Fmoc-Dap(ivDde)-OH

• 分子结构分类: 有机化合物 - 苯类化合物 - 芴
• 英文名称: Fmoc-Dap(ivDde)-OH
• 英文别名: (2S)-3-[[1-(4,4-dimethyl-2,6-dioxocyclohexylidene)-3-methylbutyl]amino]-2-(9H-fluoren-9-ylmethoxycarbonylamino)propanoic acid
• 化学式: C₃₁H₃₆N₂O₆
• 分子量: 532.637
• InChiKey: HLIFXCXTXPXGNH-VWLOTQADSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.83
• 重原子数：
  39.0
• 可旋转键数：
  9.0
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.42
• 拓扑面积：
  121.8
• 氢给体数：
  3.0
• 氢受体数：
  6.0

反应信息

• 作为反应物：
  描述：

  Fmoc-Dap(ivDde)-OH 在 4-二甲氨基吡啶 、 N,N'-二环己基碳二亚胺 、 Wang resin 作用下， 以 DMF (N,N-dimethyl-formamide) 为溶剂， 反应 96.0h， 生成 tetrakis(acetonitrile)copper(II) hexafluiorophosphate
  参考文献：
  名称：

  EP1489081

  摘要：

  公开号：

文献信息

• [EN] HYDROPHILIC ANTIBODY-DRUG CONJUGATES<br/>[FR] CONJUGUÉS ANTICORPS-MÉDICAMENT HYDROPHILES
  申请人：SEATTLE GENETICS INC

  公开号：WO2015123679A1

  公开（公告）日：2015-08-20

  Hydrophilic Linkers, Drug-Linker compounds, Drug-Ligand Conjugate compounds and Ligand-Linkers and methods of making and using the same are provided.

  亲水性连接剂、药物-连接剂化合物、药物-配体共轭化合物和配体-连接剂以及其制备和使用方法。
• Polymeric prodrugs
  申请人：Complex Biosystems GmbH

  公开号：EP1579873A1

  公开（公告）日：2005-09-28

  A molecule is disclosed having the following structure: wherein T is D or A D being a residue of an amine containing biologically active molecule and A being a leaving group.

  揭示了具有以下结构的分子：其中T为D或AD，是含有生物活性分子的胺基残基，A为离去基团。
• Analogues of Trypsin Inhibitor SFTI-1 with Disulfide Bridge Substituted by Various Length of Carbonyl Bridges
  作者：Anna Legowska、Elzbieta Bulak、Anna Jaskiewicz、Izabella Maluch、Michal Sieracki、Magdalena Wysocka、Adam Lesner、Krzysztof Rolka

  DOI：10.2174/092986610792231483

  日期：2010.10.1

  analogues of trypsin inhibitor SFTI-1 was synthesized by the solid phase method. In these analogues disulfide bridge Cys3 - Cys11 present in native inhibitor was replaced by different-sized carbonyl bridges formed by the amino groups of the side chain of Lys, Orn, Dab or Dap located in positions 3 and/or 11. All analogues appeared to be potent trypsin inhibitors. The values of association equilibrium

  通过固相法合成了八种新的胰蛋白酶抑制剂SFTI-1单环类似物。在这些类似物中，天然抑制剂中存在的二硫键Cys3-Cys11被位于3和/或11位上的Lys，Orn，Dab或Dap侧链的氨基形成的不同大小的羰基桥所取代。是有效的胰蛋白酶抑制剂。牛β-胰蛋白酶测定的缔合平衡常数值范围为10（8）-10（9）M（-1），最高（3.90×10（9）M（-1）），适用于含有Lys和Dap的类似物在上述位置。获得的结果清楚地表明，该氧化还原稳定修饰在蛋白酶抑制剂的结构中具有良好的耐受性。
• [EN] SKELETAL MUSCLE DELIVERY PLATFORMS AND METHODS OF USE<br/>[FR] PLATEFORMES D'ADMINISTRATION À DES MUSCLES SQUELETTIQUES ET MÉTHODES D'UTILISATION
  申请人：ARROWHEAD PHARMACEUTICALS INC

  公开号：WO2022056269A1

  公开（公告）日：2022-03-17

  The present disclosure relates to delivery platforms that specifically and efficiently direct payloads to skeletal muscle cells in a subject, in vivo. The delivery platforms diclosed herein include targeting ligands (such as compounds that have affinity for integrins, including alpha- v-beta-6) and pharmacokinetic/pharmacodynamic (PK/PD) modulators, to facilitate the delivery of payloads to cells, including to skeletal muscle cells. Suitable payloads for use in the delivery platforms disclosed herein include RNAi agents, which can be linked or conjugated to the delivery platofrms, and when delivered in vivo, provide for the inhibition of gene expression in skeletal muscle cells. Pharmaceutical compositions that include the skeletal muscle cell delivery platform are also described, as well as methods of use for the treatment of various diseases and disorders where delivery of a therapeutic payload to a skeletal muscle cell is desirable.

  本公开涉及将有效载荷有针对性地且高效地引导至体内骨骼肌细胞的传递平台。所述传递平台包括靶向配体（例如具有亲和力的化合物，包括α-v-β-6整合素）和药代动力学/药效学（PK/PD）调节剂，以促进有效载荷传递到细胞，包括骨骼肌细胞。适用于本公开的传递平台的有效载荷包括RNAi剂，可以链接或结合到传递平台上，在体内传递时，可以抑制骨骼肌细胞的基因表达。还描述了包括骨骼肌细胞传递平台的药物组合物，以及用于治疗各种疾病和疾病的方法，其中传递治疗有效载荷至骨骼肌细胞是可取的。
• [EN] LIPID CONJUGATES FOR THE DELIVERY OF THERAPEUTIC AGENTS<br/>[FR] CONJUGUÉS LIPIDIQUES POUR L'ADMINISTRATION D'AGENTS THÉRAPEUTIQUES
  申请人：ARROWHEAD PHARMACEUTICALS INC

  公开号：WO2022056273A1

  公开（公告）日：2022-03-17

  Disclosed herein are compounds according to Formula (I) comprising PK/PD modulators for delivery of oligonucleotide-based agents, e.g., double stranded RNAi agents, to certain cell types, such for example skeletal muscle cells, in vivo. The PK/PD modulators disclosed herein, when conjugated to an oligonucleotide-based therapeutic or diagnostic agent, such as an RNAi agent, can enhance the delivery of the composition to the specified cells being targeted to facilitate the inhibition of gene expression in those cells.

  本文公开了公式（I）中的化合物，包括PK/PD调节剂，用于将基于寡核苷酸的制剂（例如双链RNAi制剂）递送到体内某些细胞类型，例如骨骼肌细胞。本文所披露的PK/PD调节剂与基于寡核苷酸的治疗或诊断制剂（如RNAi制剂）结合后，可以增强将该组合物递送到特定的目标细胞，以促进在这些细胞中抑制基因表达。