1-Methyl-2-pivaloyl-hydrazin | 31820-33-4

• 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: 1-Methyl-2-pivaloyl-hydrazin
• 英文别名: N',2,2-trimethylpropanehydrazide
• CAS: 31820-33-4
• 化学式: C₆H₁₄N₂O
• 分子量: 130.19
• InChiKey: FOQCTLKIEUXMCG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.7
• 重原子数：
  9
• 可旋转键数：
  2
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.83
• 拓扑面积：
  41.1
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  1-Methyl-2-(α-hydroxy-neopentyl)-diazen 在 盐酸 作用下， 以 乙醚 为溶剂， 生成 1-Methyl-2-pivaloyl-hydrazin
  参考文献：
  名称：

  Buettner,G.; Huenig,S., Chemische Berichte, 1971, vol. 104, p. 1088 - 1103

  摘要：

  DOI：

文献信息

• MODULATORS OF ALPHA-1 ANTITRYPSIN
  申请人：Vertex Pharmaceuticals Incorporated

  公开号：US20200361939A1

  公开（公告）日：2020-11-19

  The disclosure provides compounds useful for treating alpha-1 antitrypsin deficiency (AATD), according to formula (I): tautomers thereof, pharmaceutically acceptable salts of the compounds, pharmaceutically acceptable salts of the tautomers, deuterated derivatives of the compounds, deuterated derivatives of the tautomers, and deuterated derivatives of the salts, solid forms of those compounds and processes for making those compounds.

  该披露提供了用于治疗α-1抗胰蛋白酶缺乏症（AATD）的化合物，其化学式为（I）：它们的互变异构体，这些化合物的药用盐，这些互变异构体的药用盐，这些化合物的氘代衍生物，这些互变异构体的氘代衍生物，以及这些盐的氘代衍生物，这些化合物的固态形式以及制备这些化合物的方法。
• [EN] METHODS OF TREATMENT FOR ALPHA-1 ANTITRYPSIN DEFICIENCY<br/>[FR] PROCÉDÉS DE TRAITEMENT D'UNE DÉFICIENCE EN ALPHA-1 ANTITRYPSINE
  申请人：VERTEX PHARMA

  公开号：WO2021155087A1

  公开（公告）日：2021-08-05

  This application describes methods of treating alpha-1 antitrypsin deficiency (AATD) comprising administering Compound I, a deuterated derivative thereof, and/or a pharmaceutically acceptable salt thereof. The application also describes pharmaceutical compositions comprising Compound I, a deuterated derivative thereof, and/or a pharmaceutically acceptable salt thereof.

  该申请描述了治疗α-1抗胰蛋白酶缺乏症（AATD）的方法，包括给予化合物I，其氘代衍生物和/或其药用盐。该申请还描述了包括化合物I，其氘代衍生物和/或其药用盐的药物组合物。
• [EN] MRGX2 ANTAGONISTS<br/>[FR] ANTAGONISTES DE MRGX2
  申请人：GLAXOSMITHKLINE IP DEV LTD

  公开号：WO2022073905A1

  公开（公告）日：2022-04-14

  This invention relates to novel compounds according to Formula (I) which are antagonists of MrgX2, to pharmaceutical compositions containing them, and to their use in therapy for the treatment of MrgX2-mediated diseases and disorders.

  本发明涉及按照式（I）的新化合物，其是MrgX2的拮抗剂，以及包含它们的制药组合物，它们在治疗MrgX2介导的疾病和障碍方面的应用。
• Pyrazolyl-substituted pyridone compounds as serine protease inhibitors
  申请人：VERSEON CORPORATION

  公开号：US10189810B2

  公开（公告）日：2019-01-29

  There are provided inter alia pyrazolyl-substituted pyridone compounds, which exhibit biological activity, e.g., inhibitory action, against serine proteases, including thrombin and various kallikreins. There are additionally provided pharmaceutical compositions. There are additionally provided methods of treating and preventing certain diseases or disorders, which disease or disorder is amenable to treatment or prevention by the inhibition of serine proteases, including thrombin and various kallikreins.

  除其他外，还提供了吡唑基取代的吡啶酮化合物，这些化合物对丝氨酸蛋白酶（包括凝血酶和各种卡里克蛋白）具有生物活性，例如抑制作用。另外还提供了药物组合物。另外还提供了治疗和预防某些疾病或失调的方法，这些疾病或失调可通过抑制丝氨酸蛋白酶（包括凝血酶和各种卡里克蛋白）来治疗或预防。
• Peptidomimetic macrocycles
  申请人：Aileron Therapeutics, Inc.

  公开号：US10967042B2

  公开（公告）日：2021-04-06

  Provided herein are peptidomimetic macrocycles containing amino acid sequences with at least two modified amino acids that form an intramolecular cross-link that can help to stabilize a secondary structure of the amino acid sequence. Suitable sequences for stabilization include those with homology to the p53 protein. These sequences can bind to the MDM2 and/or MDMX proteins. Also provided herein are methods of using such macrocycles for the treatment of diseases and disorders, such as cancers or other disorders characterized by a low level or low activity of a p53 protein or high level of activity of a MDM2 and/or MDMX protein.

  本文提供的仿肽大环含有氨基酸序列，其中至少有两个修饰氨基酸形成分子内交联，有助于稳定氨基酸序列的二级结构。适合用于稳定的序列包括与 p53 蛋白同源的序列。这些序列可与 MDM2 和/或 MDMX 蛋白结合。本文还提供了使用此类大环用于治疗疾病和失调的方法，例如癌症或其它以p53蛋白低水平或低活性或MDM2和/或MDMX蛋白高水平活性为特征的失调。