4-[2-(5-cyano-thiazol-2-ylamino)-5-methyl-pyridin-4-ylmethyl]-piperazine-1-carboxylic acid methylamide | 479612-28-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 英文名称: 4-[2-(5-cyano-thiazol-2-ylamino)-5-methyl-pyridin-4-ylmethyl]-piperazine-1-carboxylic acid methylamide
• 英文别名: 4-[[2-[(5-cyano-1,3-thiazol-2-yl)amino]-5-methylpyridin-4-yl]methyl]-N-methylpiperazine-1-carboxamide
• CAS: 479612-28-7
• 化学式: C₁₇H₂₁N₇OS
• 分子量: 371.466
• InChiKey: GNLSTDJPFMHPKT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.4
• 重原子数：
  26
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.41
• 拓扑面积：
  125
• 氢给体数：
  2
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  diisopropylethyl amine 、 2-(4-Chloromethyl-5-methyl-pyridin-2-ylamino)-thiazole-5-carbonitrile 、 N-methylpiperazine-1-carboxamide hydrochloride 以 二甲基亚砜 为溶剂， 生成 4-[2-(5-cyano-thiazol-2-ylamino)-5-methyl-pyridin-4-ylmethyl]-piperazine-1-carboxylic acid methylamide
  参考文献：
  名称：

  Tyrosine kinase inhibitors

  摘要：

  本发明涉及抑制、调节和/或调节酪氨酸激酶信号传导的化合物，包含这些化合物的组合物，以及使用它们治疗酪氨酸激酶依赖性疾病和情况的方法，例如在哺乳动物中的血管生成、癌症、肿瘤生长、动脉粥样硬化、年龄相关性黄斑变性、糖尿病性视网膜病变、炎症性疾病等。

  公开号：

  US20030100567A1

文献信息

• (5-cyano-2-thiazolyl)amino-4-pyridine tyrosine kinase inhibitors
  申请人：Bilodeau Mark T.

  公开号：US06875767B2

  公开（公告）日：2005-04-05

  The present invention relates to compounds having the formula I: which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions. The compounds of the present invention are useful in treating angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.

  本发明涉及公式I的化合物，其抑制，调节和/或调节酪氨酸激酶信号传导，包含这些化合物的组合物，以及使用它们治疗酪氨酸激酶依赖性疾病和病状的方法。本发明的化合物对于治疗哺乳动物中的血管生成，癌症，肿瘤生长，动脉粥样硬化，年龄相关性黄斑变性，糖尿病视网膜病变，炎症性疾病等都有用。
• TYROSINE KINASE INHIBITORS
  申请人：Merck & Co., Inc.

  公开号：EP1404672A1

  公开（公告）日：2004-04-07
• US6875767B2
  申请人：——

  公开号：US6875767B2

  公开（公告）日：2005-04-05
• [EN] TYROSINE KINASE INHIBITORS<br/>[FR] INHIBITEURS DE TYROSINE KINASE
  申请人：MERCK & CO INC

  公开号：WO2003000687A1

  公开（公告）日：2003-01-03

  The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals. A compound of Formula (I) wherein n is 0 or 1; X is C-H or N, provided X is C-H if n=1 and R1 is SO¿2?-(C1-C6 alkyl) and provided that X is C-H if R?1¿ is NH(C=O)NR3H; R1 is SO¿2?-(C1-C6 alkyl), (C=O)NR?3¿H, or NH(C=O)NR3H; R2 is OH OC¿1?-C6 alkyl, C1-C6 alkyl, or halo; and R?3 is C¿1-C6 alkyl.
• Tyrosine kinase inhibitors
  申请人：——

  公开号：US20030100567A1

  公开（公告）日：2003-05-29

  The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.

  本发明涉及抑制、调节和/或调节酪氨酸激酶信号传导的化合物，包含这些化合物的组合物，以及使用它们治疗酪氨酸激酶依赖性疾病和情况的方法，例如在哺乳动物中的血管生成、癌症、肿瘤生长、动脉粥样硬化、年龄相关性黄斑变性、糖尿病性视网膜病变、炎症性疾病等。