(2R)-2-{[1-({[(3S)-1-(carboxymethyl)-2-oxo-2,3,4,5-tetrahydro-1H-benzazepin-3-yl]amino}carbonyl)cyclopent-1-yl]methyl}-4-(1-naphthyl)butanoic acid | 182821-33-6

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: (2R)-2-{[1-({[(3S)-1-(carboxymethyl)-2-oxo-2,3,4,5-tetrahydro-1H-benzazepin-3-yl]amino}carbonyl)cyclopent-1-yl]methyl}-4-(1-naphthyl)butanoic acid
• 英文别名: (2R)-2-{[1-({[(3S)-1-(carboxymethyl)-2-oxo-2,3,4,5-tetrahydro-1H-1-benzazepin-3-yl]amino}carbonyl)cyclopentyl]methyl}-4-(1-naphthyl)butanoic acid；(2R)-2-{[1-({[(3S)-1-(carboxymethyl)-2-oxo-2,3,4,5-tetrahydro-1H-1-benzazepin-3-yl]amino}carbonyl)cyclopentyl]methyl}4-(1-naphthyl)butanoic acid；{(3S)-3-[({1-[(2R)-2-carboxy-4-(1-naphthyl)butyl]cyclopentyl}carbonyl)amino]-2-oxo-2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl}acetic acid；1H-1-Benzazepine-1-acetic acid, 3-(((1-((2R)-2-carboxy-4-(1-naphthalenyl)butyl)cyclopentyl)carbonyl)amino)-2,3,4,5-tetrahydro-2-oxo-, (3S)-；(2R)-2-[[1-[[(3S)-1-(carboxymethyl)-2-oxo-4,5-dihydro-3H-1-benzazepin-3-yl]carbamoyl]cyclopentyl]methyl]-4-naphthalen-1-ylbutanoic acid
• CAS: 182821-33-6
• 化学式: C₃₃H₃₆N₂O₆
• 分子量: 556.659
• InChiKey: LOFDNSDPZTVIIO-VPUSJEBWSA-N

物化性质

• 沸点：
  888.7±65.0 °C(Predicted)
• 密度：
  1.33±0.1 g/cm3(Temp: 20 °C; Press: 760 Torr)(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  5.5
• 重原子数：
  41
• 可旋转键数：
  10
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.39
• 拓扑面积：
  124
• 氢给体数：
  3
• 氢受体数：
  6

文献信息

• Neutral endopeptidase (NEP) and human soluble endopeptidase (hSEP) inhibitors for prophylaxis and treatment of neuro-degenerative disorders
  申请人：Ikonomidou Hrissanthi

  公开号：US20050153936A1

  公开（公告）日：2005-07-14

  The invention relates to a novel use of known benzazepine, benzoxazepine, benzo-thiazepine-N-acetic acid and phosphono-substituted benzazepinone derivatives having neutral endopeptidase (NEP) and/or human soluble endopeptidase (hSEP) inhibitory activity. The compounds of the invention are useful for the preparation of pharmaceutical compositions for prophylaxis and treatment of neurodegenerative disorders. The compounds of the invention are known from the European patents EP 0 733 642 and EP 0 916 679, and can be described by the general formulae (1): wherein the symbols have the meanings as given above in the description.

  本发明涉及具有中性内肽酶（NEP）和/或人类可溶性内肽酶（hSEP）抑制活性的已知苯并氮平、苯并氧氮平、苯并-硫氮平-N-乙酸和膦酸取代的苯并氮酮衍生物的新用途。 本发明的化合物可用于制备预防和治疗神经退行性疾病的药物组合物。 本发明的化合物已知于欧洲专利 EP 0 733 642 和 EP 0 916 679，可用通式（1）描述：其中符号的含义如上文所述。
• NEUTRAL ENDOPEPTIDASE (NEP) AND HUMAN SOLUBLE ENDOPEPTIDASE (HSEP) INHIBITORS FOR PROPHYLAXIS AND TREATMENT OF NEURODEGENERATIVE DISORDERS
  申请人：Solvay Pharmaceuticals B.V.

  公开号：EP1706121B1

  公开（公告）日：2008-09-03
• NEUTRAL ENDOPEPTIDASE (NEP) AND HUMAN SOLUBLE ENDOPEPTIDASE (hSEP) INHIBITORS FOR PROPHYLAXIS AND TREATMENT OF EYE DISEASES
  申请人：FORTY-FOUR PHARMACEUTICALS SP. Z.O.O

  公开号：US20210046097A1

  公开（公告）日：2021-02-18

  The invention relates to a novel use of benzazepine, benzoxazepine, benzothiazepine-N-acetic acid and phosphono-substituted benzazepinone derivatives having both neutral endopeptidase (NEP) and/or human soluble endopeptidase (hSEP), and endothelin convertase (ECE) inhibitory activity. The compounds of the invention are useful for the preparation of pharmaceutical compositions for prophylaxis and treatment of eye diseases.
• NEUTRAL ENDOPEPTIDASE (NEP) AND HUMAN SOLUBLE ENDOPEPTIDASE (hSEP) INHIBITORS TO REDUCE DETRIMENTAL EFFECTS OF PERFUSION DEFICIENCY OF PARENCHYMAL ORGANS
  申请人：Turski Christopher

  公开号：US20210047352A1

  公开（公告）日：2021-02-18

  The invention relates to a novel use of benzazepine, benzoxazepine, benzothiazepine-N-acetic acid and phosphono-substituted benzazepinone derivatives having both neutral endopeptidase (NEP) and/or human soluble endopeptidase (hSEP), and endothelin convertase (ECE), inhibitory activity. The compounds of this invention are useful for the preparation of pharmaceutical compositions to reduce harmful effects of symptomless progressive disseminated perfusion deficiency of organs, or parts thereof, that may be suggestive of systemic diseases.
• US7232813B2
  申请人：——

  公开号：US7232813B2

  公开（公告）日：2007-06-19