2-(6-Amino-pyridin-3-ylmethyl)-3-mercapto-butyric acid

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: 2-(6-Amino-pyridin-3-ylmethyl)-3-mercapto-butyric acid
• 英文别名: 2-[(6-aminopyridin-3-yl)methyl]-3-sulfanylbutanoic acid
• 化学式: C₁₀H₁₄N₂O₂S
• 分子量: 226.3
• InChiKey: GYIYAOUGKJSCCG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1
• 重原子数：
  15
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  77.2
• 氢给体数：
  3
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  3-Acetylsulfanyl-2-(6-tert-butoxycarbonylamino-pyridin-3-ylmethyl)-butyric acid ethyl ester 在 氩 、 hydrochloride salt 作用下， 以 盐酸 为溶剂， 反应 1.0h， 以to afford 28.4 mg of the title compound as the hydrochloride salt的产率得到2-(6-Amino-pyridin-3-ylmethyl)-3-mercapto-butyric acid
  参考文献：
  名称：

  Pyridine mercapto carboxylic acids as carboxypeptidase U inhibitors

  摘要：

  本发明涉及式I的化合物，以及其药学上可接受的盐或溶剂或这些盐的溶剂，这些化合物抑制羧肽酶U，因此可用于预防和治疗与羧肽酶U相关的疾病。在进一步方面，本发明涉及用于治疗的本发明化合物；制备这种新化合物的过程；包含本发明化合物中至少一种作为活性成分的药物组合物；以及在制造上述医疗用途的药物中使用活性化合物。

  公开号：

  US07071175B1

文献信息

• [EN] NEW COMPOUNDS<br/>[FR] NOUVEAUX COMPOSES
  申请人：ASTRAZENECA AB

  公开号：WO2000066557A1

  公开（公告）日：2000-11-09

  The present invention relates to compounds of Formula (I), and pharmaceutically acceptable salts or solvates thereof, or solvates of such salts, which compounds inhibit carboxypeptidase U and thus can be used in the prevention and treatment of diseases associated with carboxypeptidase U. In further aspects, the invention relates to compounds of the invention for use in therapy; to processes for preparation of such new compounds; to pharmaceutical compositions containing at least one compound of the invention, or a pharmaceutically acceptable salt or solvate thereof, as active ingredient; and to the use of the active compounds in the manufacture of medicaments for the medical use indicated above.

  本发明涉及式(I)的化合物，以及其药学上可接受的盐或溶剂，或这些盐的溶剂，这些化合物抑制羧肽酶U，因此可用于预防和治疗与羧肽酶U相关的疾病。在进一步方面，本发明涉及用于治疗的本发明化合物；制备这些新化合物的过程；包含本发明化合物中至少一种，或其药学上可接受的盐或溶剂的制药组合物，作为活性成分；以及在制造上述医疗用途的药物中使用活性化合物。
• NEW COMPOUNDS
  申请人：AstraZeneca AB

  公开号：EP1180098A1

  公开（公告）日：2002-02-20
• US7071175B1
  申请人：——

  公开号：US7071175B1

  公开（公告）日：2006-07-04
• [EN] METHOD FOR MONITORING THE PROGRESSION OF FIBRINOLYSIS'646<br/>[FR] PROCÉDÉ DE SUIVI DE LA PROGRESSION DE LA FIBRINOLYSE
  申请人：ASTRAZENECA AB

  公开号：WO2009082340A1

  公开（公告）日：2009-07-02

  It is an object of the present invention to provide biological markers ( 'biomarkers' ) indicative for fibrinolysis. This object has been reached in that a method is provided for monitoring the progression of fibrinolysis in a subject that have received a therapeutically effective dose of a carboxypeptidase U (CPU) inhibitor, comprising detecting and quantifying the amount of protein (s) or polypeptides in a blood sample from said subject. According to another aspect of the invention, a method is provided for monitoring the progression of fibrinolysis in a subject, comprising determining the levels of fibrin fragments, in a blood sample from the subject, wherein said fibrin fragment is selected from the group consisting of the fibrin gamma-chain and fibrin α-fragments.
• Pyridine mercapto carboxylic acids as carboxypeptidase U inhibitors
  申请人：Astrazeneca AB

  公开号：US07071175B1

  公开（公告）日：2006-07-04

  The present invention relates to compounds of Formula I, and pharmaceutically acceptable salts or solvates thereof, or solvates of such salts, which compounds inhibit carboxypeptidase U and thus can be used in the prevention and treatment of diseases associated with carboxypeptidase U. In further aspects, the invention relates to compounds of the invention for use in therapy; to processes for preparation of such new compounds: to pharmaceutical compositions containing at least one compound of the invention, or a pharmaceutically acceptable salt or solvate thereof, as active ingredient; and to the use of the active compounds in the manufacture of medicaments for the medical use indicated above.

  本发明涉及式I的化合物，以及其药学上可接受的盐或溶剂或这些盐的溶剂，这些化合物抑制羧肽酶U，因此可用于预防和治疗与羧肽酶U相关的疾病。在进一步方面，本发明涉及用于治疗的本发明化合物；制备这种新化合物的过程；包含本发明化合物中至少一种作为活性成分的药物组合物；以及在制造上述医疗用途的药物中使用活性化合物。