5H-吡咯并[3,2-d]嘧啶,7-溴-5-[(1,1-二甲基乙基)二甲基甲硅烷基]-2,4-二(苯基甲氧基)- | 83724-76-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡唑并嘧啶类
• 中文名称: 5H-吡咯并[3,2-d]嘧啶,7-溴-5-[(1,1-二甲基乙基)二甲基甲硅烷基]-2,4-二(苯基甲氧基)-
• 英文名称: 6-Isopropylpyrazolo[1,5-a]pyrimidine
• 英文别名: 6-propan-2-ylpyrazolo[1,5-a]pyrimidine
• CAS: 83724-76-9
• 化学式: C₉H₁₁N₃
• 分子量: 161.206
• InChiKey: WJWGYDFQPFDTHB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.5
• 重原子数：
  12
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  30.2
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  3-氨基吡唑 、 2-iso-Propyl-3-ethoxyacrolein 以 溶剂黄146 为溶剂， 反应 3.0h， 以84%的产率得到5H-吡咯并[3,2-d]嘧啶,7-溴-5-[(1,1-二甲基乙基)二甲基甲硅烷基]-2,4-二(苯基甲氧基)-
  参考文献：
  名称：

  Muehmel, G.; Hanke, R.; Breitmaier, E., Synthesis, 1982, # 8, p. 673 - 677

  摘要：

  DOI：

文献信息

• Substituted aryl acylthioureas and related compounds; inhibitors of viral replication
  申请人：Phadke Avinash

  公开号：US20060025416A1

  公开（公告）日：2006-02-02

  The invention provides compounds and pharmaceutically acceptable salts of Formula I wherein the variables A 1 , A 2 , R 1 , R 2 , V, W, X, Y, and Z are defined herein. Certain compounds of Formula I described herein which possess potent antiviral activity. The invention particularly provides compounds of Formula I that are potent and/or selective inhibitors of Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more compound of Formula I, or a salt, solvate, or acylated prodrug of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents. The invention further comprises methods of treating patients suffering from certain infectious diseases by administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease or disorder. These infectious diseases include viral infections, particularly HCV infections. The invention is particularly includes methods of treating human patients suffering from an infectious disease, but also encompasses methods of treating other animals, including livestock and domesticated companion animals, suffering from an infectious disease. Methods of treatment include administering a compound of Formula I as a single active agent or administering a compound of Formula I in combination with on or more other therapeutic agent.

  该发明提供了化合物和药用可接受的盐的公式I，其中变量A1、A2、R1、R2、V、W、X、Y和Z在此处定义。本文描述了公式I的某些化合物具有强效的抗病毒活性。该发明特别提供了公式I的化合物，这些化合物是对丙型肝炎病毒复制具有强效和/或选择性抑制作用的。该发明还提供了含有一个或多个公式I化合物、或这些化合物的盐、溶剂合物或酰化前药，以及一个或多个药用可接受的载体、辅料或稀释剂的药物组合物。该发明还包括通过向患有某些传染病的患者投与有效量的公式I化合物来减轻疾病或紊乱的症状或迹象的治疗方法。这些传染病包括病毒感染，特别是HCV感染。该发明特别包括治疗患有传染病的人类患者的方法，但也包括治疗其他动物，包括家畜和驯养的伴侣动物，患有传染病的方法。治疗方法包括单独使用公式I化合物作为活性剂或与一个或多个其他治疗剂联合使用公式I化合物。
• [EN] HYDANTOIN DERIVATIVE<br/>[FR] DÉRIVÉ D'HYDANTOÏNE
  申请人：ONO PHARMACEUTICAL CO

  公开号：WO2021043245A1

  公开（公告）日：2021-03-11

  A compound represented by general formula (I-a) : has a strong DDR1 inhibitory activity, and can be a therapeutic agent for DDR1-related diseases, for example, a cancer, a kidney disease, a cardiovascular disease, a central nervous system disease, or fibrosis.

