8Xdp7T5xlu | 2271209-99-3

• 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: 8Xdp7T5xlu
• 英文别名: 3-[5-cyano-4-(cyclopropylamino)pyridin-2-yl]-1-[6-formyl-5-[(4-methyl-2-oxopiperazin-1-yl)methyl]pyridin-2-yl]-1-methylurea
• CAS: 2271209-99-3
• 化学式: C₂₃H₂₆N₈O₃
• 分子量: 462.5
• InChiKey: MXHSTECIDQMETN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.9
• 重原子数：
  34
• 可旋转键数：
  7
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.39
• 拓扑面积：
  135
• 氢给体数：
  2
• 氢受体数：
  8

文献信息

• FORMYLPYRIDINE DERIVATIVE HAVING FGFR4 INHIBITORY ACTIVITY, PREPARATION METHOD THEREFOR AND USE THEREOF
  申请人：Abbisko Therapeutics Co., Ltd.

  公开号：US20210130323A1

  公开（公告）日：2021-05-06

  Formylpyridine derivatives having FGFR4 inhibitory activities, a preparation method therefor and use thereof are described. In particular, the formylpyridine derivatives have a structure of formula (I), and the definition of each substituent in the formula are described in the description and claims. The series of compounds of the formula (I) have very strong inhibitory effects on FGFR4 kinases and very high selectivity, and can be widely used in the preparation of medicaments for treating cancers, particularly prostate cancer, liver cancer, pancreatic cancer, esophageal cancer, stomach cancer, lung cancer, breast cancer, ovarian cancer, colon cancer, skin cancer, neuroglioblastoma or rhabdomyosarcoma, and prospectively will be further developed to become a new generation of FGFR4 inhibitors.

  描述了具有FGFR4抑制活性的甲酰吡啶衍生物，其制备方法及用途。具体来说，这些甲酰吡啶衍生物具有式（I）的结构，该式中每个取代基的定义在描述和权利要求中有所描述。式（I）的一系列化合物对FGFR4激酶具有非常强的抑制作用和非常高的选择性，并可广泛用于制备用于治疗癌症的药物，特别是前列腺癌、肝癌、胰腺癌、食道癌、胃癌、肺癌、乳腺癌、卵巢癌、结肠癌、皮肤癌、神经胶质母细胞瘤或横纹肌肉瘤，并有望进一步发展成为新一代FGFR4抑制剂。
• Formylpyridine derivative having FGFR4 inhibitory activity, preparation method therefor and use thereof
  申请人：Abbisko Therapeutics Co., Ltd.

  公开号：US11312701B2

  公开（公告）日：2022-04-26

  Formylpyridine derivatives having FGFR4 inhibitory activities, a preparation method therefor and use thereof are described. In particular, the formylpyridine derivatives have a structure of formula (I), and the definition of each substituent in the formula are described in the description and claims. The series of compounds of the formula (I) have very strong inhibitory effects on FGFR4 kinases and very high selectivity, and can be widely used in the preparation of medicaments for treating cancers, particularly prostate cancer, liver cancer, pancreatic cancer, esophageal cancer, stomach cancer, lung cancer, breast cancer, ovarian cancer, colon cancer, skin cancer, neuroglioblastoma or rhabdomyosarcoma, and prospectively will be further developed to become a new generation of FGFR4 inhibitors.

  本发明描述了具有 FGFR4 抑制活性的甲酰基吡啶衍生物、其制备方法及其用途。其中，甲酰基吡啶衍生物具有式（I）结构，式中各取代基的定义见说明书和权利要求书。式（I）系列化合物对FGFR4激酶具有很强的抑制作用和很高的选择性，可广泛应用于制备治疗癌症的药物，特别是前列腺癌、肝癌、胰腺癌、食管癌、胃癌、肺癌、乳腺癌、卵巢癌、结肠癌、皮肤癌、神经胶质母细胞瘤或横纹肌肉瘤等，并有望进一步开发成为新一代的FGFR4抑制剂。