N-alpha-苯甲酰基-L-精氨酸乙酯盐酸盐 | 971-21-1

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: N-alpha-苯甲酰基-L-精氨酸乙酯盐酸盐
• 中文别名: N-苯甲酰基-L-精氨酸
• 英文名称: N^α-benzoyl-L-arginine ethyl ester
• 英文别名: N_α-benzoyl L-arginine ethyl ester；N_α-benzoyl-L-arginine ethyl ester；N^α-benzoyl-L-arginine ethyl ester；N^α-Bz-L-arginine ethyl ester；N²-benzoyl-L-arginine ethyl ester；α-N-benzoyl-L-arginine ethyl ester；Benzoyl-L-arginine ethyl ester；ethyl (2S)-2-benzamido-5-(diaminomethylideneamino)pentanoate
• CAS: 971-21-1
• 化学式: C₁₅H₂₂N₄O₃
• mdl: MFCD00398808
• 分子量: 306.365
• InChiKey: YQDHCCVUYCIGSW-LBPRGKRZSA-N

物化性质

• 密度：
  1.23±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.7
• 重原子数：
  22
• 可旋转键数：
  9
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  120
• 氢给体数：
  3
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  N-alpha-苯甲酰基-L-精氨酸乙酯盐酸盐 在 氨 作用下， 生成 N-Alpha-苯甲酰-L-精氨酰胺盐酸盐
  参考文献：
  名称：

  Dirr; Spaeth, Hoppe-Seyler's Zeitschrift fur Physiologische Chemie, 1935, vol. 237, p. 121,126

  摘要：

  DOI：
• 作为产物：
  描述：

  苯甲酰氯 在 盐酸 、 水 作用下， 生成 N-alpha-苯甲酰基-L-精氨酸乙酯盐酸盐
  参考文献：
  名称：

  Kimmel; Smith, Biochemical Preparations, 1958, vol. 6, p. 61,64

  摘要：

  DOI：

文献信息

• Compositions Comprising Enzyme-Cleavable Oxycodone Prodrug
  申请人：Jenkins Thomas E.

  公开号：US20120178773A1

  公开（公告）日：2012-07-12

  The embodiments provide Compound KC-7, N-1-[(S)-2-(oxycodone-6-enol-carbonyl-methyl-amino)-2-carbonyl-sarcosine-ethyl amine]-arginine-glycine-acetate, or acceptable salts, solvates, and hydrates thereof. The present disclosure also provides compositions, and their methods of use, where the \compositions comprise a prodrug, Compound KC-7, that provides controlled release of oxycodone. Such compositions can optionally provide a trypsin inhibitor that interacts with the enzyme that mediates the controlled release of oxycodone from the prodrug so as to attenuate enzymatic cleavage of the prodrug.

  提供了一种名为KC-7的化合物，N-1-[(S)-2-(氧可酮-6-烯醇-羰基-甲基-氨基)-2-羰基-肌氨酸-乙胺]-精氨酸-甘氨酸-乙酸盐，或其可接受的盐、溶剂化物和水合物。本公开还提供了包含前药的组合物及其使用方法，其中组合物包含前药KC-7，该前药能够控制释放氧可酮。这样的组合物可以选择性地提供一种胰蛋白酶抑制剂，该抑制剂与介导前药控制释放氧可酮的酶相互作用，以减弱前药的酶切。
• [EN] COMPOSITIONS COMPRISING ENZYME-CLEAVABLE OPIOID PRODRUGS AND INHIBITORS THEREOF<br/>[FR] COMPOSITIONS COMPRENANT DES PROMÉDICAMENTS OPIACÉS CLIVABLES PAR ENZYME ET LEURS INHIBITEURS
  申请人：PHARMACOFORE INC

  公开号：WO2011133149A1

  公开（公告）日：2011-10-27

  The present disclosure provides pharmaceutical compositions, and their methods of use, where the pharmaceutical compositions comprise a prodrug that provides enzymatically-controlled release of a drug and an enzyme inhibitor that interacts with the enzyme(s) that mediates the enzymatically-controlled release of the drug from the prodrug so as to attenuate enzymatic cleavage of the prodrug. The disclosure provides pharmaceutical compositions which comprise an enzyme inhibitor and a prodrug that contains an enzyme-cleavable moiety that, when cleaved, facilitates release of the drug.

