8-carbamoyl-3-(2-methoxyethyl)-[3H]-imidazo[5,1-d]-1,2,3,5-tetrazin-4-one | 85623-03-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 咪唑四嗪类
• 英文名称: 8-carbamoyl-3-(2-methoxyethyl)-[3H]-imidazo[5,1-d]-1,2,3,5-tetrazin-4-one
• 英文别名: 3-(2-Methoxyethyl)-4-oxoimidazo[5,1-d][1,2,3,5]tetrazine-8-carboxamide
• CAS: 85623-03-6
• 化学式: C₈H₁₀N₆O₃
• 分子量: 238.206
• InChiKey: PQBKCEXTGCRVAP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.2
• 重原子数：
  17
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  115
• 氢给体数：
  1
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  8-carbamoyl-3-(2-methoxyethyl)-[3H]-imidazo[5,1-d]-1,2,3,5-tetrazin-4-one 、 肼 以60%的产率得到
  参考文献：
  名称：

  BAIG G. U.; STEVENS M. F. G., J. CHEM. SOC. PERKIN TRANS.,(1987) N 3, 665-670

  摘要：

  DOI：

文献信息

• 3-Substituted-4-Oxo-3,4-Dihydro-Imidazo[5,1-d][1,2,3,5-Tetrazine-8-Carboxylic Acid Amides and Their Use
  申请人：Stevens Malcolm Francis Graham

  公开号：US20100286088A1

  公开（公告）日：2010-11-11

  The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain 3-substituted-4-oxo-3,4-dihydro-imidazo[5,1-d][1,2,3,5]tetrazine-8-carboxylic acid amide (collectively referred to herein as 3TM compounds). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit cell proliferation, and in the treatment of proliferative disorders such as cancer, etc., and methods of preparing such compounds.

  本发明涉及治疗化合物领域，更具体地涉及某些3-取代-4-氧代-3,4-二氢咪唑[5,1-d][1,2,3,5]四嗪-8-羧酸酰胺（统称为3TM化合物）。本发明还涉及包含这种化合物的制药组合物，以及在体内外使用这种化合物和组合物来抑制细胞增殖，在治疗增生性疾病如癌症等方面的应用，以及制备这种化合物的方法。
• METHODS AND COMPOSITIONS FOR TREATING CANCER
  申请人：Kolhe Parag

  公开号：US20100143340A1

  公开（公告）日：2010-06-10

  The present invention provides methods for preventing or treating a medical disorder in a subject comprising administering to the subject an effective amount of a stable pharmaceutical formulation comprising an antibody or antigen-binding fragment thereof.

  本发明提供了一种预防或治疗受试者医疗障碍的方法，包括向受试者投与一种包含抗体或其抗原结合片段的稳定药物制剂的有效量。
• Treatment of brain and central nervous system tumors
  申请人：KADMON CORPORATION LLC

  公开号：US10080752B2

  公开（公告）日：2018-09-25

  The present invention provides methods for treating tumors of the brain by administering the compounds of the Formula A and particularly N-(3,4-dichloro-2-fluorophenyl)-7-([(3aR,6aS)-2-methyloctahydrocyclopenta[c]pyrrol-5-yl]methyl}oxy)-6-(methyloxy)quinazolin-4-amine, or a pharmaceutically acceptable salt thereof, to a subject in need of such treatment. In the methods of the invention, the compounds disclosed herein were surprisingly found to cross the blood brain barrier. The method of the present invention further relates to the treatment of cancers of any type potentially responding to EGFR, HER2, VEGFR2, or Src family kinase inhibitors and that are found in the brain.

  本发明提供了治疗脑肿瘤的方法，通过向需要治疗的受试者施用式A化合物，特别是N-(3,4-二氯-2-氟苯基)-7-([(3aR,6aS)-2-甲基八氢环戊并[c]吡咯-5-基]甲基}氧基)-6-(甲氧基)喹唑啉-4-胺或其药学上可接受的盐。在本发明的方法中，令人惊讶地发现本发明公开的化合物可以穿过血脑屏障。本发明的方法进一步涉及对表皮生长因子受体（EGFR）、HER2、血管内皮生长因子受体（VEGFR2）或Src家族激酶抑制剂有潜在反应的任何类型癌症的治疗，这些癌症在大脑中发现。
• Platinum therapeutic combinations
  申请人：Zong Chen

  公开号：US20060205810A1

  公开（公告）日：2006-09-14

  The present invention provides combination compositions comprising Pt based compounds, including satraplatin, along with another chemotherapeutic agent such as temozolomide or lonafarnib. The combinations are useful for the prevention or treatment of cancer. Method of using the combinations to treat or prevent cancer are also provided

  本发明提供了由铂类化合物（包括沙拉铂）与另一种化疗药物（如替莫唑胺或洛纳法尼）组成的组合物。这些组合物可用于预防或治疗癌症。还提供了使用这些组合物治疗或预防癌症的方法
• BAIG G. U.; STEVENS M. F. G., J. CHEM. SOC. PERKIN TRANS.,(1987) N 3, 665-670
  作者：BAIG G. U.、 STEVENS M. F. G.

  DOI：——

  日期：——