  一种由一般化学式（I-a）表示的化合物具有强大的DDR1抑制活性，可作为DDR1相关疾病的治疗药物，例如癌症、肾脏疾病、心血管疾病、中枢神经系统疾病或纤维化病。
• [EN] 5- AND 6-AZAINDOLE COMPOUNDS FOR INHIBITION OF BCR-ABL TYROSINE KINASES<br/>[FR] COMPOSÉS DE 5- ET 6-AZAINDOLE POUR L'INHIBITION DE TYROSINE KINASES BCR-ABL
  申请人：ENLIVEN THERAPEUTICS INC

  公开号：WO2022076975A1

  公开（公告）日：2022-04-14

  The present disclosure relates to compounds and compositions for inhibition of Bcr- Abl tyrosine kinases, methods of preparing said compounds and compositions, and their use in the treatment of various cancers, such as chronic myeloid leukemia (CML).

  本公开涉及抑制Bcr-Abl酪氨酸激酶的化合物和组合物，制备该化合物和组合物的方法，以及它们在治疗各种癌症，如慢性髓细胞白血病（CML）中的应用。
• SUBSTITUTED ARYL ACYLTHIOUREAS AND RELATED COMPOUNDS; INHIBITORS OF VIRAL REPLICATION
  申请人：Phadke Avinash

  公开号：US20090023730A1

  公开（公告）日：2009-01-22

  The invention provides compounds and pharmaceutically acceptable salts of Formula I wherein the variables A 1 , A 2 , R 1 , R 2 , V, W, X, Y, and Z are defined herein. Certain compounds of Formula I described herein which possess potent antiviral activity. The invention particularly provides compounds of Formula I that are potent and/or selective inhibitors of Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more compound of Formula I, or a salt, solvate, or acylated prodrug of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents. The invention further comprises methods of treating patients suffering from certain infectious diseases by administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease or disorder. These infectious diseases include viral infections, particularly HCV infections. The invention is particularly includes methods of treating human patients suffering from an infectious disease, but also encompasses methods of treating other animals, including livestock and domesticated companion animals, suffering from an infectious disease. Methods of treatment include administering a compound of Formula I as a single active agent or administering a compound of Formula I in combination with on or more other therapeutic agent.

  本发明提供了式I的化合物和药学上可接受的盐，其中变量A1、A2、R1、R2、V、W、X、Y和Z在此定义。本文所描述的式I的某些化合物具有强效的抗病毒活性。本发明特别提供了式I的化合物，它们是强效和/或选择性的丙型肝炎病毒复制抑制剂。本发明还提供了含有式I的一个或多个化合物，或这些化合物的盐、溶剂合物或酰化前药的药物组合物，以及一个或多个药学上可接受的载体、赋形剂或稀释剂的制剂。本发明还包括通过向这些患者投与有效量的式I的化合物来治疗患有某些传染性疾病的患者的方法，以减轻疾病或失调的症状。这些传染性疾病包括病毒感染，特别是丙型肝炎病毒感染。本发明特别包括治疗患有传染性疾病的人类患者的方法，但也包括治疗其他动物，包括牲畜和家养伴侣动物，患有传染性疾病的方法。治疗方法包括将式I的化合物作为单一活性剂或将式I的化合物与一个或多个其他治疗剂联合使用。
• N4-PHENYL-QUINAZOLINE-4-AMINE DERIVATIVES AND RELATED COMPOUNDS AS ERBB TYPE I RECEPTOR TYROSINE KINASE INHIBITORS FOR THE TREATMENT OF HYPERPROLIFERATIVE DISEASES
  申请人：ARRAY BIOPHARMA, INC.

  公开号：US20140023643A1

  公开（公告）日：2014-01-23

  This invention provides compounds of Formula I wherein B, G, A, E, R 1 , R 2 , R 3 , m and n are as defined herein, which are useful as type I receptor tyrosine kinase inhibitors, and methods of use thereof in the treatment of hyperproliferative disorders in mammals.

  本发明提供了I式化合物，其中B、G、A、E、R1、R2、R3、m和n如本文所定义，它们可用作I型受体酪氨酸激酶抑制剂，并且在哺乳动物的增殖过度疾病治疗中使用的方法。