Antarelix

• 分子结构分类: 有机化合物 - 有机聚合物 - 多肽
• 英文名称: Antarelix
• 英文别名: (2R)-1-[(2S)-2-[[(2S)-2-[[(2R)-2-[[(2S)-2-[[(2S)-2-[[(2R)-2-[[(2S)-2-[[(2R)-2-acetamido-3-naphthalen-2-ylpropanoyl]amino]-3-(4-chlorophenyl)propanoyl]amino]-3-pyridin-3-ylpropanoyl]amino]-3-hydroxypropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-6-(carbamoylamino)hexanoyl]amino]-4-methylpentanoyl]amino]-6-(propan-2-ylamino)hexanoyl]-N-(1-amino-1-oxopropan-2-yl)pyrrolidine-2-carboxamide
• 化学式: C₇₄H₁₀₀ClN₁₅O₁₄
• 分子量: 1459.1
• InChiKey: NOENHWMKHNSHGX-FAZSUBJTSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.5
• 重原子数：
  104
• 可旋转键数：
  41
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.47
• 拓扑面积：
  446
• 氢给体数：
  15
• 氢受体数：
  16

文献信息

• Conjugates of disorazoles and their derivatives with cell-binding molecules, novel disorazole derivatives, processes of manufacturing and uses thereof
  申请人：AEterna Zentaris GmbH

  公开号：EP1900742A1

  公开（公告）日：2008-03-19

  The present invention provides conjugates of disorazoles and their derivatives with cell-binding molecules, such as peptides, proteins, hormones, blood proteins and antibodies. The present invention further provides novel disorazole derivatives and processes of manufacturing such conjugates and disorazole derivatives. These compounds can be used as medicaments for the treatment of physiological and/or pathophysiological conditions in mammals, in particular for the treatment of various tumors.

  本发明提供了二氢异菊烯酮及其衍生物与细胞结合分子（如肽、蛋白质、激素、血液蛋白和抗体）结合的共轭物。本发明还提供了新的二氢异菊烯酮衍生物及制造这些共轭物和二氢异菊烯酮衍生物的方法。这些化合物可用作治疗哺乳动物的生理和/或病理状况，特别是治疗各种肿瘤的药物。
• CONJUGATES OF DISORAZOLES AND THEIR DERIVATIVES WITH CELL-BINDING MOLECULES, NOVEL DISORAZOLE DERIVATIVES, PROCESSES OF MANUFACTURING AND USES THEREOF
  申请人：Æterna Zentaris GmbH

  公开号：EP2066679A1

  公开（公告）日：2009-06-10
• 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.