(2S)-2-amino-1-oxazolo[4,5-b]pyridin-2-yl-butan-1-ol | 477940-26-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 恶唑并吡啶类
• 英文名称: (2S)-2-amino-1-oxazolo[4,5-b]pyridin-2-yl-butan-1-ol
• 英文别名: (2S)-2-amino-1-([1,3]oxazolo[4,5-b]pyridin-2-yl)butan-1-ol
• CAS: 477940-26-4
• 化学式: C₁₀H₁₃N₃O₂
• 分子量: 207.232
• InChiKey: VGFUWKUEUFAMNM-UUEFVBAFSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.2
• 重原子数：
  15
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  85.2
• 氢给体数：
  2
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  (2S)-2-amino-1-oxazolo[4,5-b]pyridin-2-yl-butan-1-ol 、 2-(1-methyl-cyclopentylmethyl)-4-morpholin-4-yl-4-oxo-butyric acid 、 戴斯-马丁氧化剂 在 N-甲基吗啉 、 1-羟基苯并三唑 、 sodium thiosulfate 、 1,2-二氯乙烷 作用下， 以 二氯甲烷 、 碳酸氢钠 、 乙酸乙酯 为溶剂， 生成 2-(1-Methyl-cyclopentylmethyl)-4-morpholin-4-yl-N-[-(oxazolo[4,5-b]pyridine-2-carbonyl)-propyl]-4-oxo-butyramide
  参考文献：
  名称：

  Novel compounds and compositions as cathepsin inhibitors

  摘要：

  本发明涉及新型卡特普西林S抑制剂、其药学上可接受的盐和N-氧化物，它们作为治疗剂的用途以及它们的制备方法。

  公开号：

  US20030105099A1

文献信息

• [EN] AMIDINO COMPOUNDS AS CYSTEINE PROTEASE INHIBITORS<br/>[FR] COMPOSES AMIDINO SERVANT D'INHIBITEURS DE PROTEASES A CYSTEINE
  申请人：AXYS PHARMACEUTICALS

  公开号：WO2004108661A1

  公开（公告）日：2004-12-16

  The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.

  本发明涉及一种抑制半胱氨酸蛋白酶的化合物，特别是包括B、K、L、F和S半胱氨酸蛋白酶，因此在治疗由这些蛋白酶介导的疾病方面具有用处。本发明涉及包含这些化合物的药物组合物以及其制备方法。
• [EN] HALOALKYL CONTAINING COMPOUNDS AS CYSTEINE PROTEASE INHIBITORS<br/>[FR] COMPOSES CONTENANT UN HALOALKYLE UTILISE COMME INHIBITEURS DE CYSTEINE PROTEASE
  申请人：AXYS PHARM INC

  公开号：WO2005028454A1

  公开（公告）日：2005-03-31

  The application is directed to haloalkyl-substituted compounds of Formula (I), wherein R1, R1a, R2, R3, R4’ and E are as defined in the claims. The compounds are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. Pharmaceutical compositions comprising these compounds and their use are also disclosed.

  该应用程序针对式(I)的卤代烷基取代化合物，其中R1、R1a、R2、R3、R4'和E如索权中所定义。这些化合物是半胱氨酸蛋白酶的抑制剂，特别是卡托普斯蛋白酶B、K、L、F和S，因此可用于治疗由这些蛋白酶介导的疾病。还公开了包含这些化合物的药物组合物及其用途。
• Amidino compounds as cysteine protease inhibitors
  申请人：Graupe Michael

  公开号：US20070105892A1

  公开（公告）日：2007-05-10

  The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.

  本发明涉及一种抑制半胱氨酸蛋白酶的化合物，特别是cathepsins B、K、L、F和S，因此在治疗由这些蛋白酶介导的疾病方面具有用处。本发明涉及包含这些化合物的药物组合物和其制备过程。
• Silinane compounds as cysteine protease inhibitors
  申请人：Link O. John

  公开号：US20070088001A1

  公开（公告）日：2007-04-19

  The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is also directed to pharmaceutical compositions comprising these compounds and processes for preparing them. The present invention is also directed to the use of these inhibitors in combination with a therapy that causes a deleterious immune response in patients receiving the therapy.

  本发明涉及一种抑制半胱氨酸蛋白酶的化合物，特别是抑制B、K、L、F和S型蛋白酶，因此可用于治疗由这些蛋白酶介导的疾病。本发明还涉及包含这些化合物的制药组合物和其制备方法。本发明还涉及在治疗引起患者免疫反应不良的疗法中与这些抑制剂的联合使用。
• Haloalkyl Containing Compounds as Cysteine Protease Inhibitors
  申请人：Link O. John

  公开号：US20070276019A1

  公开（公告）日：2007-11-29

  The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.

  本发明涉及一种抑制半胱氨酸蛋白酶的化合物，尤其是对B、K、L、F和S型猫蛋白酶具有抑制作用，因此可用于治疗由这些蛋白酶介导的疾病。本发明涉及包含这些化合物的药物组合物以及制备它们的过程。