N-((8-methoxy-3,6-dioxaoctyloxy)carbonyl)-L-leucine N-hydroxysuccinimide ester | 854402-78-1

• 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-((8-methoxy-3,6-dioxaoctyloxy)carbonyl)-L-leucine N-hydroxysuccinimide ester
• 英文别名: (2,5-dioxopyrrolidin-1-yl) (2S)-2-[2-[2-(2-methoxyethoxy)ethoxy]ethoxycarbonylamino]-4-methylpentanoate
• CAS: 854402-78-1
• 化学式: C₁₈H₃₀N₂O₉
• 分子量: 418.444
• InChiKey: CKFOHHGLGBYDHB-AWEZNQCLSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.3
• 重原子数：
  29
• 可旋转键数：
  16
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.78
• 拓扑面积：
  130
• 氢给体数：
  1
• 氢受体数：
  9

反应信息

• 作为反应物：
  描述：

  (3S)-3-amino-N-cyclopropyl-2-hydroxy-4-phenylbutanamide hydrochloride 、 N-((8-methoxy-3,6-dioxaoctyloxy)carbonyl)-L-leucine N-hydroxysuccinimide ester 在 三乙胺 作用下， 以 二氯甲烷 为溶剂， 生成 ((1S)-1-((((1S)-1-benzyl-3-cyclopropylamino-2-hydroxy-3-oxopropyl)amino)carbonyl)-3-methylbutyl)carbamic acid 8-methoxy-3,6-dioxaoctyl ester
  参考文献：
  名称：

  Molecular design to enhance the penetration into the retina via ocular instillation

  摘要：

  To investigate the molecular design of drugs that have good penetration into the retina from anterior segment of the eye via ocular instillation, we optimized the length of methoxyethylene glycol chain (mEG) in the P3 region of an oral bioavailable calpain inhibitor SNJ-1945 (2) as a model compound. Modulation of the mEG length led to the optimal balance between hydrophilicity and lipophilicity and provided the compound with higher retinal exposure via ocular instillation. Incorporation of a mEG moiety would be a useful and convenient approach to attain high intraocular penetration. (C) 2008 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2008.08.089
• 作为产物：
  描述：

  8-methoxy-3,6-dioxaoctyl N-succinimidyl carbonate 生成 N-((8-methoxy-3,6-dioxaoctyloxy)carbonyl)-L-leucine N-hydroxysuccinimide ester
  参考文献：
  名称：

  LISSENCEPHALY THERAPEUTIC AGENT

  摘要：

  公开号：

  EP2647386B1

文献信息

• COMPOSITION FOR TREATMENT AND/OR PREVENTION OF PERIPHERAL NERVE DISORDER
  申请人：OSAKA CITY UNIVERSITY

  公开号：US20190314320A1

  公开（公告）日：2019-10-17

  The present invention provides a means for treating and/or preventing peripheral nerve disorder by facilitating regeneration of peripheral nerves. Specifically, the present invention provides a composition for treating and/or preventing peripheral nerve disorder comprising a compound represented by the general formula (I): wherein R 1 is lower alkyl substituted with lower alkoxy, lower alkyl substituted with a heterocyclic group, a heterocyclic group, or a group represented by the formula (IIa): R 4 O—R 5  m (IIa) wherein R 4 is lower alkyl, R 5 is lower alkylene, and m is an integer of 1 to 6; R 2 is lower alkyl optionally substituted with phenyl; and R 3 is lower alkyl optionally substituted with halogen, lower alkoxy, or phenyl; condensed polycyclic hydrocarbon; or hydrogen.

  本发明提供了一种治疗和/或预防外周神经障碍的方法，通过促进外周神经再生。具体地，本发明提供了一种用于治疗和/或预防外周神经障碍的组合物，包括由通式（I）表示的化合物： 其中R1为与低烷氧基取代的低烷基，与杂环基取代的低烷基，杂环基，或由式（IIa）表示的基团： R4O—R5m（IIa） 其中R4为低烷基，R5为低烷基烯，m为1至6的整数； R2为可选择地取代苯基的低烷基；和 R3为可选择地取代卤素，低烷氧基，或苯基的低烷基；缩合多环碳氢化合物；或氢。
• Alpha-ketoamide derivative, and production method and use thereof
  申请人：Shirasaki Yoshihisa

  公开号：US20070004643A1

  公开（公告）日：2007-01-04

  The present invention provides a compound represented by the formula (I): (wherein R 1 is a lower alkyl substituted by a lower alkoxy or a heterocyclic group, or a heterocyclic group; R 2 is a lower alkyl optionally substituted by a phenyl; and R 3 is a lower alkyl optionally substituted by a halogen, a lower alkoxy or a phenyl, or a fused polycyclic hydrocarbon group), which is well absorbed orally, exhibits durability of good blood level and has potent calpain inhibitory activity.

  本发明提供了一种化合物，其化学式表示为(I):(其中，R1是一个低烷基，该低烷基被低烷氧基或杂环基取代，或者是一个杂环基；R2是一个低烷基，可选地被苯基取代；R3是一个低烷基，可选地被卤素、低烷氧基或苯基取代，或者是一个融合的多环碳氢基)，该化合物口服吸收良好，血液水平持久，具有强大的钙蛋白酶抑制活性。
• ALPHA-KETOAMIDE DERIVATIVE, AND PRODUCTION METHOD AND USE THEREOF
  申请人：Senju Pharmaceutical Co., Ltd.

  公开号：EP1692098B1

  公开（公告）日：2009-10-28
• US7491705B2
  申请人：——

  公开号：US7491705B2

  公开（公告）日：2009-02-17
• US9371359B2
  申请人：——

  公开号：US9371359B2

  公开（公告）日：2016-06-21