2-benzyloxy-4-iodophenylamine | 1057341-60-2

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯酚醚
• 英文名称: 2-benzyloxy-4-iodophenylamine
• 英文别名: 4-iodo-2-phenylmethoxyaniline
• CAS: 1057341-60-2
• 化学式: C₁₃H₁₂INO
• 分子量: 325.149
• InChiKey: KOULBZNFSSSSDN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.4
• 重原子数：
  16
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.08
• 拓扑面积：
  35.2
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  2-benzyloxy-4-iodophenylamine 在 偶氮二甲酸二异丙酯 、 potassium carbonate 、 三乙胺 、 三苯基膦 作用下， 以 二氯甲烷 、 N,N-二甲基甲酰胺 、 甲苯 为溶剂， 反应 23.5h， 生成 tert-butyl N-[2-(benzyloxy)-4-iodophenyl]-N-{{(tert-butoxycarbonyl)[2-(trimethylsilyl)ethyl]amino}sulfonyl}glycinate
  参考文献：
  名称：

  WO2007/115058

  摘要：

  公开号：
• 作为产物：
  描述：

  溴甲苯 在 铁粉 、 potassium carbonate 、 溶剂黄146 作用下， 以 乙醇 、 N,N-二甲基甲酰胺 为溶剂， 反应 2.0h， 生成 2-benzyloxy-4-iodophenylamine
  参考文献：
  名称：

  WO2007/115058

  摘要：

  公开号：

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。
• Organic compounds
  申请人：Novartis AG

  公开号：US08084448B2

  公开（公告）日：2011-12-27

  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, musculoskeletal, 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（PTPase）的抑制剂，因此可用于治疗PTPase活性介导的疾病。本发明的化合物也可用作其他酶的抑制剂，这些酶具有磷酸酪氨酸结合区域，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、葡萄糖耐受性、糖尿病、高血压和大、小血管缺血性疾病相关的胰岛素抵抗，以及伴随2型糖尿病的情况，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、脂质代谢异常和其他表现为胰岛素抵抗的疾病。此外，本发明的化合物可用于治疗和/或预防癌症、骨质疏松症、肌肉骨骼、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：US08119666B2

  公开（公告）日：2012-02-21

  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.

  式(I)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用作其他特征为磷酸酪氨酸结合区域（如SH2结构域）的酶的抑制剂。因此，式(I)的化合物可用于预防和/或治疗与肥胖、葡萄糖不耐受、糖尿病、高血压和大、小血管缺血性疾病相关的胰岛素抵抗症状。这些症状伴随着2型糖尿病，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、失调脂质血症以及其他胰岛素抵抗症状。此外，本发明的化合物可用于治疗和/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。
• ORGANIC COMPOUNDS
  申请人：Neubert Alan

  公开号：US20090181928A1

  公开（公告）日：2009-07-16

  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, musculoskeletal, neurodegenerative and infectious diseases, and diseases involving inflammation and the immune system.

  公式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用作其他酶的抑制剂，这些酶具有磷酸酪氨酸结合区域，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、葡萄糖不耐受、糖尿病、高血压以及大、小血管缺血性疾病有关的胰岛素抵抗。这些疾病包括高脂血症、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等癌症，以及其他显示胰岛素抵抗的疾病。此外，本发明的化合物可用于治疗和/或预防癌症、骨质疏松症、肌肉骨骼、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。
• WO2007/67613
  申请人：——

  公开号：——

  公开（公告）日：——