2-(1-methyl-1H-imidazol-2-yl)thieno[3,2-d]pyrimidin-4-ol | 884539-63-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 噻吩并嘧啶酮衍生物
• 英文名称: 2-(1-methyl-1H-imidazol-2-yl)thieno[3,2-d]pyrimidin-4-ol
• 英文别名: 2-(1-methylimidazol-2-yl)-3H-thieno[3,2-d]pyrimidin-4-one
• CAS: 884539-63-3
• 化学式: C₁₀H₈N₄OS
• 分子量: 232.266
• InChiKey: BQBQKFPKGPANJM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.8
• 重原子数：
  16
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.1
• 拓扑面积：
  87.5
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  2-(1-methyl-1H-imidazol-2-yl)thieno[3,2-d]pyrimidin-4-ol 、 methyl (2S,6S,12Z,13aS,14aR,16aS)-6-amino-2-hydroxy-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylate 在 偶氮二甲酸二异丙酯 、 三苯基膦 作用下， 以 四氢呋喃 为溶剂， 反应 16.0h， 以74%的产率得到methyl (2R,6S,12Z,13aS,14aR,16aS)-6-amino-2-{[2-(1-methyl-1H-imidazol-2-yl)thieno[3,2-d]pyrimidin-4-yl]oxy}-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylate trifluoroacetate
  参考文献：
  名称：

  WO2006/43145

  摘要：

  公开号：

文献信息

• Inhibitors Of Hepatitis C Virus Protease, And Compositions And Treatments Using The Same
  申请人：Collins Raymond Michael

  公开号：US20070249637A1

  公开（公告）日：2007-10-25

  The present invention provides compounds of formula (I), (II) or (IV), or pharmaceutically acceptable salts and solvates thereof, which are useful as inhibitors of the Hepatitis C virus (HCV) protease enzyme and are also useful for the treatment of HCV infections in HCV-infected mammals, including humans. The present invention also provides pharmaceutical compositions comprising compounds of formula (I), (II) or (IV), their pharmaceutically acceptable salts and solvates. Furthermore, the present invention provides intermediate compounds and methods useful in the preparation of compounds of formulas (I), (II) and (IV).

  本发明提供了公式(I)、(II)或(IV)的化合物，以及其药学上可接受的盐和溶剂，这些化合物对丙型肝炎病毒(HCV)蛋白酶酶具有抑制作用，并且也可用于治疗HCV感染的哺乳动物，包括人类。本发明还提供了包含公式(I)、(II)或(IV)的化合物、其药学上可接受的盐和溶剂的制药组合物。此外，本发明还提供了中间体化合物和制备公式(I)、(II)和(IV)化合物的方法。
• Compounds that interact with the Ras superfamily for the treatment of cancers, inflammatory diseases, rasopathies, and fibrotic disease
  申请人：SHY Therapeutics LLC

  公开号：US10588894B2

  公开（公告）日：2020-03-17

  Provided herein are methods and compositions for treating cancers, inflammatory diseases, rasopathies, and fibrotic disease involving aberrant Ras superfamily signaling through the binding of compounds to the GTP binding domain of Ras superfamily proteins including, in certain cases, K-Ras and mutants thereof, and a novel method for assaying such compositions.

  本文提供了通过化合物与 Ras 超家族蛋白（在某些情况下包括 K-Ras 及其突变体）的 GTP 结合结构域结合，治疗涉及 Ras 超家族信号异常的癌症、炎症性疾病、rasopathies 和纤维化疾病的方法和组合物，以及检测此类组合物的新方法。
• COMPOUNDS THAT INTERACT WITH THE RAS SUPERFAMILY FOR THE TREATMENT OF CANCERS, INFLAMMATORY DISEASES, RASOPATHIES, AND FIBROTIC DISEASE
  申请人：SHY Therapeutics LLC

  公开号：US20190022074A1

  公开（公告）日：2019-01-24

  Provided herein are methods and compositions for treating cancers, inflammatory diseases, rasopathies, and fibrotic disease involving aberrant Ras superfamily signaling through the binding of compounds to the GTP binding domain of Ras superfamily proteins including, in certain cases, K-Ras and mutants thereof, and a novel method for assaying such compositions.
• [EN] INHIBITORS OF HEPATITIS C VIRUS PROTEASE, AND COMPOSITIONS AND TREATMENTS USING THE SAME<br/>[FR] INHIBITEURS DE LA PROTEASE DU VIRUS DE L'HEPATITE C ET COMPOSITIONS ET TRAITEMENTS REPOSANT SUR L'EMPLOI DESDITS INHIBITEURS
  申请人：PFIZER

  公开号：WO2006043145A1

  公开（公告）日：2006-04-27

  [EN] The present invention provides compounds of formula (I), (II) or (IV), or pharmaceutically acceptable salts and solvates thereof, which are useful as inhibitors of the Hepatitis C virus (HCV) protease enzyme and are also useful for the treatment of HCV infections in HCV-­infected mammals, including humans. The present invention also provides pharmaceutical compositions comprising compounds of formula (I), (II) or (IV), their pharmaceutically acceptable salts and solvates. Furthermore, the present invention provides intermediate compounds and methods useful in the preparation of compounds of formulas (I), (II) and (IV).
  [FR] La présente invention concerne des composés représentés les formules (I), (II) ou (IV), ou bien des sels ou solvates pharmaceutiquement acceptables de ces composés, qui interviennent en tant qu'inhibiteurs de la protéase du virus de l'hépatite C (VCH) et qui conviennent également pour le traitement des infections par VCH chez des mammifères atteints par ledit virus, dont l'homme. Cette invention concerne également des compositions pharmaceutiques contenant les composés représentés par les formules (I), (II) ou (IV) ainsi que des sels ou solvates paharmaceutiquement acceptables de ces composés, et des méthodes d'obtention des composés de formule (I), (II) et (IV).