methyl (4S)-3-({[3-(4-[3-(acetylamino)phenyl]-3,6-dihydro-1(2H)-pyridinyl)propyl]amino}carbonyl)-4-(3,4-difluorophenyl)-6-(methoxymethyl)-2-oxo-1,2,3,4-tetrahydro-5-pyrimidine carboxylate | 488098-60-8

• 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: methyl (4S)-3-({[3-(4-[3-(acetylamino)phenyl]-3,6-dihydro-1(2H)-pyridinyl)propyl]amino}carbonyl)-4-(3,4-difluorophenyl)-6-(methoxymethyl)-2-oxo-1,2,3,4-tetrahydro-5-pyrimidine carboxylate
• 英文别名: methyl (4S)-3-({[3-(4-[3-(acetylamino)phenyl]-3,6-dihydro-1(2H)-pyridinyl)propyl]amino}carbonyl)-4-(3,4-difluorophenyl)-6-(methoxymethyl)-2-oxo-1,2,3,4-tetrahydro-5-pyrimidinecarboxylate；methyl (4S)-3-[3-[4-(3-acetamidophenyl)-3,6-dihydro-2H-pyridin-1-yl]propylcarbamoyl]-4-(3,4-difluorophenyl)-6-(methoxymethyl)-2-oxo-1,4-dihydropyrimidine-5-carboxylate
• CAS: 488098-60-8
• 化学式: C₃₁H₃₅F₂N₅O₆
• 分子量: 611.646
• InChiKey: IQNORNRXRNJFSI-NDEPHWFRSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  44
• 可旋转键数：
  11
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.35
• 拓扑面积：
  129
• 氢给体数：
  3
• 氢受体数：
  9

反应信息

• 作为反应物：
  描述：

  methyl (4S)-3-({[3-(4-[3-(acetylamino)phenyl]-3,6-dihydro-1(2H)-pyridinyl)propyl]amino}carbonyl)-4-(3,4-difluorophenyl)-6-(methoxymethyl)-2-oxo-1,2,3,4-tetrahydro-5-pyrimidine carboxylate 在 钯 氢气 作用下， 以 甲醇 为溶剂， 反应 16.0h， 以to give the tritiated methyl (4S)-3-{[(3-{4-[3-(acetylamino)phenyl]-1-piperidinyl}propyl)amino]carbonyl}-4-(3,4-difluorophenyl)-6-(methoxymethyl)-2-oxo-1,2,3,4-tetrahydro-5-pyrimidinecarboxylate ((+)−isomer), which in turn的产率得到SNAP-7941
  参考文献：
  名称：

  Secondary amino anilinic piperidines as MCH1 antagonists and uses thereof

  摘要：

  该发明涉及选择性拮抗黑色素浓集激素-1（MCH1）受体的化合物。该发明提供了一种制药组合物，包括本发明化合物的治疗有效量和药学上可接受的载体。该发明提供了一种制药组合物的制备方法，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结合。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。该发明还提供了一种治疗患有尿液障碍的受试者的方法。

  公开号：

  US07473698B2
• 作为产物：
  描述：

  N1-{3-[1-(3-aminopropyl)-1,2,3,6-tetrahydro-4-pyridinyl] phenyl}acetamide 、 (4S)-4-(3,4-Difluorophenyl)-6-methoxymethyl-3-(4-nitrophenoxycarbonyl)-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylic acid methyl ester 生成 methyl (4S)-3-({[3-(4-[3-(acetylamino)phenyl]-3,6-dihydro-1(2H)-pyridinyl)propyl]amino}carbonyl)-4-(3,4-difluorophenyl)-6-(methoxymethyl)-2-oxo-1,2,3,4-tetrahydro-5-pyrimidine carboxylate
  参考文献：
  名称：

  Substituted anilinic piperidines as MCH selective antagonists

  摘要：

  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。

  公开号：

  US06727264B1

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。
• [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。
• 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。
• Substituted alkyl amido piperidines
  申请人：——

  公开号：US20040073036A1

  公开（公告）日：2004-04-15

  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.

  本发明涉及一种选择性拮抗黑色素浓集激素-1（MCH1）受体的化合物。该发明提供了一种包含本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。本发明提供了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混合。本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。
• 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。