(4S)-5-amino-4-methyl-5-oxopentanoic acid

• 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: (4S)-5-amino-4-methyl-5-oxopentanoic acid
• 化学式: C₆H₁₁NO₃
• 分子量: 145.16
• InChiKey: XWBFWUVUWQLRKB-BYPYZUCNSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.5
• 重原子数：
  10
• 可旋转键数：
  4
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.67
• 拓扑面积：
  80.4
• 氢给体数：
  2
• 氢受体数：
  3

文献信息

• SELF-ASSEMBLING MOLECULES THAT ACCUMULATE IN ACIDIC TUMOR MICROENVIRONMENTS
  申请人：The Ohio State University

  公开号：US20140363378A1

  公开（公告）日：2014-12-11

  Disclosed are compositions that contain a plurality of biocompatible self-assembling molecules that transform from isolated molecules or spherical micelles in the circulation into cylindrical nanofibers in the acidic extracellular environment of tumors which can be used to achieve a higher relative concentration of imaging, drug delivery, or radiotherapeutic agents at the tumor site compared to non-tumor tissues. This transition is rapid and reversible, indicating the system is in thermodynamic equilibrium.

  揭示了包含多种生物相容性自组装分子的组合物，这些分子在循环中从孤立分子或球形胶束转变为肿瘤酸性细胞外环境中的圆柱形纳米纤维，可用于在肿瘤部位实现成像、药物传递或放射治疗剂的相对浓度高于非肿瘤组织。这种转变是快速且可逆的，表明系统处于热力学平衡状态。
• NOVEL BICYCLIC NITROGEN CONTAINING HETEROARYL TGR5 RECEPTOR MODULATORS
  申请人：Robl Jeffrey A.

  公开号：US20140080788A1

  公开（公告）日：2014-03-20

  Novel compounds of Formula I:or an enantiomer, diastereomer, tautomer, prodrug or salt thereof, wherein m, Q, T, U, V, ring A, X, Y, R 3 , R 4 , R 4a , R 5a , R 5b , R 5c , R 5d , R 5e , R 6a , R 6b , and R 6c are defined herein, are provided which are TGR5 G protein-coupled receptor modulators. TGR5 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring TGR5 G protein-coupled receptor modulator therapy. Thus, the disclosure also concerns compositions comprising these novel compounds and methods of treating diseases or conditions related to the activity of the TGR5 G protein-coupled receptor by using any of these novel compounds or a composition comprising any of such novel compounds.

  本发明提供了一种公式I的新化合物：或其对映异构体、顺反异构体、互变异构体、前药或其盐，其中m、Q、T、U、V、环A、X、Y、R3、R4、R4a、R5a、R5b、R5c、R5d、R5e、R6a、R6b和R6c的定义如本文所述，这些化合物是TGR5 G蛋白偶联受体调节剂。 TGR5 G蛋白偶联受体调节剂在治疗、预防或减缓需要TGR5 G蛋白偶联受体调节剂治疗的疾病方面具有用途。因此，本公开还涉及包含这些新化合物的组合物以及使用任何这些新化合物或包含任何这些新化合物的组合物来治疗与TGR5 G蛋白偶联受体活性相关的疾病或病症的方法。
• [EN] ANTIBODY DRUG CONJUGATES USING MATES TECHNOLOGY FOR DELIVERING CYTOTOXIC AGENTS<br/>[FR] CONJUGUÉS ANTICORPS-MÉDICAMENT UTILISANT UNE TECHNOLOGIE DE COUPLAGE POUR ADMINISTRER DES AGENTS CYTOTOXIQUES
  申请人：BIOHAVEN THERAPEUTICS LTD

  公开号：WO2022246086A1

  公开（公告）日：2022-11-24

  Among other things, the present disclosure provides technologies for site-directed conjugation of various moieties of interest to target agents. In some embodiments, the present disclosure utilizes target binding moieties to provide high conjugation efficiency and selectivity. In some embodiments, provided technologies are useful for preparing antibody conjugates.

  除其他事项外，本公开提供了用于将各种感兴趣的物质定向结合到目标试剂上的技术。在某些实施例中，本公开利用目标结合物质提供高结合效率和选择性。在某些实施例中，提供的技术对于制备抗体结合物很有用。
• Thrombospondin 1-binding peptide
  申请人：DAIICHI SANKYO COMPANY, LIMITED

  公开号：US11149066B2

  公开（公告）日：2021-10-19

  Provided is a compound that can promote angiogenesis by inhibiting the function of TSP1, and is useful for the treatment or prophylaxis of diseases such as critical limb ischemia. Specifically provided is a macrocyclic polypeptide represented by formula (I) [wherein A is selected from the linking groups A1 to A6; Xaa1 is a residue of an aliphatic amino acid, an aromatic amino acid, a basic amino acid, a neutral amino acid, or an acidic amino acid, or is absent; Xaa2 is a residue of an aromatic amino acid or a neutral amino acid; Xaa3 is a residue of an aliphatic amino acid, an aromatic amino acid, or a basic amino acid; Xaa4 is Ser, Thr, Ala, or mS; Xaa5 is Gly or Ser; Xaa6 is a residue of a basic amino acid or a neutral amino acid; Xaa7 is a residue of a neutral amino acid or an acidic amino acid; Xaa8 is a residue of an aromatic amino acid; Xaa9 is a residue of an aliphatic amino acid, a neutral amino acid, or an aromatic amino acid; Xaa10 is a residue of a basic amino acid, an aliphatic amino acid, an aromatic amino acid, or a neutral amino acid; Xaa11 is a residue of an aromatic amino acid; and Xaa12 is a residue of an aliphatic amino acid, an aromatic amino acid, or a basic amino acid], or a pharmacologically acceptable salt thereof.

  本发明提供了一种化合物，该化合物可通过抑制 TSP1 的功能促进血管生成，并可用于治疗或预防危重肢体缺血等疾病。 具体而言，提供了一种由式（I）代表的大环多肽 [其中 A 选自连接基团 A1 至 A6；Xaa1 是脂肪族氨基酸、芳香族氨基酸、碱性氨基酸、中性氨基酸或酸性氨基酸的残基，或者不存在；Xaa2 是芳香族氨基酸或中性氨基酸的残基；Xaa3 是脂肪族氨基酸、芳香族氨基酸或碱性氨基酸的残基； Xaa4 是 Ser、Thr、Ala 或 mS； Xaa5 是 Gly 或 Ser； Xaa6 是碱性氨基酸或中性氨基酸的残基；Xaa7 是中性氨基酸或酸性氨基酸的残基； Xaa8 是芳香族氨基酸的残基； Xaa9 是脂肪族氨基酸、中性氨基酸或芳香族氨基酸的残基；Xaa10 是碱性氨基酸、脂肪族氨基酸、芳香族氨基酸或中性氨基酸的残基； Xaa11 是芳香族氨基酸的残基；以及 Xaa12 是脂肪族氨基酸、芳香族氨基酸或碱性氨基酸的残基]，或其药理学上可接受的盐。
• PSEUDO-DIPEPTIDES COMME INHIBITEURS DE MMP
  申请人：Commissariat à l'Énergie Atomique et aux Énergies Alternatives

  公开号：EP2470514B1

  公开（公告）日：2017-07-12