[(3R)-5-methoxy-4-[(2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl]-1-oxaspiro[2.5]octan-6-yl] N-(2-chloroacetyl)carbamate

• 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)-5-methoxy-4-[(2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl]-1-oxaspiro[2.5]octan-6-yl] N-(2-chloroacetyl)carbamate
• 化学式: C₁₉H₂₈ClNO₆
• 分子量: 401.9
• InChiKey: MSHZHSPISPJWHW-DFIKQBLQSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  27
• 可旋转键数：
  7
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.79
• 拓扑面积：
  89.7
• 氢给体数：
  1
• 氢受体数：
  6

文献信息

• MODIFIED OR POLYMER-CONJUGATED FUMAGILLOL METAP2 INHIBITORS FOR USE IN IMPROVING OR RESTORING INSULIN SENSITIVITY
  申请人：Syndevrx, Inc.

  公开号：EP3574922A1

  公开（公告）日：2019-12-04

  The present invention relates to modified or polymer conjugated MetAP2 inhibitors for use in improving or restoring insulin sensitivity in a subject in need thereof, wherein the subject is overweight or obese. Also disclosed is the modified or polymer conjugated MetAP2 inhibitors for use in methods of preventing, inducing, causing or increasing weight loss, treating obesity and/or treating metabolic syndrome or in methods of improving glycemic control, reducing insulin levels and/or improving leptin sensitivity.

  本发明涉及改性或聚合物共轭 MetAP2 抑制剂，用于改善或恢复有需要的受试者的胰岛素敏感性，其中受试者超重或肥胖。本发明还公开了用于预防、诱导、导致或增加体重减轻、治疗肥胖和/或治疗代谢综合征的方法或用于改善血糖控制、降低胰岛素水平和/或改善瘦素敏感性的方法的改性或聚合物共轭 MetAP2 抑制剂。
• POLYMER-CONJUGATED METAP2 INHIBITORS, AND THERAPEUTIC METHODS OF USE THEREOF
  申请人：Syndevrx, Inc.

  公开号：EP3858385A2

  公开（公告）日：2021-08-04

  One aspect of the invention provides polymer conjugated MetAP2 inhibitors. While not being bound by any particular theory, it is believed that coupling the MetAP2 inhibitory core via the linkers described herein provides compounds with superior efficacy to the parent small molecules and superior pharmacokinetic profiles. In one aspect of the invention, the polymer conjugated MetAP2 inhibitors are useful in methods of treating disease, comprising administering to a subject in need thereof a therapeutically effective amount of a polymer conjugated MetAP2 inhibitor.

  本发明的一个方面提供了聚合物共轭 MetAP2 抑制剂。虽然不受任何特定理论的束缚，但我们相信，通过本文所述的连接体偶联 MetAP2 抑制核心，可提供疗效优于母体小分子和药代动力学特征优越的化合物。在本发明的一个方面，聚合物共轭 MetAP2 抑制剂可用于治疗疾病的方法中，包括向有需要的受试者施用治疗有效量的聚合物共轭 MetAP2 抑制剂。
• METAP2 inhibitors and methods of treating obesity
  申请人：SynDevRx, Inc.

  公开号：US10588904B2

  公开（公告）日：2020-03-17

  The present invention relates to modified or polymer conjugated MetAP2 inhibitors. The present invention also relates to methods of preventing, inducing, causing or increasing weight loss, treating obesity and/or treating metabolic syndrome utilizing the modified or polymer conjugated MetAP2 inhibitors. The present invention also relates to methods of improving insulin sensitivity and glycemic control, reducing insulin levels and/or improving leptin sensitivity utilizing the modified or polymer conjugated MetAP2 inhibitors.

  本发明涉及改性或聚合物共轭 MetAP2 抑制剂。本发明还涉及利用改性或聚合物共轭 MetAP2 抑制剂预防、诱导、导致或增加体重减轻、治疗肥胖和/或治疗代谢综合征的方法。本发明还涉及利用改性或聚合物共轭 MetAP2 抑制剂改善胰岛素敏感性和血糖控制、降低胰岛素水平和/或改善瘦素敏感性的方法。
• MODIFIED OR POLYMER-CONJUGATED FUMAGILLOL METAP2 INHIBITORS FOR USE IN TREATING OBESITY
  申请人：Syndevrx, Inc.

  公开号：EP2984085B1

  公开（公告）日：2019-07-17
• METAP2 INHIBITORS AND METHODS OF TREATING OBESITY
  申请人：SynDevRx, Inc.

  公开号：US20200155545A1

  公开（公告）日：2020-05-21

  The present invention relates to modified or polymer conjugated MetAP2 inhibitors. The present invention also relates to methods of preventing, inducing, causing or increasing weight loss, treating obesity and/or treating metabolic syndrome utilizing the modified or polymer conjugated MetAP2 inhibitors. The present invention also relates to methods of improving insulin sensitivity and glycemic control, reducing insulin levels and/or improving leptin sensitivity utilizing the modified or polymer conjugated MetAP2 inhibitors.