L-Alanine, N-[(9H-fluoren-9-ylmethoxy)carbonyl]-N-2-propen-1-yl- | 923035-13-6

• 分子结构分类: 有机化合物 - 苯类化合物 - 芴
• 英文名称: L-Alanine, N-[(9H-fluoren-9-ylmethoxy)carbonyl]-N-2-propen-1-yl-
• 英文别名: (2S)-2-[9H-fluoren-9-ylmethoxycarbonyl(prop-2-enyl)amino]propanoic acid
• CAS: 923035-13-6
• 化学式: C₂₁H₂₁NO₄
• 分子量: 351.4
• InChiKey: DQEKHVILZICIBU-AWEZNQCLSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.9
• 重原子数：
  26
• 可旋转键数：
  7
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.24
• 拓扑面积：
  66.8
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• Stabilized insulinotropic peptides and methods of use
  申请人：Dana-Farber Cancer Institute, Inc.

  公开号：US10487129B2

  公开（公告）日：2019-11-26

  The present invention provides stably crosslinked insulinotropic polypeptides having superior and unexpected benefits in the treatment of conditions involving abnormal glucose homeostasis, e.g., type 2 diabetes and conditions relating to type 2 diabetes. Such benefits include, but are not limited to, extended polypeptide half-life, enhanced alpha-helicity, improved thermal stability and protease resistance, increased functional activity and pharmacologic properties, improved bioavailability when administered by any route, and improved bioavailability and gastrointestinal absorption when delivered orally, as compared to the corresponding unmodified polypeptides. The invention also provides compositions for administering the polypeptides of the invention, as well as methods for preparing and evaluating the polypeptides of the invention.

  本发明提供的稳定交联的促胰岛素多肽在治疗涉及葡萄糖平衡异常的病症（如2型糖尿病和与2型糖尿病有关的病症）方面具有意想不到的优越性。这些优点包括但不限于：与相应的未修饰多肽相比，延长了多肽的半衰期，增强了α-螺旋性，提高了热稳定性和抗蛋白酶能力，增加了功能活性和药理特性，通过任何途径给药时提高了生物利用度，口服给药时提高了生物利用度和胃肠道吸收。本发明还提供了施用本发明多肽的组合物，以及制备和评估本发明多肽的方法。
• STABILIZED INSULINOTROPIC PEPTIDES AND METHODS OF USE
  申请人：Dana-Farber Cancer Institute, Inc.

  公开号：EP2590997B1

  公开（公告）日：2018-04-04
• US9296805B2
  申请人：——

  公开号：US9296805B2

  公开（公告）日：2016-03-29
• US9695224B2
  申请人：——

  公开号：US9695224B2

  公开（公告）日：2017-07-04
• [EN] STABILIZED INSULINOTROPIC PEPTIDES AND METHODS OF USE<br/>[FR] PEPTIDES INSULINOTROPES STABILISÉS ET PROCÉDÉS D'UTILISATION
  申请人：DANA FARBER CANCER INST INC

  公开号：WO2012006598A2

  公开（公告）日：2012-01-12

  The present invention provides stably crosslinked insulionotropic polypeptides having superior and unexpected benefits in the treatment of conditions involving abnormal glucose homeostasis, e.g., type 2 diabetes and conditions relating to type 2 diabetes. Such benefits include, but are not limited to, extended polypeptide half-life, enhanced alpha-helicity, improved thermal stability and protease resistance, increased functional activity and pharmacologic properties, improved bioavailability when administered by any route, and improved bioavailability and gastrointestinal absorption when delivered orally, as compared to the corresponding unmodified polypeptides. The invention also provides compositions for administering the polypeptides of the invention, as well as methods for preparing and evaluating the polypeptides of the invention.