4-azaniumyl-3-hydroxy-5-phenylpentanoate

• 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: 4-azaniumyl-3-hydroxy-5-phenylpentanoate
• 化学式: C11H15NO3
• 分子量: 209.24
• InChiKey: JAJQQUQHMLWDFB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -2.1
• 重原子数：
  15
• 可旋转键数：
  5
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.36
• 拓扑面积：
  83.6
• 氢给体数：
  3
• 氢受体数：
  4

文献信息

• Solid phase method for synthesis peptide-spacer-lipid conjugates, conjugates synthesized thereby and targeted liposomes containing the same
  申请人：DEVELOPMENT CENTER FOR BIOTECHNOLOGY

  公开号：US20030229017A1

  公开（公告）日：2003-12-11

  A solid phase synthesis method for preparing peptide-spacer-lipid conjugates, the peptide-spacer-lipid conjugates synthesized by the method, and liposomes containing the peptide-spacer-lipid conjugates. The present invention provides a convenient solid phase synthesis method for preparing peptide-spacer-lipid conjugates and provides various linkage groups (such as amide group) for conjugating peptide, spacer and lipid, wherein the spacer may comprise PEG. Several advantages can be achieved, such as the synthetic procedure can be simplified, the synthesis process can be set to automation, the purification is easier in each reaction step, and the product losses can be reduced to minimal during synthesis. The present synthesis method is suitable for preparing a wide range of peptide-spacer-lipid conjugates, provides a peptide-spacer-lipid conjugate prepared by the solid phase synthesis method of the present invention, which can be incorporated into a liposome as the targeting moiety for liposomal drug delivery to specific cells, and provides a targeting liposome containing the present peptide-spacer-lipid conjugate.

  一种用于制备肽-间隔子-脂质共轭物的固相合成方法，所述方法合成的肽-间隔子-脂质共轭物，以及含有肽-间隔子-脂质共轭物的脂质体。本发明提供了一种便利的固相合成方法，用于制备肽-间隔子-脂质共轭物，并提供了各种连接基团（如酰胺基团）用于连接肽、间隔子和脂质，其中间隔子可以包括PEG。可以实现几项优点，例如合成过程可以简化，合成过程可以设定为自动化，每个反应步骤中的纯化更容易，并且在合成过程中产品损失可以降至最低。本合成方法适用于制备各种肽-间隔子-脂质共轭物，提供了一种由本发明的固相合成方法制备的肽-间隔子-脂质共轭物，可作为靶向单元被纳入脂质体，用于将脂质体药物传递到特定细胞，并提供了含有本肽-间隔子-脂质共轭物的靶向脂质体。
• Identification and use of protease inhibitors
  申请人：ELI LILLY AND COMPANY

  公开号：EP0652009A1

  公开（公告）日：1995-05-10

  β-amyloid peptide (βAF) production in cell culture and in vivo is inhibited by administering aspartyl protease inhibitors, particularly inhibitors of proteases of cathepsin D. Useful aspartyl protease inhibitors can be selected in a two-step assay, where test compounds are first screened for aspartyl protease inhibition activity in vitro in noncellular assays. Those test compounds which are found to display protease inhibition activity are then tested in cellular assays for βAP production inhibition. Those test compounds which are capable of inhibiting intracellular β-amyloid production may be incorporated in pharmaceutical compositions.

  β-淀粉样蛋白（βAF）在细胞培养和体内的产生受到阻断，通过给予天冬氨酸蛋白酶抑制剂，特别是半胱氨酸蛋白酶D的抑制剂。有用的天冬氨酸蛋白酶抑制剂可以在两步法测定中选择，其中首先在非细胞试验中筛选测试化合物是否具有体外天冬氨酸蛋白酶抑制活性。那些被发现具有蛋白酶抑制活性的测试化合物随后在细胞试验中进行βAP产生抑制的测试。那些能够抑制细胞内β-淀粉样蛋白产生的测试化合物可以被纳入药物组合物中。
• Antiviral agents
  申请人：Coates Jonathan Alan Victor

  公开号：US20090170926A1

  公开（公告）日：2009-07-02

  The present invention provides a method of treatment or prophylaxis of hepatitis B virus in a subject comprising administering an effective amount of a compound of formula ( 1 ) or a pharmaceutically acceptable derivative, salt or prodrug thereof. In addition, there is provided compounds of formula ( 1 ) and pharmaceutical compositions thereof. Further, methods of preparing compounds of formula ( 1 ) are disclosed.

  本发明提供了一种治疗或预防乙型肝炎病毒的方法，包括向受试者施用化合物（1）的有效量或其药学上可接受的衍生物、盐或前药。此外，还提供了化合物（1）及其药物组合物。此外，还公开了制备化合物（1）的方法。
• [EN] GLUCAGON SUPERFAMILY PEPTIDES EXHIBITING GLUCOCORTICOID RECEPTOR ACTIVITY<br/>[FR] PEPTIDES DE LA SUPERFAMILLE DU GLUCAGON PRÉSENTANT UNE ACTION SUR LES RÉCEPTEURS AUX GLUCOCORTICOÏDES
  申请人：UNIV INDIANA RES & TECH CORP

  公开号：WO2013074910A1

  公开（公告）日：2013-05-23

  Provided herein are glucagon superfamily peptides conjugated with GR ligands that are capable of acting at a glucocorticoid receptor. Also provided herein are pharmaceutical compositions and kits of the conjugates of the invention. Further provided herein are methods of treating a disease, e.g., a metabolic disorder, such as diabetes and obesity, comprising administering the conjugates of the invention.

  本文提供了与GR配体结合的葡萄糖素超家族肽，这些肽能够作用于糖皮质激素受体。本文还提供了该发明的结合物的药物组合物和工具包。此外，本文还提供了治疗疾病的方法，例如代谢紊乱，如糖尿病和肥胖，包括给予该发明的结合物。
• [EN] INSULIN RECEPTOR PARTIAL AGONISTS AND GLP-1 ANALOGUES<br/>[FR] AGONISTES PARTIELS DU RÉCEPTEUR DE L'INSULINE ET ANALOGUES DU GLP-1
  申请人：MERCK SHARP & DOHME

  公开号：WO2017205191A1

  公开（公告）日：2017-11-30

  The present invention provides compositions comprising insulin receptor partial agonists in association with GLP-1 analogues (e.g., liraglutide) as well as methods for using the compositions for example, to treat or prevent diabetes or to decrease body weight.

  本发明提供了包含胰岛素受体部分激动剂与GLP-1类似物（例如利拉鲁肽）的组合物，以及使用该组合物的方法，例如用于治疗或预防糖尿病或减轻体重。