Amidinophenylpyruvic acid | 10290-63-8

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: Amidinophenylpyruvic acid
• 英文别名: 4-amino-4-imino-2-oxo-3-phenylbutanoic acid
• CAS: 10290-63-8
• 化学式: C₁₀H₁₀N₂O₃
• 分子量: 206.2
• InChiKey: MPXCPPIJRDRZES-UHFFFAOYSA-N

物化性质

• 沸点：
  391.4±52.0 °C(Predicted)
• 密度：
  1.37±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.5
• 重原子数：
  15
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.1
• 拓扑面积：
  104
• 氢给体数：
  3
• 氢受体数：
  4

安全信息

• 海关编码：
  2925290090

文献信息

• [EN] POLYSUBUNIT OPIOID PRODRUGS RESISTANT TO OVERDOSE AND ABUSE<br/>[FR] PROMÉDICAMENTS D'OPIOÏDES À SOUS-UNITÉS MULTIPLES RÉSISTANTS AUX SURDOSES ET AUX ABUS
  申请人：ELYSIUM THERAPEUTICS INC

  公开号：WO2018170465A1

  公开（公告）日：2018-09-20

  The invention provides compositions and methods for the treatment or prevention of pain. Compositions provided are resistant to overdose and abuse. Compositions provided comprise two or more different molecules, where each molecule comprises at least one GI enzyme-labile opioid agonist releasing subunit comprising an opioid agonist that is covalently linked to at least one GI enzyme inhibitor subunit.

  这项发明提供了用于治疗或预防疼痛的组合物和方法。所提供的组合物具有抗过量和滥用的特性。所提供的组合物包括两种或两种以上不同的分子，其中每种分子至少包括一个至少含有一个胃肠酶敏感的阿片类受体激动剂释放亚基的阿片类受体激动剂，该阿片类受体激动剂与至少一个胃肠酶抑制剂亚基共价连接。
• Amidinophenylpyruvic acid derivatives
  申请人：AJINOMOTO CO. INC

  公开号：US20030109547A1

  公开（公告）日：2003-06-12

  An amidinophenylpyruvic acid derivative of the following formula, analogs thereof and pharmaceutically acceptable salts thereof have an excellent antagonistic effect against activated blood coagulation factor VII. 1

  以下是该公式的一种氨基苯丙酸衍生物，其类似物和药学上可接受的盐具有出色的对激活的凝血因子VII的拮抗作用。
• POLYSUBUNIT OPIOID PRODRUGS RESISTANT TO OVERDOSE AND ABUSE
  申请人：Elysium Therapeutics, Inc.

  公开号：US20170100390A1

  公开（公告）日：2017-04-13

  The invention provides compositions and methods for the treatment or prevention of pain. The invention provides constructs whereby hydrolysis of the construct by a specified gastrointestinal enzyme directly, or indirectly, releases an opioid when taken orally as prescribed. The gastrointestinal enzyme mediated release of opioid from constructs of the invention is designed to be attenuated in vivo via a saturation or inhibition mechanism when overdoses are ingested. The invention further provides constructs that are highly resistant to oral overdose, chemical tampering, and abuse via non-oral routes of administration.

  这项发明提供了用于治疗或预防疼痛的组合物和方法。该发明提供了构造物，通过指定的胃肠酶在口服时直接或间接地水解构造物释放阿片类物质。该发明中构造物中的胃肠酶介导的阿片类物质释放被设计为在体内通过饱和或抑制机制在摄入过量时减弱。该发明进一步提供了对口服过量、化学篡改和通过非口服途径滥用高度抵抗的构造物。
• [EN] AMIDINOPHENYLPYRUVIC ACID DERIVATIVE<br/>[FR] DERIVE DE L'ACIDE AMIDINOPHENYLPYRUVIQUE
  申请人：AJINOMOTO KK

  公开号：WO2001042199A1

  公开（公告）日：2001-06-14

  An amidinophenylpyruvic acid derivative represented by the following formula, its analogs and pharmaceutically acceptable salts thereof which have an excellent effect of inhibiting activated blood coagulation factor VII.

  以下是一个由下式表示的氨基甲酰苯丙酸衍生物，其类似物和药学上可接受的盐，具有优异的抑制活化血凝因子VII的效果。
• Combination therapy involving a sodium-hydrogen exchanger type 1 or NHE-1 inhibitor for use in treatment of ischemia
  申请人：Pfizer Products Inc.

