N-Fmoc-1,4-丁二胺 氢溴酸盐 | 352235-99-5

• 分子结构分类: 有机化合物 - 苯类化合物 - 芴
• 中文名称: N-Fmoc-1,4-丁二胺 氢溴酸盐
• 中文别名: N-Fmoc-1,4-丁二胺氢溴酸盐
• 英文名称: N-Fmoc 1,4-butanediamine hydrobromide
• 英文别名: N-Fmoc-1,4-diaminobutane hydrobromide；N-Fmoc-1,4-butanediamine hydrobromide；9H-fluoren-9-ylmethyl N-(4-aminobutyl)carbamate;hydrobromide
• CAS: 352235-99-5
• 化学式: BrH*C₁₉H₂₂N₂O₂
• 分子量: 391.308
• InChiKey: IZGCBOCFUHJPMD-UHFFFAOYSA-N

物化性质

• 熔点：
  ~133°C (dec.)

计算性质

• 辛醇/水分配系数(LogP)：
  3.84
• 重原子数：
  24
• 可旋转键数：
  7
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.32
• 拓扑面积：
  64.4
• 氢给体数：
  3
• 氢受体数：
  3

安全信息

• WGK Germany：
  3

反应信息

• 作为反应物：
  描述：

  4-amino-6-[[2-(4-formylphenoxymethyl)benzoyl]amino]-2-methylquinoline 、 N-Fmoc-1,4-丁二胺 氢溴酸盐 在 N,N-二异丙基乙胺 作用下， 以 甲醇 为溶剂， 生成
  参考文献：
  名称：

  Synthesis and pharmacological evaluation of bivalent antagonists of the nociceptin opioid receptor

  摘要：

  Bivalent ligands constituted by two identical pharmacophores structurally related to the Nociceptin Opioid Receptor (NOPr) antagonist JTC-801 were synthesized and their binding affinities for NOPr were evaluated. The novel ligands are formed by two modified JTC-801 units linked by di-iminic and di-aminic spacers with length ranging from three to ten methylene units. Moreover, the synthesis and the pharmacological characterization were extended to the corresponding univalent ligands. The latter compounds consisted in a single modified JTC-801 unit and an alkyl or alkylamino or alkylimino tail. The purpose of this study is to feature the location and surroundings of the allosteric binding site(s) of pharmacophores containing the 4-aminoquinoline structure. Most important, the bivalent ligands were exploited to reveal the eventual occurrence of a supramolecular receptorial architecture of the NOPr.All the bivalent derivatives 4 and 5 proved to be active in the nanomolar range with no outstanding dependence on the chain length. They showed potencies from three to ten times higher than the corresponding monomers. Consequently, results clearly indicated a positive role of the second pharmacophore in the ligand-protein interaction. The pharmacological profile of I he monomers 7 and 8 clarified the contribution of the linker chain to NOP receptor affinity and suggested the presence of a lipophilic acidic site neighbouring the binding site of the JTC-like ligands.Selectivity of saturated compounds 5, 7, and 8 was tested by binding experiments on delta, kappa and mu opioid receptors. Results indicated a general loss of selectivity as compared to JTC-801. In the [(35)S]GTP gamma S binding assay, all the compounds revealed antagonistic properties at the NOP Receptor.In conclusion the present study set the basis for a systematic investigation on the structural modifications that can be introduced into novel ligands for NOPr and helped to feature the surrounds of the allosteric site of NOPr. (C) 2011 Elsevier Masson SAS. All rights reserved.

  DOI：

  10.1016/j.ejmech.2011.01.040

文献信息

• TARGETED MTOR INHIBITORS
  申请人：FORREST MARCUS LAIRD

  公开号：US20160279108A1

  公开（公告）日：2016-09-29

  The present invention is directed to drug conjugates of mTOR inhibitors comprising an mTOR inhibitor, such as rapamycin, conjugated to hyaluronic acid by a linker comprising an ester, carbonate, or carbamate. The present invention is also directed to pharmaceutical compositions comprising the drug conjugates, and methods of making and using the drug conjugates and the pharmaceutical compositions.

