3-Methyl-2-(3H-[1,2,3]triazol-4-yl)-pyridine

• 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: 3-Methyl-2-(3H-[1,2,3]triazol-4-yl)-pyridine
• 英文别名: 3-methyl-2-(1H-1,2,3-triazol-5-yl)pyridine；3-methyl-2-(2H-triazol-4-yl)pyridine
• 化学式: C₈H₈N₄
• 分子量: 160.178
• InChiKey: IYTHSSNIJXFAQN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.6
• 重原子数：
  12
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.12
• 拓扑面积：
  54.5
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  2-乙炔-3-甲基吡啶 在 叠氮基三甲基硅烷 、 水 作用下， 以 甲苯 为溶剂， 以35%的产率得到3-Methyl-2-(3H-[1,2,3]triazol-4-yl)-pyridine
  参考文献：
  名称：

  4-Aryl-1,2,3-triazole:  A Novel Template for a Reversible Methionine Aminopeptidase 2 Inhibitor, Optimized To Inhibit Angiogenesis in Vivo

  摘要：

  Inhibitors of human methionine aminopeptidase type 2 (hMetAP2) are of interest as potential treatments for cancer. A new class of small molecule reversible inhibitors of hMetAP2 was discovered and optimized, the 4-aryl-1,2,3-triazoles. Compound 24, a potent inhibitor of cobalt-activated hMetAP2, also inhibits human and mouse endothelial cell growth. Using a mouse matrigel model, this reversible hMetAP2 inhibitor was also shown to inhibit angiogenesis in vivo.

  DOI：

  10.1021/jm050408c

文献信息

• [EN] 4-AMINO-5-PHENYL-7-CYCLOHEXYL-PYRROLO[2,3-d]PYRIMIDINE DERIVATIVES<br/>[FR] DERIVES DE 4-AMINO-5-PHENYL-7-CYCLOHEXYL-PYRROLO[2,3-D]PYRIMIDINE
  申请人：NOVARTIS AG

  公开号：WO2004043962A1

  公开（公告）日：2004-05-27

  The invention relates to new 4-amino-5-phenyl-7-cyclohexyl-pyrrolo[2,3-d] pyrimidine derivatives, processes for the preparation thereof, the application thereof in a process for the treatment of the human or animal body, the use thereof - alone or in combination with one or more other pharmaceutically active compounds - for the treatment of a disease, especially a proliferative disease, such as a tumour disease, a method for the treatment of such diseases in mammals, especially in humans, and the use of such a compound - alone or in combination with one or more other pharmaceutically active compounds - for the preparation of a pharmaceutical composition (medicament) for the treatment especially of a proliferative disease, such as a tumour.

  该发明涉及新的4-氨基-5-苯基-7-环己基-吡咯并[2,3-d]嘧啶衍生物，其制备方法，其在治疗人体或动物体内的应用过程，其单独使用或与一个或多个其他药用活性化合物结合用于治疗疾病，特别是增殖性疾病，如肿瘤疾病，哺乳动物，特别是人类中治疗此类疾病的方法，以及使用这种化合物，单独或与一个或多个其他药用活性化合物结合，用于制备药物组合物（药物）以特别治疗增殖性疾病，如肿瘤。
• [EN] COMPOUNDS AND METHODS<br/>[FR] COMPOSES ET PROCEDES
  申请人：SMITHKLINE BEECHAM CORP

  公开号：WO2003031434A1

  公开（公告）日：2003-04-17

  Disclosed are compounds of formula (I) wherein the formula variables are as defined herein. The compounds of this invention are non-peptide, reversible inhibitors of type 2 methionine aminopeptidase. Also disclosed is the use of such compounds in treating conditions mediated by angiogenesis, such as cancer, haemangioma, proliferative retinopathy, rheumatoid arthritis, atherosclerotic neovascularization, psoriasis, ocular neovascularization and obesity.

  本发明揭示了式(I)的化合物，其中式变量如本文所定义。本发明的化合物是非肽类，可逆抑制剂，可抑制2型蛋氨酸氨肽酶。本发明还揭示了这些化合物在治疗由血管生成介导的疾病方面的用途，如癌症、血管瘤、增生性视网膜病变、类风湿性关节炎、动脉粥样硬化性新生血管形成、牛皮癣、眼部新生血管形成和肥胖症。
• METALLOENZYME INHIBITOR COMPOUNDS
  申请人：Innocrin Pharmaceuticals, Inc.

  公开号：US20170143694A1

  公开（公告）日：2017-05-25

  The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.

  本发明描述了具有金属酶调节活性的化合物，以及治疗由这些金属酶介导的疾病、疾病或症状的方法。
• Compounds and methods
  申请人：——

  公开号：US20040192914A1

  公开（公告）日：2004-09-30

  Disclosed are compounds of the formula: 1 wherein the formula variables are as defined herein. The compounds of this invention are non-peptide, reversible inhibitors of type 2 methionine aminopeptidase. Also disclosed is the use of such compounds in treating conditions mediated by angiogenesis, such as cancer, haemangioma, proliferative retinopathy, rheumatoid arthritis, atherosclerotic neovascularization, psoriasis, ocular neovascularization and obesity.

  本发明揭示了式1的化合物：其中式中的变量在此定义。本发明的化合物是非肽类、可逆抑制剂2型甲硫氨酰肽酶。本发明还揭示了这些化合物在治疗通过血管生成介导的疾病中的应用，例如癌症、血管瘤、增生性视网膜病变、类风湿性关节炎、动脉粥样硬化性新生血管形成、牛皮癣、眼部新生血管形成和肥胖症。
• COMPOUNDS AND METHODS
  申请人：SmithKline Beecham Corporation

  公开号：EP1434772A1

  公开（公告）日：2004-07-07