  公开号：EP1226830A2

  公开（公告）日：2002-07-31

  The invention provdes methods of reducing tissue damage resulting from ischemia which comprise administering to a mammal in need of such reduction an effective amount of a combination, or a pharmaceutical composition comprising such combination, of an NHE-1 inhibitor and a second compound selected from the group consisting of: (a) a complement modulator, (b) a metabolic modulator, (c) an anti-apoptotic agent, (d) a nitric oxide synthase-related agent, and (e) an enzyme/protein modulator. The invention further provides pharmaceutical compositions comprising an amount of an NHE-1 inhibitor; an amount of a second compound selected from the group consisting of (a) a complement modulator, (b) a metabolic modulator, (c) an anti-apoptotic agent, (d) a nitric oxide synthase-related agent, and an enzyme/protein modulator selected from the group consisting of a protein kinase C activator, an endothelin converting enzyme inhibitor, a thrombin-activatable fibrinolysis inhibitor (TAFI) inhibitor, an activated thrombin-activatable fibrinolysis inhibitor (TAFIa) inhibitor, a Na+/Ca+2 exchanger isoform-1 (NCX-1) inhibitor, and a poly (ADP ribose) synthetase (PARS/PARP) inhibitor; and, preferably, a pharmaceutically acceptable pharmaceutically acceptable carrier, vehicle, or diluent. The invention further provides kits comprising an amount of a sodium-hydrogen exchanger type-1 inhibitor, and a pharmaceutically acceptable carrier, vehicle, or diluent in a first unit dosage form; an amount of a second compound selected from the group consisting of (a) a complement modulator, (b) a metabolic modulator, (c) an anti-apoptotic agent, (d) a nitric oxide synthase-related agent, and (e) an enzyme/protein modulator selected from the group consisting of a protein kinase C activator, an endothelin converting enzyme inhibitor, a thrombin-activatable fibrinolysis inhibitor (TAFI) inhibitor, an activated thrombin-activatable fibrinolysis inhibitor (TAFIa) inhibitor, a Na+/Ca+2 exchanger isoform-1 (NCX-1) inhibitor, and a poly (ADP ribose) synthetase (PARS/PARP) inhibitor, and a pharmaceutically acceptable carrier, vehicle, or diluent in a second unit dosage form; and a container.

  本发明提供了减少缺血导致的组织损伤的方法，该方法包括向需要减少损伤的哺乳动物施用有效量的 NHE-1 抑制剂和选自以下组别的第二种化合物的组合或包含这种组合的药物组合物：(a) 补体调节剂，(b) 代谢调节剂，(c) 抗凋亡剂，(d) 一氧化氮合酶相关剂，和 (e) 酶/蛋白调节剂。本发明进一步提供了药物组合物，其中包含一定量的 NHE-1 抑制剂；一定量的选自以下组别的第二种化合物：(a) 补体调节剂；(b) 代谢调节剂；(c) 抗凋亡剂；(d) 一氧化氮合酶相关剂；以及选自以下组别的酶/蛋白调节剂：蛋白激酶 C 激活剂、内皮素转换酶抑制剂、凝血酶活化性纤维蛋白溶解抑制剂（TAFI）抑制剂、活化的凝血酶活化性纤维蛋白溶解抑制剂（TAFIa）抑制剂、Na+/Ca+2 交换异构体-1（NCX-1）抑制剂和多（ADP 核糖）合成酶（PARS/PARP）抑制剂；以及，优选药学上可接受的载体、载体或稀释剂。本发明进一步提供了包含一定量的钠-氢交换剂型-1 抑制剂和药学上可接受的载体、载体或稀释剂的试剂盒，试剂盒为第一单位剂型；一定量的选自以下组别的第二种化合物：(a) 补体调节剂；(b) 代谢调节剂；(c) 抗细胞凋亡剂；(d) 一氧化氮合酶相关剂；(e) 酶/蛋白调节剂，选自以下组别：蛋白激酶 C 激活剂；内皮素转换酶抑制剂；凝血酶激活的可凝血酶抑制剂、凝血酶活化性纤维蛋白溶解抑制剂（TAFI）抑制剂、活化的凝血酶活化性纤维蛋白溶解抑制剂（TAFIa）抑制剂、Na+/Ca+2 交换异构体-1（NCX-1）抑制剂和聚（ADP 核糖）合成酶（PARS/PARP）抑制剂，以及药学上可接受的载体、载体或稀释剂组成的组；以及一个容器。