N-pyruvoyl-alanine | 2392-63-4

• 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: N-pyruvoyl-alanine
• 英文别名: N-Pyruvoyl-alanin；DL-2-(2-Oxo-propionylamino)-propionsaeure；N-Pyruvoyl-DL-alanin；Pyruvyl-dl-alanin；Inakt.α-(α-Oxo-propionylamino)-propionsaeure；methyloxalyl-D-alanine；pyruvyl-alanine；2-(2-Oxopropanoylamino)propanoic acid
• CAS: 2392-63-4
• 化学式: C₆H₉NO₄
• 分子量: 159.142
• InChiKey: LRBARJMHQPHPQP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.6
• 重原子数：
  11
• 可旋转键数：
  3
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  83.5
• 氢给体数：
  2
• 氢受体数：
  4

安全信息

• 海关编码：
  2924199090

反应信息

• 作为反应物：
  描述：

  N-pyruvoyl-alanine 、 2-氨基-2-苯基乙酸 在 水 作用下， 生成 DL-丙氨酰-DL-丙氨酸 、 alkaline earth salt of/the/ methylsulfuric acid
  参考文献：
  名称：

  Herbst; Shemin, Journal of Biological Chemistry, 1943, vol. 147, p. 545

  摘要：

  DOI：
• 作为产物：
  描述：

  DL-2-(2,2-bis-acetylamino-propionylamino)-propionic acid 生成 N-pyruvoyl-alanine
  参考文献：
  名称：

  The Condensation of α-Keto Acids and Acetamide¹

  摘要：

  DOI：

  10.1021/ja01275a067

文献信息

• Nitric Oxide Releasing Pyruvate Compounds, Compositions and Methods of Use
  申请人：Garvey David S.

  公开号：US20080287407A1

  公开（公告）日：2008-11-20

  The invention describes novel nitrosated and/or nitrosylated pyruvate compounds and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated pyruvate compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one pyruvate compound and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one pyruvate compound, that is optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating diseases resulting from oxidative stress, diabetes, reperfusion injury following ischemia, preservation of tissues, organs, organ parts and/or limbs.

  该发明描述了新颖的硝化和/或亚硝化丙酮酸盐及其药用可接受盐，以及包含至少一种硝化和/或亚硝化丙酮酸化合物的新型组合物，以及可选地，至少一种捐赠、转移或释放一氧化氮、刺激内源性一氧化氮合成、提高内源性内皮源性舒张因子水平或是一氧化氮合酶底物的化合物，和/或至少一种治疗剂。该发明还提供了包含至少一种丙酮酸化合物和至少一种捐赠、转移或释放一氧化氮、提高内源性内皮源性舒张因子水平、刺激内源性一氧化氮合成或是一氧化氮合酶底物和/或至少一种治疗剂的新型组合物。该发明还提供了包含至少一种丙酮酸化合物的新型试剂盒，该丙酮酸化合物可选地硝化和/或亚硝化，以及可选地至少一种一氧化氮供体和/或至少一种治疗剂。该发明还提供了治疗由氧化应激、糖尿病、缺血后再灌注损伤、组织、器官、器官部分和/或肢体保护引起的疾病的方法。
• Assays, methods and means
  申请人：Maxwell Patrick Henry

  公开号：US20100272726A1

  公开（公告）日：2010-10-28

  A novel class of hydroxylases is described having the amino acid sequence of SEQ ID NO: 2, 4, 6 and 8, and variants and fragments thereof having HIF hydroxylation activity. The polypeptides of the invention have in particular prolyl hydroxylase activity. An assay method monitors the interaction of the HIF hydroxylase with a substrate. Modulators of HIF hydroxylase are provided for use in the treatment of a condition associated with increased or decreased HIF levels or activity or for the treatment of a condition where it is desirable to modulate HIF levels or activity.

