

  MCH 受体已被揭示为正电子发射断层扫描成像中非常感兴趣的目标。该受体的同名底物黑色素浓缩激素 (MCH) 是一种环肽激素，主要位于下丘脑，主要影响能量和体重调节以及水平衡和记忆。因此，人们认为它在肥胖的病理生理学中起重要作用，肥胖是当今世界范围内的一个大问题。基于选择性和高亲和力 MCH 受体 1 拮抗剂 SNAP-7941，开发了一系列新型 SNAP 衍生物，为新型 PET 放射性示踪剂 [(11)C]SNAP-7941 和[(18)F]FE@SNAP。

  DOI：

  10.3390/molecules181012119

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。
• 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。
• 4-Aryl piperidines
  申请人：Marzabadi R. Mohammad

  公开号：US20050154020A1

  公开（公告）日：2005-07-14

  This invention is directed to 4-aryl piperidines and related heterocyclic 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4-芳基哌啶及其相关杂环化合物，这些化合物是对黑素集中激素-1（MCH1）受体的选择性拮抗剂。本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的载体。本发明还提供了一种通过结合治疗有效量的本发明化合物和药用可接受的载体而制成的药物组合物。本发明进一步提供了一种制备药物组合物的方法，包括结合治疗有效量的本发明化合物和药用可接受的载体。本发明还提供了一种减少主体体质量的方法，包括向主体施用有效减少主体体质量的本发明化合物的量。本发明还进一步提供了一种治疗患有抑郁和/或焦虑的主体的方法，包括向主体施用有效治疗主体的抑郁和/或焦虑的本发明化合物的量。
• [EN] SECONDARY AMINO ANILINIC PIPERIDINES AS MCH1 ANTAGONISTS AND USES THEREOF<br/>[FR] PIPERIDINES AMINOANILINIQUES SECONDAIRES UTILISEES COMME ANTAGONISTES DE LA MCH1 ET UTILISATIONS CORRESPONDANTES
  申请人：SYNAPTIC PHARMACEUTICAL CORPOR

  公开号：WO2004005257A1

  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 compounds 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.

  本发明涉及对黑素集中激素-1（MCH1）受体具有选择性的拮抗剂化合物。该发明提供了一种含有治疗有效量的本发明化合物和药用辅料的药物组合物。本发明还提供了一种通过结合治疗有效量的本发明化合物和药用辅料制成的药物组合物。本发明进一步提供了一种制作含有治疗有效量的本发明化合物和药用辅料的药物组合物的方法。本发明还提供了一种减少主体体质量的方法，包括向主体施用有效减少主体体质量的本发明化合物的量。本发明还提供了一种治疗患有抑郁和/或焦虑的主体方法，包括向主体施用有效治疗主体的抑郁和/或焦虑的本发明化合物的量。本发明还提供了一种治疗患有尿路障碍的主体方法。
• 4-aryl piperidines
  申请人：Marzabadi R. Mohammad

  公开号：US20050154022A1

  公开（公告）日：2005-07-14

  This invention is directed to 4-aryl piperidines and related heterocyclic 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4-芳基哌啶及其相关杂环化合物，这些化合物是黑素聚集激素-1（MCH1）受体的选择性拮抗剂。本发明提供了一种药物组合物，包括治疗有效量的本发明的化合物和药用可接受的载体。本发明还提供了一种通过结合治疗有效量的本发明的化合物和药用可接受的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的化合物和药用可接受的载体。本发明还提供了一种减少主体体质量的方法，包括向主体施用有效减少主体体质量的本发明的化合物的量。本发明进一步提供了一种治疗患有抑郁和/或焦虑的主体的方法，包括向主体施用有效治疗主体的抑郁和/或焦虑的本发明的化合物的量。