1-(2,4-diethoxy-5-trifluoromethyl-phenyl)-3-{3-[8-(methyl-pyridin-4-yl-methyl-amino)-imidazo[1,2-a]pyrazin-6-yl]-phenyl}-urea | 847024-54-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 1-(2,4-diethoxy-5-trifluoromethyl-phenyl)-3-{3-[8-(methyl-pyridin-4-yl-methyl-amino)-imidazo[1,2-a]pyrazin-6-yl]-phenyl}-urea
• 英文别名: 1-[2,4-Diethoxy-5-(trifluoromethyl)phenyl]-3-[3-[8-[methyl(pyridin-4-ylmethyl)amino]imidazo[1,2-a]pyrazin-6-yl]phenyl]urea
• CAS: 847024-54-8
• 化学式: C₃₁H₃₀F₃N₇O₃
• 分子量: 605.62
• InChiKey: XMIHMRYJHPPFOW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.4
• 重原子数：
  44
• 可旋转键数：
  10
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.23
• 拓扑面积：
  106
• 氢给体数：
  2
• 氢受体数：
  10

文献信息

• Certain substituted imidazo[1,2-a]pyrazines, as modulators of kinase activity
  申请人：Mitchell A. Scott

  公开号：US20050085484A1

  公开（公告）日：2005-04-21

  Certain substituted imidazo[1,2-a]pyrazines and the pharmaceutically-acceptable salts thereof, are provided herein. Pharmaceutical compositions containing one or more compound of Formula I, or a pharmaceutically acceptable salt of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents, are also provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to EphB4 kinase modulation, which comprise administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include cancer, including breast neoplasia, endometrial cancer, colon cancer, and neck squamous cell carcinoma. Thus methods of treatment include administering a sufficient amount of a compound of the invention to decrease the symptoms or slow the progression of these diseases or disorders. 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 one or more other therapeutic agents. A method for determining the presence or absence of an angiogenic kinase in a sample comprising contacting the sample with a compound of Formula I under conditions that permit detection of activity of the angiogenic kinase, detecting a level of the activity of the angiogenic kinase, and therefrom determining the presence or absence of the angiogenic kinase in the sample.

  本文提供了某些取代的咪唑并[1,2-a]吡嗪化合物及其药物可接受的盐。本文还提供了含有一种或多种I式化合物或这些化合物的药物可接受的盐和一种或多种药物可接受的载体、赋形剂或稀释剂的制药组合物。本文公开了治疗对EphB4激酶调节敏感的某些疾病和疾病的患者的方法，该方法包括向这些患者施用足够的I式化合物的量，以减少疾病或疾病的症状或迹象。这些疾病包括癌症，包括乳腺肿瘤、子宫内膜癌、结肠癌和颈部鳞状细胞癌。因此，治疗方法包括施用足够的本发明化合物的量，以减轻这些疾病或疾病的症状或减缓其进展。治疗方法包括将I式化合物作为单一活性剂或与一种或多种其他治疗剂联合使用。一种用于确定样品中是否存在血管生成激酶的方法，包括将样品与I式化合物接触，以便在允许检测血管生成激酶活性的条件下检测血管生成激酶活性水平，并从中确定样品中是否存在血管生成激酶。
• US7259164B2
  申请人：——

  公开号：US7259164B2

  公开（公告）日：2007-08-21
• [EN] SUBSTITUTED IMIDAZO[1,2-A]PYRAZINES AS MODULATORS OF KINASE ACTIVITY<br/>[FR] IMIDAZO[1,2-A]PYRAZINES SUBSTITUEES UTILISEES COMME MODULATEURS DE L'ACTIVITE D'UNE KINASE
  申请人：CELLULAR GENOMICS INC

  公开号：WO2005019220A2

  公开（公告）日：2005-03-03

  Certain substituted imidazo[1,2-a]pyrazines and the pharmaceutically-acceptable salts thereof, are provided herein. Pharmaceutical compositions containing one or more compound of Formula I, or a pharmaceutically acceptable salt of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents, are also provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to EphB4 kinase modulation, which comprise administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include cancer, including breast neoplasia, endometrial cancer, colon cancer, and neck squamous cell carcinoma. Thus methods of treatment include administering a sufficient amount of a compound of the invention to decrease the symptoms or slow the progression of these diseases or disorders. 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 one or more other therapeutic agents. A method for determining the presence or absence of an angiogenic kinase in a sample comprising contacting the sample with a compound of Formula I under conditions that permit detection of activity of the angiogenic kinase, detecting a level of the activity of the angiogenic kinase, and therefrom determining the presence or absence of the angiogenic kinase in the sample.