  本发明涉及mTOR抑制剂的药物共轭物，包括将mTOR抑制剂（如雷帕霉素）通过酯、碳酸酯或氨甲酸酯构成的连接剂与透明质酸共轭的药物。本发明还涉及包括药物共轭物的药物组合物，以及制备和使用药物共轭物和药物组合物的方法。
• HEPARAN SULFATE/HEPARIN MIMETICS WITH ANTI-CHEMOKINE AND ANTI-INFLAMMATORY ACTIVITY
  申请人：California Institute of Technology

  公开号：US20150038455A1

  公开（公告）日：2015-02-05

  The present disclosure provides for methods and compositions comprising a series of synthetic glycopolymers. The disclosure also relates to a kit which is suitable for carrying out the inventive methods.

  本公开提供了一系列合成糖聚合物的方法和组合物。该公开还涉及一种适用于执行创新方法的试剂盒。
• TAILORED GLYCOPOLYMERS AS ANTICOAGULANT HEPARIN MIMETICS
  申请人：California Institute of Technology

  公开号：US20150038436A1

  公开（公告）日：2015-02-05

  The present disclosure provides for methods and compositions comprising a series of synthetic glycopolymers. The disclosure also relates to a kit which is suitable for carrying out the inventive methods.

  本公开提供了一系列合成糖聚合物的方法和组合物。该公开还涉及一种适用于实施创新方法的试剂盒。
• [EN] AN OSTEOADSORPTIVE FLUOROGENIC SUBSTRATE OF CATHEPSIN K FOR IMAGING OSTEOCLAST ACTIVITY AND MIGRATION<br/>[FR] SUBSTRAT FLUOROGÈNE OSTÉOADSORBANT DE CATHEPSINE K POUR L'IMAGERIE DE L'ACTIVITÉ ET DE LA MIGRATION DES OSTÉOCLASTES
  申请人：UNIV CALIFORNIA

  公开号：WO2019018238A1

  公开（公告）日：2019-01-24

  In certain embodiments osteoadsorptive fluorogenic substrates of cathepsin K (or other proteases) are provided. Utilizing a bisphosphonate targeting moiety, the fluorogenic substrates provide effective bone-targeted protease sensor(s). In certain embodiments the "probes" comprise cleavable fluorophore-quencher pair linked by a cathepsin K (or other protease) peptide substrate and tethered to a bisphosphonate. Unlike existing probes that are cleared within a few days in vivo, the probes described herein (e.g., OFS-1) allow for monitoring resorption over the course of longer time periods with a single dose.

  在某些实施例中，提供了钙蛋白酶K（或其他蛋白酶）的骨吸收荧光底物。利用双磷酸盐靶向基团，荧光底物提供有效的靶向骨蛋白酶传感器。在某些实施例中，“探针”包括可切割的荧光团-猝灭剂对，由钙蛋白酶K（或其他蛋白酶）肽底物连接，并与双磷酸盐相连。与现有的在体内几天内被清除的探针不同，本文所述的探针（例如OFS-1）允许在单剂量下监测骨吸收的长时间进程。
• Reingungsgemisch zur Entfernung beziehungsweise Vermeidung von Insektenablagerungen auf Oberflächen
  申请人：EADS Deutschland GmbH

  公开号：EP2746378A1

  公开（公告）日：2014-06-25

  Die Erfindung betrifft ein Reinigungsgemisch zur Entfernung beziehungsweise Vermeidung von Insektenablagerungen auf Oberflächen, umfassend mindestens eine Protease in Kombination mit mindestens einer Chitinase und mindestens ein kompatibles Tensid.

  本发明涉及一种用于清除或防止昆虫在物体表面沉积的清洁混合物，它由至少一种蛋白酶、至少一种几丁质酶和至少一种相容的表面活性剂组成。