2-Butyl-3-[[5-methyl-2-[4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]amino]benzenesulfonamide

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 英文名称: 2-Butyl-3-[[5-methyl-2-[4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]amino]benzenesulfonamide
• 英文别名: 2-butyl-3-[[5-methyl-2-[4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]amino]benzenesulfonamide
• 化学式: C₂₆H₃₅N₇O₂S
• 分子量: 509.7
• InChiKey: FBPLMXBBCHNVEG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.7
• 重原子数：
  36
• 可旋转键数：
  9
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  125
• 氢给体数：
  3
• 氢受体数：
  9

文献信息

• METHODS FOR TREATING TYROSINE-KINASE-INHIBITOR-RESISTANT MALIGNANCIES IN PATIENTS WITH GENETIC POLYMORPHISMS OR AHI1 DYSREGULATIONS OR MUTATIONS EMPLOYING DIANHYDROGALACTITOL, DIACETYLDIANHYDROGALACTITOL, DIBROMODULCITOL, OR ANALOGS OR DERIVATIVES THEREOF
  申请人：Del Mar Pharmaceuticals

  公开号：EP2872161A2

  公开（公告）日：2015-05-20
• FUSED HETEROCYCLIC COMPOUNDS AS RET KINASE INHIBITORS
  申请人：Array Biopharma, Inc.

  公开号：EP3849986A1

  公开（公告）日：2021-07-21
• SUBSTITUTED PYRAZOLO[1,5-A]PYRIDINE COMPOUNDS AS INHIBITORS OF FGFR TYROSINE KINASES
  申请人：Array Biopharma, Inc.

  公开号：EP3898626A1

  公开（公告）日：2021-10-27
• [EN] METHODS FOR TREATING TYROSINE-KINASE-INHIBITOR-RESISTANT MALIGNANCIES IN PATIENTS WITH GENETIC POLYMORPHISMS OR AHI1 DYSREGULATIONS OR MUTATIONS EMPLOYING DIANHYDROGALACTITOL, DIACETYLDIANHYDROGALACTITOL, DIBROMODULCITOL, OR ANALOGS OR DERIVATIVES THEREOF<br/>[FR] MÉTHODES DE TRAITEMENT DE MALIGNITÉS RÉSISTANTES À UN INHIBITEUR DE TYROSINE KINASE CHEZ DES PATIENTS AYANT DES POLYMORPHISMES GÉNÉTIQUES OU DES DÉRÉGULATIONS OU DES MUTATIONS D'AHI1 À L'AIDE DE DIANHYDROGALACTITOL, DIACÉTYLDIANHYDROGALACTITOL, DIBROMODULCITOL OU DES ANALOGUES OU DÉRIVÉS CORRESPONDANTS
  申请人：DEL MAR PHARMACEUTICALS

  公开号：WO2014004376A2

  公开（公告）日：2014-01-03

  Methods and compositions suitable for the treatment of malignancies in subjects with a germline deletion polymorphism that blocks the activity of thymidine kinase inhibitors in triggering apoptosis in tumor cells or in subjects having a mutation in or a dysregulation of the AHI1 gene are disclosed. These methods employ an alkylating hexitol derivative such as dianhydrogalactitol, a derivative or analog of dianhydrogalactitol, diacetyldianhydrogalactitol, a derivative or analog of diacetyldianhydrogalactitol, dibromodulcitol, and a derivative or analog of dibromodulcitol. The compositions can include such alkylating hexitol derivatives. The methods can further include administration of a BH3 mimetic, and the compositions can further include a BH3 mimetic. In subjects having a dysregulation of the AHI1 gene, the methods can further include the administration of an agent modulating the expression or activity of the AHI1 gene or AHI1 protein, and the compositions can further include such an agent.
• [EN] FUSED HETEROCYCLIC COMPOUNDS AS RET KINASE INHIBITORS<br/>[FR] COMPOSÉS HÉTÉROCYCLIQUES CONDENSÉS COMME INHIBITEURS DE KINASES RET
  申请人：ARRAY BIOPHARMA INC

  公开号：WO2020055672A1

  公开（公告）日：2020-03-19

  Provided herein are compounds of the Formula (I): (I) and tautomers, stereoisomers and pharmaceutically acceptable salts and solvates thereof, wherein Rx, Ry, W, X, Y, Z, Ring A and (AA) have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including RET-associated diseases and disorders.