Brivanib alaninateBMS-582664

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: Brivanib alaninateBMS-582664
• 英文别名: [(2S)-1-[4-[(4-fluoro-2-methyl-1H-indol-5-yl)oxy]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]oxypropan-2-yl] (2R)-2-aminopropanoate
• 化学式: C₂₂H₂₄FN₅O₄
• 分子量: 441.5
• InChiKey: LTEJRLHKIYCEOX-GXTWGEPZSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  32
• 可旋转键数：
  8
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.32
• 拓扑面积：
  117
• 氢给体数：
  2
• 氢受体数：
  8

文献信息

• Composition for combination therapy comprising an anti-C-met antibody and a FGFR inhibitor
  申请人：Samsung Electronics Co., Ltd.

  公开号：EP2786765A2

  公开（公告）日：2014-10-08

  Provided is a composition for use in combination therapy for prevention or treatment of a cancer including a FGFR inhibitor and an anti-c-Met antibody or an antigen-binding fragment thereof as active ingredients. The composition for use in combination therapy can achieve an excellent synergistic effect and lower the effective dose of the anti-c-Met antibody, thereby enabling a more effective cancer treatment.

  本发明提供了一种用于预防或治疗癌症的联合疗法的组合物，其活性成分包括表皮生长因子受体抑制剂和抗-Met抗体或其抗原结合片段。这种用于联合治疗的组合物可以达到很好的协同效应，降低抗-Met 抗体的有效剂量，从而实现更有效的癌症治疗。
• Deuterated triazolopyridazine as a kinase modulator
  申请人：Janssen Pharmaceutica NV

  公开号：US10138246B2

  公开（公告）日：2018-11-27

  The invention is directed to a triazolopyridazine compound of formula (I), N-oxides, pharmaceutically acceptable salts and solvates thereof, wherein D represents deuterium, the use of such compounds as protein tyrosine kinase modulators, particularly inhibitors of c-Met, and the use of such compounds to reduce or inhibit kinase activity of c-Met in a cell or a subject, and modulate c-Met expression in a cell or subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to c-Met. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating conditions such as cancers and other cell proliferative disorders.

  本发明涉及式(I)的三唑并哒嗪化合物、其N-氧化物、药学上可接受的盐和溶剂（其中D代表氘），以及将此类化合物用作蛋白酪氨酸激酶调节剂，特别是c-Met的抑制剂、以及使用此类化合物降低或抑制细胞或受试者中c-Met的激酶活性，调节细胞或受试者中c-Met的表达，以及使用此类化合物预防或治疗受试者中细胞增殖障碍和/或与c-Met相关的疾病。本发明进一步涉及包含本发明化合物的药物组合物，以及治疗癌症和其他细胞增殖障碍等疾病的方法。
• COMBINATIONS OF AN FGFR INHIBITOR AND AN IGF1R INHIBITOR
  申请人：Astex Therapeutics Ltd.

  公开号：EP3122359B1

  公开（公告）日：2020-12-16
• A DEUTERATED TRIAZOLOPYRIDAZINE AS A KINASE MODULATOR
  申请人：Janssen Pharmaceutica, N.V.

  公开号：EP3227296B1

  公开（公告）日：2020-03-04
• FGFR2 FUSION GENE
  申请人：NATIONAL CANCER CENTER

  公开号：US20150191791A1

  公开（公告）日：2015-07-09

  In order to identify genes that can serve as indicators for predicting the effectiveness of drug treatments in cancers and provide novel methods for predicting the effectiveness of treatments with drugs targeting said genes, transcriptome sequencing was performed of biliary tract cancer. As a result, in-frame fusion transcripts between the FGFR2 gene and other gene (BICC1 or AHCYL1 gene) were identified. It was also found that said gene fusions induce activation of FGFR2 protein, thereby causing canceration of cells. Further, it was demonstrated that the FGFR2 protein activation and canceration caused by said gene fusions can be suppressed by using an FGFR2 inhibitor, and that treatments with an FGFR2 inhibitor are effective in patients with detection of said gene fusions.