N-{2-[4-(1,1-dioxido-4-oxo-1,2,5-thiadiazolidin-2-yl)-3-hydroxybenzyl]-4-ethylphenyl}sulfamide | 941593-83-5

• 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: N-{2-[4-(1,1-dioxido-4-oxo-1,2,5-thiadiazolidin-2-yl)-3-hydroxybenzyl]-4-ethylphenyl}sulfamide
• 英文别名: 2-[4-[[5-Ethyl-2-(sulfamoylamino)phenyl]methyl]-2-hydroxyphenyl]-1,1,4-trioxo-1,2,5-thiadiazolidine
• CAS: 941593-83-5
• 化学式: C₁₇H₂₀N₄O₆S₂
• 分子量: 440.501
• InChiKey: RCGROYQCYACKCA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1
• 重原子数：
  29
• 可旋转键数：
  6
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.24
• 拓扑面积：
  176
• 氢给体数：
  4
• 氢受体数：
  9

文献信息

• 1,2,5-Thiazolidine Derivatives Useful for Treating Conditions Mediated by Protein Tyrosine Phosphatases (Ptpase)
  申请人：Barnes David

  公开号：US20080293776A1

  公开（公告）日：2008-11-27

  Compounds of the formula are inhibitors of protein tyrosine phosphatases (PTPases) and, thus, may be employed for the treatment of conditions mediated by PTPase activity. The compounds of the present invention may also be employed as inhibitors of other enzymes characterized with a phosphotyrosine binding region such as the SH2 domain. Accordingly, the compounds of formula (I) may be employed for prevention and/or treatment of insulin resistance associated with obesity, glucose intolerance, diabetes mellitus, hypertension and ischemic diseases of the large and small blood vessels, conditions that accompany type-2 diabetes, including hyperlipidemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, irritable bowel syndrome, pancreatitis, adipose cell tumors and carcinomas such as liposarcoma, dyslipidemia, and other disorders where insulin resistance is indicated. In addition, the compounds of the present invention may be employed to treat and/or prevent cancer, osteoporosis, neurodegenerative and infectious diseases, and diseases involving inflammation and the immune system.

  公式为的化合物是蛋白酪氨酸磷酸酶（PTPases）的抑制剂，因此可用于治疗由PTPase活性介导的疾病。本发明的化合物也可以作为其他酶的抑制剂，这些酶具有磷酸酪氨酸结合区域，例如SH2结构域。因此，公式（I）的化合物可用于预防和/或治疗与肥胖相关的胰岛素抵抗、葡萄糖不耐受、糖尿病、高血压和大、小血管的缺血性疾病，伴随2型糖尿病的疾病，包括高脂血症、高三酰甘油血症、动脉粥样硬化、血管再狭窄、肠易激综合征、胰腺炎、脂肪细胞肿瘤和脂肪肉瘤、脂质代谢紊乱以及其他表现为胰岛素抵抗的疾病。此外，本发明的化合物还可用于治疗和/或预防癌症、骨质疏松症、神经退行性和传染性疾病，以及涉及炎症和免疫系统的疾病。
• 1,2,5-THIAZOLIDINE DERIVATIVES USEFUL FOR TREATING CONDITIONS MEDIATED BY PROTEIN TYROSINE PHOSPHATASES (PTPASE)
  申请人：Novartis AG

  公开号：EP1963294B1

  公开（公告）日：2012-10-10
• INHIBITORS OF PROTEIN TYROSINE PHOSPHATASE FOR THE PROMOTION OF PHYSIOLOGICAL CARDIAC HYPERTROPHY
  申请人：NOVARTIS AG

  公开号：EP2089026A2

  公开（公告）日：2009-08-19
• COMBINATION OF PROTEIN TYROSINE PHOSPHATASE INHIBITORS AND HUMAN GROWTH HORMONE FOR THE TREATMENT OF MUSCLE ATROPHY AND RELATED DISORDERS
  申请人：Barnes David

  公开号：US20100305036A1

  公开（公告）日：2010-12-02

  The invention relates to the use of a combination of protein tyrosine phosphatase inhibitors and human growth hormone for the treatment of musculoskeletal diseases, particularly for the treatment of muscle atrophy.
• US8119666B2
  申请人：——

  公开号：US8119666B2

  公开（公告）日：2012-02-21