N-[(5R)-6-[[(2S)-1-[[(2S,5R)-5-acetamido-2-[(2R)-2-amino-3-(4-chlorophenyl)propanoyl]-2-[[(2S)-1-[(2S)-2-amino-6-(propan-2-ylamino)hexanoyl]pyrrolidine-2-carbonyl]-[(2S)-2-[[(2R)-2-amino-3-pyridin-3-ylpropanoyl]amino]-3-hydroxypropanoyl]amino]-6-naphthalen-2-yl-4-oxohexanoyl]-[(2S)-3-(4-hydroxyphenyl)-2-(methylamino)propanoyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-amino-6-oxohexyl]pyridine-3-carboxamide | 135215-95-1

• 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: N-[(5R)-6-[[(2S)-1-[[(2S,5R)-5-acetamido-2-[(2R)-2-amino-3-(4-chlorophenyl)propanoyl]-2-[[(2S)-1-[(2S)-2-amino-6-(propan-2-ylamino)hexanoyl]pyrrolidine-2-carbonyl]-[(2S)-2-[[(2R)-2-amino-3-pyridin-3-ylpropanoyl]amino]-3-hydroxypropanoyl]amino]-6-naphthalen-2-yl-4-oxohexanoyl]-[(2S)-3-(4-hydroxyphenyl)-2-(methylamino)propanoyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-amino-6-oxohexyl]pyridine-3-carboxamide
• CAS: 135215-95-1
• 化学式: C₈₀H₁₀₄ClN₁₅O₁₄
• 分子量: 1535.2
• InChiKey: CRLOOHDYULQNLS-SPAOFFDCSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4
• 重原子数：
  110
• 可旋转键数：
  41
• 环数：
  7.0
• sp3杂化的碳原子比例：
  0.45
• 拓扑面积：
  457
• 氢给体数：
  12
• 氢受体数：
  22

文献信息

• Use of LHRH Antagonists for the Treatment of Lower Urinary Tract Symptoms, in particular Overactive Bladder and/or Detrusor Overactivity
  申请人：AEterna Zentaris GmbH

  公开号：EP1967202A1

  公开（公告）日：2008-09-10

  The present invention provides at least one LHRH antagonist for use in the preparation of a medicament for the treatment or prophylaxis of at least one lower urinary tract symptom in mammals, wherein the at least one lower urinary tract symptom is selected from the group consisting of: "urinary incontinence, urge incontinence, overactive bladder, idiopathic overactive bladder, neurogenic overactive bladder, detrusor overactivity, idiopathic detrusor overactivity, neurogenic detrusor overactivity" and wherein the at least one LHRH antagonist is to be administered in an intermediate dose, which does not cause chemical (hormonal) castration.

  本发明提供至少一种LHRH拮抗剂，用于制备治疗或预防哺乳动物至少一种下尿路症状的药物，其中至少一种下尿路症状选自由以下组成的组："尿失禁、急迫性尿失禁、膀胱过度活动症、特发性膀胱过度活动症、神经源性膀胱过度活动症、逼尿肌过度活动症、特发性逼尿肌过度活动症、神经源性逼尿肌过度活动症"，其中至少一种 LHRH 拮抗剂的给药剂量为不会导致化学（激素）阉割的中等剂量。
• Method for the prophylaxis or treatment of flushing
  申请人：Maatschap Interne Geneeskunde Rijnstate

  公开号：EP2379099A1

  公开（公告）日：2011-10-26
• LHRH ANTAGONISTS FOR THE TREATMENT OF LOWER URINARY TRACT SYMPTOMS
  申请人：ENGEL Juergen

  公开号：US20090075937A1

  公开（公告）日：2009-03-19

  The present invention provides at least one LHRH antagonist for the treatment or prophylaxis of at least one lower urinary tract symptom in mammals which is to be administered in an intermediate dose, which does not cause chemical (hormonal) castration.
• METHOD FOR THE PROPHYLAXIS OR TREATMENT OF FLUSHING
  申请人：de Boer Johannes Mathijs Maria

  公开号：US20120053122A1

  公开（公告）日：2012-03-01

  The present invention relates to a method for the prophylaxis or treatment of a subject for flushing, wherein a pharmaceutical agent having LHRH antagonistic activity is administered to said subject at a dosage of less than 15 μg/kg/day. The present invention also relates to a pharmaceutical agent having LHRH antagonistic activity for use in the prophylaxis or treatment of a subject for flushing, wherein the pharmaceutical agent having LHRH antagonistic activity is administered to said subject at a dosage of less than 15 μg/kg/day. The flushing is preferably postmenopausal flushing or perimenopausal flushing.
• [EN] Method for the prophylaxis or treatment of flushing<br/>[FR] MÉTHODE DE TRAITEMENT PROPHYLACTIQUE OU THÉRAPEUTIQUE DES BOUFFÉES VASOMOTRICES
  申请人：MIJ INTERNE GENEESKUNDE RIJNST

  公开号：WO2010085145A1

  公开（公告）日：2010-07-29

  The present invention relates to a method for the prophylaxis or treatment of a subject for flushing, wherein a pharmaceutical agent having LHRH antagonistic activity is administered to said subject at a dosage of less than 15 µg/kg/day. The present invention also relates to a pharmaceutical agent having LHRH antagonistic activity for use in the prophylaxis or treatment of a subject for flushing, wherein the pharmaceutical agent having LHRH antagonistic activity is administered to said subject at a dosage of less than 15 µg/kg/day.The flushing is preferably postmenopausal flushing or perimenopausal flushing.