  本公开提供了一种药物组合物及其使用方法，其中所述药物组合物包含一种前药，该前药能够提供通过酶控释放的药物，以及一种酶抑制剂，该酶抑制剂与介导从该前药酶控释放药物的酶相互作用，以减弱前药的酶裂解。本公开还提供了包含酶抑制剂和含酶可裂解基团的前药的药物组合物，所述酶可裂解基团在裂解时有助于药物的释放。
• [EN] COMPOSITIONS COMPRISING ENZYME-CLEAVABLE PRODRUGS OF ACTIVE AGENTS AND INHIBITORS THEREOF<br/>[FR] COMPOSITIONS COMPRENANT DES PROMÉDICAMENTS CLIVABLES PAR ENZYME DE PRINCIPES ACTIFS ET LEURS INHIBITEURS
  申请人：PHARMACOFORE INC

  公开号：WO2011133150A1

  公开（公告）日：2011-10-27

  The present disclosure provides pharmaceutical compositions, and their methods of use, where the pharmaceutical compositions comprise a prodrug that provides enzymatically-controlled release of a drug and an enzyme inhibitor that interacts with the enzyme(s) that mediates the enzymatically-controlled release of the drug from the prodrug so as to attenuate enzymatic cleavage of the prodrug. The disclosure provides pharmaceutical compositions which comprise an enzyme inhibitor and a prodrug that contains an enzyme-cleavable moiety that, when cleaved, facilitates release of the drug.

  本公开提供了一种药物组合物及其使用方法，其中所述药物组合物包含一种前药，该前药能够提供通过酶控释放的药物，以及一种酶抑制剂，该酶抑制剂与介导药物从该前药通过酶控释放的酶相互作用，以减弱前药的酶切。本公开还提供了一种包含酶抑制剂和前药的药物组合物，所述前药包含一个酶可切割的部分，切割后可促进药物的释放。
• COMPOSITIONS COMPRISING ENZYME-CLEAVABLE OPIOID PRODRUGS AND INHIBITORS THEREOF
  申请人：Jenkins Thomas E.

  公开号：US20110262355A1

  公开（公告）日：2011-10-27

  Pharmaceutical compositions and their methods of use are provided, where the pharmaceutical compositions comprise an opioid prodrug that provides enzymatically-controlled release of an opioid, and an enzyme inhibitor that interacts with the enzyme(s) that mediates the enzymatically-controlled release of the opioid from the opioid prodrug so as to attenuate enzymatic cleavage of the opioid prodrug.

  提供的药物组合物及其使用方法，其中药物组合物包括一种阿片类药物的前药，该前药提供酶控释放的阿片类药物，以及一种酶抑制剂，该酶抑制剂与介导阿片类药物前药酶控释放的酶相互作用，以减弱对阿片类药物前药的酶切。
• COMPOSITIONS COMPRISING ENZYME-CLEAVABLE PRODRUGS OF ACTIVE AGENTS AND INHIBITORS THEREOF
  申请人：Jenkins Thomas E.

  公开号：US20110262359A1

  公开（公告）日：2011-10-27

  The present disclosure provides pharmaceutical compositions, and their methods of use, where the pharmaceutical compositions comprise a prodrug that provides enzymatically-controlled release of a drug and an enzyme inhibitor that interacts with the enzyme(s) that mediates the enzymatically-controlled release of the drug from the prodrug so as to attenuate enzymatic cleavage of the prodrug. The disclosure provides pharmaceutical compositions which comprise an enzyme inhibitor and a prodrug that contains an enzyme-cleavable moiety that, when cleaved, facilitates release of the drug.

  本公开提供了药物组合物及其使用方法，其中药物组合物包括一种前药，该前药提供酶控释放药物的能力，以及一种酶抑制剂，与介导前药中药物酶控释放的酶相互作用，以减弱前药的酶解作用。该公开提供了包括酶抑制剂和含有酶可切割基团的前药的药物组合物，当切割时，促进药物释放。