(3R)-N~2~-(cyclopropylmethyl)-N~1~-hydroxy-3-(3-hydroxybenzyl)-N~4~-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-L-aspartamide

• 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: (3R)-N~2~-(cyclopropylmethyl)-N~1~-hydroxy-3-(3-hydroxybenzyl)-N~4~-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-L-aspartamide
• 英文别名: (2S,3R)-2-(cyclopropylmethylamino)-N-hydroxy-N'-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-3-[(3-hydroxyphenyl)methyl]butanediamide
• 化学式: C₂₄H₂₉N₃O₅
• 分子量: 439.5
• InChiKey: UACUZULRKJKTHE-CZYKHXBRSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.8
• 重原子数：
  32
• 可旋转键数：
  9
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.42
• 拓扑面积：
  131
• 氢给体数：
  6
• 氢受体数：
  6

文献信息

• Inhibitors of ADAMTS4 or ADAMTS5 for use in preventing or treating cardiac remodeling and chronic heart failure
  申请人：Universitetet i Oslo

  公开号：US10322143B2

  公开（公告）日：2019-06-18

  The present invention provides an inhibitor of an ADAMTS proteoglycanase for use in treating or preventing cardiac remodeling or for use in treating or preventing heart failure in a subject. In particular, the present invention provides an inhibitor of ADAMTS4 or ADAMTS5 for use in treating or preventing cardiac remodeling or chronic heart failure in a subject with cardiac remodeling or with chronic heart failure, or with a condition that may lead to cardiac remodeling and/or chronic heart failure. Also provided is a method of treating or preventing cardiac remodeling or treating or preventing heart failure which method comprises administering to a subject in need thereof a therapeutically effective amount of an inhibitor of an ADAMTS proteoglycanase. Also provided is the use of an inhibitor of an ADAMTS proteoglycanase in the manufacture of a medicament for treating or preventing cardiac remodeling or treating or preventing heart failure.

  本发明提供了一种ADAMTS蛋白聚糖酶抑制剂，用于治疗或预防心脏重塑或用于治疗或预防受试者的心力衰竭。特别是，本发明提供了一种ADAMTS4或ADAMTS5的抑制剂，用于治疗或预防患有心脏重塑或慢性心力衰竭或可能导致心脏重塑和/或慢性心力衰竭的病症的受试者的心脏重塑或慢性心力衰竭。还提供了一种治疗或预防心脏重塑或治疗或预防心衰的方法，该方法包括向有需要的受试者施用治疗有效量的 ADAMTS 蛋白聚糖酶抑制剂。还提供了一种ADAMTS蛋白聚糖酶抑制剂在制造治疗或预防心脏重塑或治疗或预防心衰的药物中的用途。
• INHIBITORS OF ADAMTS4 OR ADAMTS5 FOR USE IN PREVENTING OR TREATING CARDIAC REMODELING AND CHRONIC HEART FAILURE
  申请人：UNIVERSITETET I OSLO

  公开号：US20160158271A1

  公开（公告）日：2016-06-09

  The present invention provides an inhibitor of an ADAMTS proteoglycanase for use in treating or preventing cardiac remodeling or for use in treating or preventing heart failure in a subject. In particular, the present invention provides an inhibitor of ADAMTS4 or ADAMTS5 for use in treating or preventing cardiac remodeling or chronic heart failure in a subject with cardiac remodeling or with chronic heart failure, or with a condition that may lead to cardiac remodeling and/or chronic heart failure. Also provided is a method of treating or preventing cardiac remodeling or treating or preventing heart failure which method comprises administering to a subject in need thereof a therapeutically effective amount of an inhibitor of an ADAMTS proteoglycanase. Also provided is the use of an inhibitor of an ADAMTS proteoglycanase in the manufacture of a medicament for treating or preventing cardiac remodeling or treating or preventing heart failure.