3-hydrazinocarbonyl-propionic acid ethyl ester

• 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: 3-hydrazinocarbonyl-propionic acid ethyl ester
• 英文别名: ethyl 4-hydrazino-4-oxobutanoate；ethyl 4-hydrazinyl-4-oxobutanoate
• 化学式: C₆H₁₂N₂O₃
• mdl: MFCD01365918
• 分子量: 160.173
• InChiKey: DZUKQJAVQCGPAL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.1
• 重原子数：
  11
• 可旋转键数：
  5
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.666
• 拓扑面积：
  81.4
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  [2-[(3R,5S)-1-(3-acetyloxy-2,2-dimethylpropyl)-7-chloro-5-(2,3-dimethoxyphenyl)-2-oxo-5H-4,1-benzoxazepin-3-yl]acetyl] 2,2-dimethylpropanoate 、 3-hydrazinocarbonyl-propionic acid ethyl ester 在 三乙胺 作用下， 反应 2.0h， 生成 ethyl 4-({2-[(3R,5S)-1-(3-acetoxy-2,2-dimethylpropyl)-7-chloro-5-(2,3-dimethoxyphenyl)-1,2,3,5-tetrahydro-2-oxo-4,1-benzoxazepin-3-yl]acetyl}hydrazino)-4-oxobutanoate
  参考文献：
  名称：

  EP1650201

  摘要：

  公开号：
• 作为产物：
  描述：

  丁二酸单乙酯 在 1-羟基苯并三唑 、 盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺 、 肼 、 环己烯 作用下， 以 乙腈 为溶剂， 以93%的产率得到3-hydrazinocarbonyl-propionic acid ethyl ester
  参考文献：
  名称：

  一种制备羧酸酰肼的新方法。

  摘要：

  制备羧酸酰肼的标准方法是在醇溶液中酯的肼解。然而，当应用于α，β-不饱和酯时，主要产物通常是由不希望的迈克尔型环化反应产生的吡唑烷酮。据报道，用于从酸直接制备酰肼的其他替代方法效率低下。我们开发了一种有效且通用的方法，包括预形成活化的酯和/或酰胺，然后与肼反应，以制备包括α，β-不饱和酸在内的酰肼。该方法在温和条件下以优异的产率和纯度得到所需的酰肼。

  DOI：

  10.1021/jo026288n

文献信息

• Methods for treating an inflammatory condition or inhibiting JNK
  申请人：——

  公开号：US20040127536A1

  公开（公告）日：2004-07-01

  This invention is generally directed to Indazole Derivatives having the following structure: 1 or pharmaceutically acceptable salt thereof, wherein R 1 , R 2 and A are as defined herein. Such compounds have utility in the treatment of a wide range of diseases and disorders that are responsive to JNK inhibition, such as an inflammatory disease or disorder. Thus, methods of treating such diseases and disorders are also disclosed, as are pharmaceutical compositions containing one or more compounds of the above compounds.

  这项发明通常涉及吲唑衍生物，具有以下结构： 1 或药用可接受的盐，其中R 1 ，R 2 和A如本文所述定义。这类化合物在治疗对JNK抑制剂有响应的广泛疾病和障碍，如炎症性疾病或障碍中具有用途。因此，还披露了治疗这些疾病和障碍的方法，以及包含一个或多个上述化合物的药物组合物。
• Indazole compounds, compositions thereof and methods of treatment therewith
  申请人：Bhagwat S. Shripad

  公开号：US20050009876A1

  公开（公告）日：2005-01-13

  This invention is generally directed to the use of Indazole Compounds for treating or preventing diseases associated with protein kinases, including tyrosine kinases, such as proliferative diseases, inflammatory diseases, abnormal angiogenesis and diseases related thereto, atherosclerosis, macular degeneration, diabetes, obesity, pain and others. The methods comprise the administration to a patient in need thereof of an effective amount of an indazole compound that inhibits, modulates or regulates tyrosine kinase signal transduction. Novel indazole compounds or pharmaceutically acceptable salt thereof are presented herein.

