(I+/-R)-I+/--Amino-N-methyl-3-pyridinepropanamide | 851509-49-4

• 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: (I+/-R)-I+/--Amino-N-methyl-3-pyridinepropanamide
• 英文别名: (2R)-2-amino-N-methyl-3-pyridin-3-ylpropanamide
• CAS: 851509-49-4
• 化学式: C₉H₁₃N₃O
• 分子量: 179.22
• InChiKey: CDYPEXJFPUHKFD-MRVPVSSYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.4
• 重原子数：
  13
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  68
• 氢给体数：
  2
• 氢受体数：
  3

文献信息

• [EN] INHIBITORS OF DIPEPTIDYL PEPTIDASE IV<br/>[FR] INHIBITEURS DE LA DIPEPTIDYL-PEPTIDASE IV
  申请人：ASTRAZENECA AB

  公开号：WO2005040095A1

  公开（公告）日：2005-05-06

  The invention relates to compounds of the formula (I) or pharmaceutically-acceptable salts thereof wherein Ar, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 and R 8 have any of the meanings defined in the description, which possess dipeptidyl peptidase IV (DPP-IV) inhibitory activity and accordingly have value in the treatment of disease states associated with DPP-IV activity, such as diabetes mellitus. Processes for the preparation of said compounds, intermediates in said processes, pharmaceutical compositions containing said compounds or salts, and the use of said compounds or salts are also described.

  该发明涉及式（I）的化合物或其药学上可接受的盐，其中Ar，R1，R2，R3，R4，R5，R6，R7和R8具有描述中定义的任何含义，这些化合物具有二肽基肽酶IV（DPP-IV）抑制活性，因此在治疗与DPP-IV活性相关的疾病状态，如糖尿病等方面具有价值。还描述了制备该化合物的方法，该方法中间体，含有该化合物或其盐的药物组合物以及使用该化合物或其盐的用途。
• 3-substituted pyrrolidines useful as inhibitors of matrix metalloproteinases
  申请人：——

  公开号：US20020037859A1

  公开（公告）日：2002-03-28

  The present invention provides novel 3-substituted pyrrolidines of the formula 1 useful in as inhibitors of matrix metallo-proteinases (MMPs). Pharmaceutical compositions containing said compounds as well as methods of treating disease states responding to inhibition of matrix metalloproteinase are also claimed herein.

  本发明提供了新型的3-取代吡咯烷化合物，其化学式为1，可用作基质金属蛋白酶（MMPs）的抑制剂。本文还声明了含有该化合物的制药组合物以及治疗对基质金属蛋白酶抑制有反应的疾病状态的方法。
• Prodrugs of aspartyl protease inhibitors
  申请人：VERTEX PHARMACEUTICALS INCORPORATED

  公开号：EP1944300A2

  公开（公告）日：2008-07-16

  The present invention relates to prodrugs of a class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of prodrugs of HIV aspartyl protease inhibitors characterized by favorable aqueous solubility, high oral bioavailability and facile in vivo generation of the active ingredient. This invention also relates to pharmaceutical compositions comprising these prodrugs. The prodrugs and pharmaceutical compositions of this invention are particularly well suited for decreasing the pill burden and increasing patient compliance. This invention also relates to methods of treating mammals with these prodrugs and pharmaceutical compositions.

  本发明涉及一类属于天冬氨酰蛋白酶抑制剂的磺胺类药物的原药。在一个实施方案中，本发明涉及一类新型的 HIV 天冬氨酰蛋白酶抑制剂原药，其特点是具有良好的水溶性、高口服生物利用度和活性成分易于在体内生成。本发明还涉及包含这些原药的药物组合物。本发明的原药和药物组合物尤其适用于减轻药片负担和提高患者依从性。本发明还涉及用这些原药和药物组合物治疗哺乳动物的方法。
• Sulphonamide derivatives as prodrugs of aspartyl protease inhibitors
  申请人：VERTEX PHARMACEUTICALS INCORPORATED

  公开号：EP0933372B1

  公开（公告）日：2007-12-26
• SULPHONAMIDE DERIVATIVES AS PRODRUGS OF ASPARTYL PROTEASE INHIBITORS
  申请人：Tung Roger Dennis

  公开号：US20100124543A1

  公开（公告）日：2010-05-20

  The present invention relates to prodrugs of a class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of prodrugs of HIV aspartyl protease inhibitors characterized by favorable aqueous solubility, high oral bioavailability and facile in vivo generation of the active ingredient. This invention also relates to pharmaceutical compositions comprising these prodrugs. The prodrugs and pharmaceutical compositions of this invention are particularly well suited for decreasing the pill burden and increasing patient compliance. This invention also relates to methods of treating mammals with these prodrugs and pharmaceutical compositions.