tert-butyl 4-(3-amino-4,6-difluorophenyl)piperidinecarboxylate | 643746-87-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: tert-butyl 4-(3-amino-4,6-difluorophenyl)piperidinecarboxylate
• 英文别名: tert-butyl 4-(5-amino-2,4-difluorophenyl)-1-pyperidinecarboxylate；tert-butyl 4-(5-amino-2,4-difluorophenyl)-1-piperidinecarboxylate；tert-butyl 4-(5-amino-2,4-difluorophenyl)piperidine-1-carboxylate
• CAS: 643746-87-6
• 化学式: C₁₆H₂₂F₂N₂O₂
• 分子量: 312.36
• InChiKey: RTXIBLJHNGELMX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.9
• 重原子数：
  22
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.56
• 拓扑面积：
  55.6
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  tert-butyl 4-(3-amino-4,6-difluorophenyl)piperidinecarboxylate 、 5-(2'-methoxyxyphenyl)pentanoic acid 在 4-二甲氨基吡啶 、 盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺 作用下， 以 DMF (N,N-dimethyl-formamide) 、 二氯甲烷 为溶剂， 反应 12.0h， 以83.2%的产率得到tert-butyl 4-(2,4-difluoro-5-{[5-(2-methoxyphenyl)pentanoyl]amino}phenyl)-1-piperidinecarboxylate
  参考文献：
  名称：

  [EN] SECONDARY AMINO ANILINIC PIPERIDINES AS MCH1 ANTAGONISTS AND USES THEREOF
  [FR] PIPERIDINES AMINOANILINIQUES SECONDAIRES UTILISEES COMME ANTAGONISTES DE LA MCH1 ET UTILISATIONS CORRESPONDANTES

  摘要：

  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。

  公开号：

  WO2004005257A1
• 作为产物：
  描述：

  tert-butyl 4-(5-nitro-2,4-difluorophenyl)-3,6-dihydro-1(2H)-pyridine carboxylate 在 钯 氢气 、 乙醇 作用下， 以 乙醇 为溶剂， 反应 16.0h， 以to give 17.0 g of thick oil that的产率得到tert-butyl 4-(3-amino-4,6-difluorophenyl)piperidinecarboxylate
  参考文献：
  名称：

  4-aryl piperidines

  摘要：

  本发明涉及4-芳基哌啶和相关杂环化合物，它们是黑色素浓聚激素-1（MCH1）受体的选择性拮抗剂。本发明提供了一种药物组成物，包括本发明化合物的治疗有效量和药学上可接受的载体。本发明提供了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药物组成物。本发明还提供了一种制备药物组成物的方法，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。本发明还提供了一种减轻受试者体重的方法，包括向受试者投与本发明化合物的有效量以减轻受试者的体重。本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，包括向受试者投与本发明化合物的有效量以治疗受试者的抑郁和/或焦虑。

  公开号：

  US20050154022A1

文献信息

• 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。
• Amino substituted aryloxybenzylpiperidine derivatives
  申请人：Marzabadi R. Mohammad

  公开号：US20060079522A1

  公开（公告）日：2006-04-13

  This invention is directed to Amino substituted Aryloxybenzylpiperidine derivatives which are ligands at the MCH1 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition made by admixing a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also 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 subject invention. This invention also provides a method of treating a subject suffering from obesity which comprises administering to the subject an amount of a compound of the subject invention.

  这项发明涉及氨基取代的芳氧基苄哌啶衍生物，它们是MCH1受体的配体。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。该发明还提供了一种通过混合该发明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。该发明进一步提供了一种制备药物组合物的方法，包括结合该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，包括向受试者施用该发明化合物的剂量。该发明还提供了一种治疗患有肥胖症的受试者的方法，包括向受试者施用该发明化合物的剂量。
• Arylthiobenzylpiperidine derivatives
  申请人：Marzabadi R. Mohammad

  公开号：US20060079523A1

  公开（公告）日：2006-04-13

  This invention is directed to Arylthiobenzylpiperidine derivatives which are ligands at the MCH1 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition made by admixing a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of treating a subject suffering from depression and/or anxiety which comprises administering to the subject a therapeutically effective amount of a compound of the subject invention. This invention also provides a method of treating a subject suffering from obesity which comprises administering to the subject a therapeutically effective amount of a compound of the subject invention.

  这项发明涉及芳基硫代苯基哌啶衍生物，这些衍生物是MCH1受体的配体。该发明提供了一种包含该发明化合物的治疗有效量和药用载体的药物组合物。该发明还提供了一种通过混合该发明化合物的治疗有效量和药用载体制备的药物组合物。该发明进一步提供了一种制备药物组合物的方法，包括结合该发明化合物的治疗有效量和药用载体。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，包括向受试者施用该发明化合物的治疗有效量。该发明还提供了一种治疗患有肥胖症的受试者的方法，包括向受试者施用该发明化合物的治疗有效量。
• Secondary amino anilinic piperidines as mch1 antagonists and uses thereof
  申请人：Marzabadi R. Mohammad

  公开号：US20050245743A1

  公开（公告）日：2005-11-03

  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 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.

  本发明涉及一种选择性抗黑色素浓集激素-1（MCH1）受体的化合物。本发明提供一种药物组合物，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成的药物组合物。本发明还提供一种制备药物组合物的方法，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，包括向受试者投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症和/或焦虑症的受试者的方法，包括向受试者投予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。本发明还提供一种治疗患有泌尿系统疾病的受试者的方法。
• Arylthiobenzylpiperidine Derivatives
  申请人：Marzabadi Mohammad R.

  公开号：US20080139555A1

  公开（公告）日：2008-06-12

  This invention is directed to Arylthiobenzylpiperidine derivatives which are ligands at the MCH1 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition made by admixing a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of treating a subject suffering from depression and/or anxiety which comprises administering to the subject a therapeutically effective amount of a compound of the subject invention. This invention also provides a method of treating a subject suffering from obesity which comprises administering to the subject a therapeutically effective amount of a compound of the subject invention.

  本发明涉及芳基硫代苄基哌啶衍生物，其为MCH1受体的配体。本发明提供一种制备药物组合物的方法，包括将本发明化合物的治疗有效量与药学上可接受的载体混合。本发明还提供一种制备药物组合物的方法，包括将本发明化合物的治疗有效量与药学上可接受的载体混合。本发明还提供一种制备药物组合物的方法，包括将本发明化合物的治疗有效量与药学上可接受的载体混合。本发明还提供一种治疗抑郁症和/或焦虑症的方法，包括向患者施用本发明化合物的治疗有效量。本发明还提供一种治疗肥胖症的方法，包括向患者施用本发明化合物的治疗有效量。