  这项发明通常涉及使用吲唑化合物来治疗或预防与蛋白激酶相关的疾病，包括酪氨酸激酶，诸如增殖性疾病、炎症性疾病、异常血管生成及其相关疾病、动脉硬化、黄斑变性、糖尿病、肥胖、疼痛等。这些方法包括向有需要的患者施用有效量的吲唑化合物，以抑制、调节或控制酪氨酸激酶信号转导。本文中提供了一种新型的吲唑化合物或其药用可接受的盐。
• Indazole derivatives as JNK inhibitors and compositions and methods related thereto
  申请人：——

  公开号：US20020103229A1

  公开（公告）日：2002-08-01

  Compounds having activity as selective inhibitors of JNK are disclosed. The compounds of this invention are indazole derivatives having the following structure: 1 wherein R 1 , R 2 and A are as defined herein. Such compounds have utility in the treatment of a wide range of conditions that are responsive to JNK inhibition. Thus, methods of treating such conditions are also disclosed, as are pharmaceutical compositions containing one or more compounds of the above compounds.

  本发明公开了作为JNK选择性抑制剂的化合物。本发明的化合物是吲唑衍生物，具有以下结构： 1 其中R 1 ，R 2 和A如本文所述定义。此类化合物在治疗对JNK抑制产生响应的广泛病症方面具有用途。因此，还公开了治疗此类病症的方法，以及包含一个或多个上述化合物的药物组合物。
• Benzoxazepine Compound
  申请人：Marui Shogo

  公开号：US20080227770A1

  公开（公告）日：2008-09-18

  A compound represented by the formula [1]: wherein ring A and ring B each represent an optionally substituted benzene ring; ring C represents an optionally further substituted aromatic ring; R 1 represents a lower alkyl group optionally substituted with an optionally substituted hydroxyl group; X 1a represents a bond or optionally substituted lower alkylene; X 1b represents a bond or optionally substituted lower alkylene; x 2 represents a bond, —O— or —S—; X 3 represents a bond or an optionally substituted divalent hydrocarbon group; Y represents an optionally esterified or amidated carboxyl group, or a salt thereof. The compound of the formula [I] is safer and has more potent lipid lowering activity such as squalene synthase inhibitory activity (cholesterol lowering activity) and triglyceride lowering activity, and thus it is a compound useful as an agent for preventing or treating hyperlipemia.

  一种由公式[1]表示的化合物：其中环A和环B分别表示可选择性取代的苯环；环C表示可选择性进一步取代的芳香环；R1表示可选择性取代的较低的烷基，其中还可选择性地取代有一个或多个羟基基团；X1a表示一个键或可选择性取代的较低的烷基烯；X1b表示一个键或可选择性取代的较低的烷基烯；x2表示一个键，-O-或-S-；X3表示一个键或可选择性取代的双价碳氢基团；Y表示可选择性酯化或酰胺化的羧基，或其盐。公式[I]的化合物更安全，并具有更强的降脂活性，如角鲨烷合酶抑制活性（降低胆固醇活性）和三酰甘油降低活性，因此它是一种有用的化合物，可用作预防或治疗高脂血症的药物。
• Methods for treating, preventing and managing chronic lymphocytic leukemia with indazole compounds
  申请人：Bennett Brydon

  公开号：US20070060616A1

  公开（公告）日：2007-03-15

  This invention is generally directed to the use of Indazole Compounds for treating or preventing chronic lymphocytic leukemia. The methods comprise the treatment or prevention of chronic lymphocytic leukemia comprising administering an effective amount of an indazole compound, or a pharmaceutically acceptable salt or composition thereof, to a patient in need thereof.

  这项发明通常是针对使用吲唑类化合物治疗或预防慢性淋巴细胞白血病。该方法包括向需要治疗或预防慢性淋巴细胞白血病的患者给予有效量的吲唑类化合物，或其药学上可接受的盐或组合物。