  本文描述了一种新型的羟化酶，其氨基酸序列为SEQ ID NO：2、4、6和8，以及具有HIF羟化活性的变体和片段。本发明的多肽特别具有脯氨酸羟化酶活性。一种测定方法监测HIF羟化酶与底物的相互作用。提供了HIF羟化酶的调节剂，用于治疗与HIF水平或活性增加或减少相关的疾病，或用于治疗需要调节HIF水平或活性的疾病。
• INHIBITORS OF SERINE PROTEASES, PARTICULARLY HCV NS3-NS4A PROTEASE
  申请人：Perni Robert B.

  公开号：US20130116169A1

  公开（公告）日：2013-05-09

  The present invention relates to compounds that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The invention further relates to compositions comprising these compounds either for ex vivo use or for administration to a patient suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a patient by administering a composition comprising a compound of this invention. The invention further relates to processes for preparing these compounds.

  本发明涉及抑制丝氨酸蛋白酶活性的化合物，特别是抑制丙型肝炎病毒NS3-NS4A蛋白酶活性的化合物。因此，它们通过干扰丙型肝炎病毒的生命周期发挥作用，并且也可用作抗病毒药物。本发明还涉及包含这些化合物的组合物，用于体外使用或用于治疗患有HCV感染的患者。本发明还涉及通过给患者施用包含本发明化合物的组合物来治疗HCV感染的方法。本发明还涉及制备这些化合物的过程。
• Sustained release dosage form having latex coating and method of making the same
  申请人：ABBOTT LABORATORIES

  公开号：EP1579853A2

  公开（公告）日：2005-09-28

  Dosage form unit is provided to deliver one or more beneficial agents into a fluid, such as liquid enteral nutritional product. The dosage form unit includes a core containing at least one beneficial agent, preferably a marker dye, which is dispersible in the fluid. The core also contains a compatible binding agent to bind the beneficial agent together. Additional components of the core may include a plasticizer, a standard flow agent, a lubricant, additional tableting aids and at least one hydrophilic agent. A latex coating encases the core. The latex coating includes a mixture containing a substantially hydrophobic base material, preferably formed from an emulsion of cellulose acetate microspheres, which is capable of defining a matrix-type membrane, and at least one hydrophilic component being dispersible in the fluid. A dispersible beneficial agent is preferred as one of the hydrophilic components of the latex coating to allow immediate release of the beneficial agent therefrom. A method of making the dosage form unit also is provided.

  所提供的剂型单元可将一种或多种有益制剂输送到液体中，如液体肠内营养产品。该剂型装置包括一个内核，内核含有至少一种可分散在液体中的有益制剂，最好是标记染料。核心还含有一种兼容的结合剂，可将有益制剂结合在一起。核心的其他成分可包括增塑剂、标准流动剂、润滑剂、其他制片助剂和至少一种亲水剂。乳胶涂层包裹芯材。乳胶涂层包括一种混合物，其中包含一种基本疏水的基质材料，最好是由醋酸纤维素微球乳液形成，它能够形成基质型膜，以及至少一种可在流体中分散的亲水成分。乳胶涂层的亲水成分之一最好是可分散的有益剂，以便有益剂能立即从涂层中释放出来。此外，还提供了一种制造剂型单元的方法。
• Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
  申请人：VERTEX PHARMACEUTICALS INCORPORATED

  公开号：EP2573083A1

  公开（公告）日：2013-03-27

  The present invention relates to compounds of formula I-A and I-B that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The invention further relates to compositions comprising these compounds either for ex vivo use for administration to a patient suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a patient by administering a composition comprising a compound of this invention. The invention further relates to processes for preparing these compounds.

  本发明涉及式 I-A 和 I-B 的化合物 可抑制丝氨酸蛋白酶活性，尤其是丙型肝炎病毒 NS3-NS4A 蛋白酶的活性。因此，它们通过干扰丙型肝炎病毒的生命周期发挥作用，也可用作抗病毒药物。本发明还涉及包含这些化合物的组合物，这些组合物既可用于体内外给丙型肝炎病毒感染患者用药，也可用于体内外给丙型肝炎病毒感染患者用药。本发明还涉及通过施用包含本发明化合物的组合物治疗患者 HCV 感染的方法。本发明还涉及制备这些化合物的工艺。