GW2GD2S2HK | 1936472-44-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 英文名称: GW2GD2S2HK
• 英文别名: 6-[difluoro-[6-(1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-b]pyridazin-3-yl]methyl]-1H-quinolin-2-one
• CAS: 1936472-44-4
• 化学式: C₁₈H₁₁F₂N₇O
• 分子量: 379.3
• InChiKey: JCVFQQMQKIWKOV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.2
• 重原子数：
  28
• 可旋转键数：
  3
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.06
• 拓扑面积：
  101
• 氢给体数：
  2
• 氢受体数：
  7

文献信息

• [EN] A DEUTERATED TRIAZOLOPYRIDAZINE AS A KINASE MODULATOR<br/>[FR] TRIAZOLOPYRIDAZINE DEUTÉRÉE EN TANT QUE MODULATEUR DE KINASE
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：WO2016087586A1

  公开（公告）日：2016-06-09

  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.

  该发明涉及一种三唑吡嗪化合物，其化学式为（I），以及其氮氧化物、药学上可接受的盐和溶剂化物，其中D代表氘。该化合物的用途为蛋白酪氨酸激酶调节剂，特别是c-Met的抑制剂，并用于减少或抑制细胞或主体中c-Met的激酶活性，并调节细胞或主体中c-Met的表达。该化合物的用途还包括预防或治疗细胞增殖紊乱和/或与c-Met相关的疾病。本发明还涉及包含该化合物的制药组合物以及治疗癌症和其他细胞增殖紊乱的方法。
• 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。
• A DEUTERATED TRIAZOLOPYRIDAZINE AS A KINASE MODULATOR
  申请人：Janssen Pharmaceutica, N.V.

  公开号：EP3227296A1

  公开（公告）日：2017-10-11
• DEUTERATED TRIAZOLOPYRIDAZINE AS A KINASE MODULATOR
  申请人：Janssen Pharmaceutica NV

  公开号：US20190031670A1

  公开（公告）日：2019-01-31

  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.