(S)-tert-butyl 3-(tert-butoxycarbonylamino)-4-hydroxybutanoate

• 分子结构分类: 有机化合物 - 脂质和类脂质分子 - 脂肪酰基
• 英文名称: (S)-tert-butyl 3-(tert-butoxycarbonylamino)-4-hydroxybutanoate
• 英文别名: tert-butyl 4-hydroxy-3-[(2-methylpropan-2-yl)oxycarbonylamino]butanoate
• 化学式: C₁₃H₂₅NO₅
• 分子量: 275.34
• InChiKey: VYLKHZZDXASXLR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.1
• 重原子数：
  19
• 可旋转键数：
  8
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.85
• 拓扑面积：
  84.9
• 氢给体数：
  2
• 氢受体数：
  5

文献信息

• [EN] HETEROARYL BUTANOIC ACID DERIVATIVES AS LTA4H INHIBITORS<br/>[FR] DÉRIVÉS D'ACIDE HÉTÉROARYL BUTANOÏQUE EN TANT QU'INHIBITEURS DE LA LTA4H
  申请人：NOVARTIS AG

  公开号：WO2015092740A1

  公开（公告）日：2015-06-25

  The present invention describes novel heteroaryl butanoic acid derivatives that are good drug candidates especially with regard to leukotriene A4 hydrolase (LTA4H). The present invention also relates to pharmaceutical compositions comprising said novel heteroaryl butanoic acid derivatives, methods of using said compounds in the treatment of various diseases and disorders, and processes for preparing the said novel compounds.

  本发明描述了新颖的杂环烷基丁酸衍生物，特别是在白三烯A4水解酶（LTA4H）方面具有良好的药物候选性。本发明还涉及包含所述新颖的杂环烷基丁酸衍生物的药物组合物，使用这些化合物治疗各种疾病和疾病的方法，以及制备这些新颖化合物的方法。
• METHOD FOR MANUFACTURING DIPEPTIDYL PEPTIDASE-IV INHIBITOR AND INTERMEDIATE
  申请人：Kwak Woo Young

  公开号：US20120016126A1

  公开（公告）日：2012-01-19

  The present invention relates to an improved method for manufacturing dipeptidyl peptidase-IV inhibitor and intermediate. The present invention allows reduction of production costs by reacting low cost reagents, improves yield and is adaptable for mass production.

  本发明涉及一种改进的二肽基胰岛素释放肽酶-IV抑制剂及中间体制备方法。本发明通过使用低成本试剂反应，降低生产成本，提高产量，并适用于大规模生产。
• [EN] CYSTEINE PROTEASE CAPTURING AGENTS<br/>[FR] AGENTS DE CAPTURE DE PROTÉASE À CYSTÉINE
  申请人：STICHTING NL KANKER INST

  公开号：WO2014007632A1

  公开（公告）日：2014-01-09

  The invention concerns cysteine protease capturing agents capable of highly selective and irreversible binding of the corresponding cysteine protease. Such compounds may have utility in fundamental biological research and diagnostics, e.g. involving labeled or immobilized versions of such compounds, and they may also have potential utility in therapy, basedon competitive inhibition of the cysteine protease, as will be readily apparent to those skilled in the art. The present inventors have discovered that such capturing agents can be obtained by modification of a cleavage fragment of a 'natural' substrate for the cysteine protease of interest, said modification involving the introduction of a propargyl moiety in such a way that the terminal alkyne group is positioned to allow for interaction with the free thiol group of the cysteine residue at the active site of the protease.

  本发明涉及半胱氨酸蛋白酶捕获剂，能够高度选择性和不可逆地结合对应的半胱氨酸蛋白酶。这些化合物可能在基础生物研究和诊断中有用，例如涉及这些化合物的标记或固定化版本，它们也可能在治疗中具有潜在用途，基于对半胱氨酸蛋白酶的竞争性抑制，这对熟练的技术人员来说是显而易见的。本发明人发现，通过修改半胱氨酸蛋白酶感兴趣的“天然”底物的裂解片段，可以获得这样的捕获剂，该修饰涉及以这样的方式引入丙炔基官能团，以使末端炔基团位于蛋白酶活性位点的半胱氨酸残基与自由巯基团相互作用的位置。
• INHIBITORS OF CARNITINE PALMITOYLTRANSFERASE AND TREATING CANCER
  申请人：Pauls Heinz W.

  公开号：US20100105900A1

  公开（公告）日：2010-04-29

  A CPT inhibitor compound is represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof: or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating a subject having cancer comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.

  一种CPT抑制剂化合物由结构式(I)或其药学上可接受的盐所代表：或其药学上可接受的盐。一种制药组合物包括由结构式(I)或其药学上可接受的盐所代表的化合物。一种治疗患有癌症的受试者的方法包括向该受试者施用由结构式(I)或其药学上可接受的盐所代表的治疗有效量的化合物。
• IMPROVED METHOD FOR MANUFACTURING DIPEPTIDYL PEPTIDASE-IV INHIBITOR AND INTERMEDIATE
  申请人：Dong-A Pharmaceutical Co., Ltd.

  公开号：EP2415754A2

  公开（公告）日：2012-02-08

  The present invention relates to an improved method for manufacturing dipeptidyl peptidase-IV inhibitor and intermediate. The present invention allows reduction of production costs by reacting low cost reagents, improves yield and is adaptable for mass production.

  本发明涉及一种制造二肽基肽酶-IV 抑制剂和中间体的改进方法。本发明通过使用低成本试剂进行反应，降低了生产成本，提高了产量，并适用于大规模生产。