TMI-1

• 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: TMI-1
• 英文别名: (3S)-4-{[4-(But-2-ynyloxy)phenyl]sulfonyl}-N-hydroxy-2,2-dimethylthiomorpholine-3-carboxamide；(3S)-4-(4-but-2-ynoxyphenyl)sulfonyl-N-hydroxy-2,2-dimethylthiomorpholine-3-carboxamide
• 化学式: C₁₇H₂₂N₂O₅S₂
• 分子量: 398.504
• InChiKey: CVZIHNYAZLXRRS-HNNXBMFYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  26
• 可旋转键数：
  5
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.47
• 拓扑面积：
  130
• 氢给体数：
  2
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  D-青霉胺 在 sodium hydroxide 、 草酰氯 、 四溴化碳 、 羟胺 、 sodium carbonate 、 potassium carbonate 、 N,N-二甲基甲酰胺 、 三苯基膦 、 三氟乙酸 作用下， 生成 TMI-1
  参考文献：
  名称：

  Acetylenic TACE inhibitors. Part 2: SAR of six-membered cyclic sulfonamide hydroxamates

  摘要：

  The SAR of a series of potent sulfonamide hydroxamate TACE inhibitors bearing a butynyloxy P1' group was explored. In particular, compound 5k has excellent in vitro potency against TACE enzyme and in cells, and oral activity in an in vivo model of TNF-alpha production and a collagen-induced arthritis model.

  DOI：

  10.1016/j.bmcl.2005.06.072

文献信息

• Acetylenic alpha -amino acid-based sulfonamide hydroxamic acid tace inhibitors
  申请人：——

  公开号：US20030008849A1

  公开（公告）日：2003-01-09

  Compounds of the formula: 1 are useful in treating disease conditions mediated by TNF-&agr;, such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative cartilage loss.

  公式为1的化合物可用于治疗由TNF-&agr;介导的疾病条件，例如类风湿性关节炎、骨关节炎、败血症、艾滋病、溃疡性结肠炎、多发性硬化症、克罗恩病和退行性软骨丢失。
• Acetylenic alpha-amino acid-based sulfonamide hydroxamic acid tace inhibitors
  申请人：Levin I. Jeremy

  公开号：US20050113346A1

  公开（公告）日：2005-05-26

  Compounds of the formula: are useful in treating disease conditions mediated by TNF-α, such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative cartilage loss.

  式为的化合物在治疗由TNF-α介导的疾病条件方面非常有用，例如类风湿性关节炎、骨关节炎、败血症、艾滋病、溃疡性结肠炎、多发性硬化症、克罗恩病和退行性软骨损失。
• Method for the treatment of polycystic kidney disease
  申请人：——

  公开号：US20040063672A1

  公开（公告）日：2004-04-01

  The present invention provides a method for treating, inhibiting the progression of, or eradicating polycystic kidney disease of in a patient in need thereof which comprises providing to said patient an effective amount of a TACE inhibitor compound alone or in combination with an effective amount of an EDF receptor kinase inhibitor.

  本发明提供了一种治疗、抑制进展或根除多囊肾病的方法，该方法包括向需要该治疗的患者提供有效量的TACE抑制剂化合物，单独或与有效量的EDF受体激酶抑制剂化合物联合使用。
• Compounds and methods for improving platelet recovery and function
  申请人：Wagner D. Denisa

  公开号：US20050019743A1

  公开（公告）日：2005-01-27

  The present invention describes an improved blood product suitable for use in transfusions comprising, in combination, blood platelets and an inhibitor of platelet glycoprotein Ibα cleavage from platelets, such as a metalloproteinase inhibitor or a TACE inhibitor. Containers for storing the improved blood product for periods of up to about 10 days, and methods for testing and using the recovered improved blood product in patient transfusions, are also provided.

  本发明描述了一种适用于输血的改良血液制品，它由血小板和血小板糖蛋白Ⅰbα裂解抑制剂（如金属蛋白酶抑制剂或TACE抑制剂）组合而成。此外，还提供了可将改良血液制品储存 10 天左右的容器，以及在患者输血中检测和使用回收的改良血液制品的方法。
• ACETYLENIC ALPHA-AMINO ACID-BASED SULFONAMIDE HYDROXAMIC ACID TACE INHIBITORS
  申请人：Wyeth Holdings Corporation

  公开号：EP1144368B1

  公开（公告）日：2004-07-14