(3S)-3-(1-Diethylphosphonomethylcyclopentane-1-carbonylamino)-2,3,4,5-tetrahydro-2-oxo-1H-1-benzazepine-1-acetic acid | 224793-23-1

• 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: (3S)-3-(1-Diethylphosphonomethylcyclopentane-1-carbonylamino)-2,3,4,5-tetrahydro-2-oxo-1H-1-benzazepine-1-acetic acid
• 英文别名: 2-[(3S)-3-[[1-(diethoxyphosphorylmethyl)cyclopentanecarbonyl]amino]-2-oxo-4,5-dihydro-3H-1-benzazepin-1-yl]acetic acid
• CAS: 224793-23-1
• 化学式: C₂₃H₃₃N₂O₇P
• 分子量: 480.498
• InChiKey: BNJYTSVKVRTUBW-SFHVURJKSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2
• 重原子数：
  33
• 可旋转键数：
  10
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.61
• 拓扑面积：
  122
• 氢给体数：
  2
• 氢受体数：
  7

文献信息

• Compounds with NEP/MP-inhibitory activity and uses thereof
  申请人：Solvay Pharmaceuticals GmbH

  公开号：US20040162345A1

  公开（公告）日：2004-08-19

  Compounds having combined, particularly concurrent, inhibitory activity on neutral endopeptidase (NEP) and on a novel metalloprotease designated IGS5, or of a pharmaceutically acceptable salt or solvate or biolabile ester thereof, and related methods for treating and for the manufacture of a pharmaceutical composition for a mammal, preferably a larger mammal such as a human, suffering from or being susceptible to a disease or condition which can be alleviated or inhibited by combined or concurrent inhibition of NEP and IGS5. Treatments for diseases or conditions where big-ET-1 levels are elevated, or where ET-1 is upregulated, where such diseases or conditions can be alleviated or inhibited by combined or concurrent inhibition of NEP and IGS5.

  对中性内肽酶(NEP)和一种被命名为IGS5的新型金属蛋白酶或其药学上可接受的盐或溶解物或生物可降解酯具有联合、特别是并发抑制活性的化合物，以及用于治疗和制造药物组合物的相关方法，该药物组合物用于哺乳动物，最好是较大的哺乳动物，如人类，患有或易患可通过联合或并发抑制NEP和IGS5而减轻或抑制的疾病或病症。治疗big-ET-1水平升高或ET-1上调的疾病或病症，这些疾病或病症可通过联合或同时抑制NEP和IGS5而减轻或抑制。
• USE OF COMPOUNDS WITH COMBINED NEP/MP-INHIBITORY ACTIVITY IN THE PREPARATION OF MEDICAMENTS
  申请人：Solvay Pharmaceuticals GmbH

  公开号：EP1397141A2

  公开（公告）日：2004-03-17
• US5952327A
  申请人：——

  公开号：US5952327A

  公开（公告）日：1999-09-14
• [EN] USE OF COMPOUNDS WITH COMBINED NEP/MP-INHIBITORY ACTIVITY IN THE PREPARATION OF MEDICAMENTS<br/>[FR] UTILISATION DE COMPOSES PRESENTANT UNE ACTIVITE D'INHIBITION DE NEP/MP COMBINEE DANS LA PREPARATION DE MEDICAMENTS
  申请人：SOLVAY PHARM GMBH

  公开号：WO2002094176A2

  公开（公告）日：2002-11-28

  This invention relates to the use of a compound having combined, in particular concurrent, inhibitorz activity on neutral endopeptidase (NEP) and on a novel metalloprotease designated IGS5, or of a pharmaceutically acceptable salt or solvate or biolabile ester thereof, for the manufacture of a medicament (pharmaceutical composition) for treating a larger mammal, preferably a human, suffering from or being susceptible to a disease or condition which can be alleviated or prevented by combined or concurrent inhibition of NEP and IGS5. In a particular aspect the present invention pertains to the use of said compounds with combined or concurrent NEP/IGS5 inhibitory activity for treating a larger mammal, preferably a human, suffering from or being susceptible to a disease or condition where bit-ET-l levels are elevated and which disease or condition can be alleviated or prevented by cobined or concurrent inhibition of NEP and IGS5. In a further particular aspect the present invention pertainsto the use of said compounds with combined or concurrent NEP/IGS5 inhibitory activity for treating a larger mammal, preferably a human, suffering from or being susceptible to a disease or condition where ET-1 is significantly upregulated and which disease or condition can be alleviated or prevented by combined or concurrent inhibition of NEP and IGS5. In the present invention said compounds with combined or concurrent NEP/IGS5-inhibitory activity preferably are used for the treatment and/or prophylaxis of hypertension, including secondary forms of hypertension such as renal or pulmonary hypertension, heart failure, angina pectoris, arrhythmias, myorcadial infarction, cardiac hypertrophy, cerebral ischemia, peripheral vascular disease, subarachnoidal hemorrhage, chronic obstructive pulmonary disease (COPD), asthma, renal disease, atherosclerosis, and pain in colorectal cancer or prostate cancer, in mammals, preferably in humans, and more preferably in a patient sub-population suffering from or being susceptible to a disease or condition which can be alleviated or prevented by combined or concurrent inhibition of NEP and IGS5. Furthermore, it may be beneficial to additionally combine the said compounds showing combined or concurrent NEP/IGS5 inhibitory activity with other individual and/or combined metalloprotease inhibitors than the NEP/IGS5 inhibitors, e.g. with separate ACE- and/or NEP-inhibitors and/or mixed inhibitors of these metalloproteases.