[5-amino-1-(2-methyl-1H-benzimidazol-5-yl)-1H-pyrazol-4-yl][5-(3,3-difluoropiperidine-1-carbonyl)-1H-indol-2-yl]methanone | 1265229-51-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: [5-amino-1-(2-methyl-1H-benzimidazol-5-yl)-1H-pyrazol-4-yl][5-(3,3-difluoropiperidine-1-carbonyl)-1H-indol-2-yl]methanone
• 英文别名: [2-[5-amino-1-(2-methyl-3H-benzimidazol-5-yl)pyrazole-4-carbonyl]-1H-indol-5-yl]-(3,3-difluoropiperidin-1-yl)methanone
• CAS: 1265229-51-3
• 化学式: C₂₆H₂₃F₂N₇O₂
• 分子量: 503.511
• InChiKey: XPJZNFSHCZZAQF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.5
• 重原子数：
  37
• 可旋转键数：
  4
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.23
• 拓扑面积：
  126
• 氢给体数：
  3
• 氢受体数：
  7

文献信息

• Aminopyrazole Derivative
  申请人：Taka Naoki

  公开号：US20120208811A1

  公开（公告）日：2012-08-16

  A compound represented by formula (I) or a pharmacologically acceptable salt thereof, which can inhibit a fibroblast growth factor receptor (FGFR) family kinase in cancer tissues. (In the formula, A represents a 5- to 10-membered heteroaryl group, or a C 6-10 aryl group; R 1 and R 2 independently represent H, OH, X, CN, NO 2 , a C 1-4 haloalkyl group, a C 1-6 alkyl group, or the like ; R 3 represents H, a C 1-5 alkyl group, a C 6-10 aryl group, a C 1-5 alkyl group, or a C 1-4 haloalkyl group; and R 4 represents H, X, a C 1-3 alkyl group, a C 1-4 haloalkyl group, OH, CN, NO 2 , or the like.)

  化合物(I)或其药学上可接受的盐，可以抑制癌组织中的成纤维细胞生长因子受体（FGFR）家族激酶。在公式中，A代表5-至10-成员的杂环芳基基团或C6-10芳基基团；R1和R2独立地表示H、OH、X、CN、NO2、C1-4卤代烷基、C1-6烷基或类似物；R3表示H、C1-5烷基、C6-10芳基基团、C1-5烷基或C1-4卤代烷基；R4表示H、X、C1-3烷基、C1-4卤代烷基、OH、CN、 或类似物。
• FGFR3 fusion gene and pharmaceutical drug targeting same
  申请人：Chugai Seiyaku Kabushiki Kaisha

  公开号：US10689705B2

  公开（公告）日：2020-06-23

  The FGFR-encoding gene was studied extensively with regard to its expression, hyperamplification, mutation, translocation, or such in various cancer cells. As a result, novel fusion polypeptides in which the FGFR3 polypeptide is fused with a different polypeptide were identified and isolated from several types of bladder cancer-derived cells and lung cancer cells. The use of a fusion polypeptide of the present invention as a biomarker in FGFR inhibitor-based cancer therapy enables one to avoid side effects in cancer therapy and control the therapeutic condition to produce the best therapeutic effect, thereby enabling individualized medicine.

  对表皮生长因子受体编码基因在各种癌细胞中的表达、高扩增、突变、易位等情况进行了广泛研究。结果，从几种类型的膀胱癌衍生细胞和肺癌细胞中鉴定并分离出了新型融合多肽，其中 FGFR3 多肽与另一种多肽融合。在基于表皮生长因子受体抑制剂的癌症治疗中，使用本发明的融合多肽作为生物标记物，可以避免癌症治疗中的副作用，控制治疗条件以产生最佳治疗效果，从而实现个体化医疗。
• AMINOPYRAZOLE DERIVATIVE
  申请人：Chugai Seiyaku Kabushiki Kaisha

  公开号：EP2471786B1

  公开（公告）日：2015-11-04
• FGFR3 FUSION GENE AND PHARMACEUTICAL DRUG TARGETING SAME
  申请人：Chugai Seiyaku Kabushiki Kaisha

  公开号：US20150307945A1

  公开（公告）日：2015-10-29

  The FGFR-encoding gene was studied extensively with regard to its expression, hyperamplification, mutation, translocation, or such in various cancer cells. As a result, novel fusion polypeptides in which the FGFR3 polypeptide is fused with a different polypeptide were identified and isolated from several types of bladder cancer-derived cells and lung cancer cells. The use of a fusion polypeptide of the present invention as a biomarker in FGFR inhibitor-based cancer therapy enables one to avoid side effects in cancer therapy and control the therapeutic condition to produce the best therapeutic effect, thereby enabling individualized medicine.
• US8829199B2
  申请人：——

  公开号：US8829199B2

  公开（公告）日：2014-09-09