3-benzyl-2-chloro-6-methyl-N-phenylpyridine-4-carboxamide

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 3-benzyl-2-chloro-6-methyl-N-phenylpyridine-4-carboxamide
• 化学式: C₂₀H₁₇ClN₂O
• 分子量: 336.8
• InChiKey: ODCYZPSEGPKUHU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5
• 重原子数：
  24
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.1
• 拓扑面积：
  42
• 氢给体数：
  1
• 氢受体数：
  2

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
• THERAPEUTIC BENEFIT OF SUBOPTIMALLY ADMINISTERED CHEMICAL COMPOUNDS
  申请人：Brown, Dennis M.

  公开号：EP2983674A1

  公开（公告）日：2016-02-17
• [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] THERAPEUTIC BENEFIT OF SUBOPTIMALLY ADMINISTERED CHEMICAL COMPOUNDS<br/>[FR] BÉNÉFICE THÉRAPEUTIQUE DE COMPOSÉS CHIMIQUES ADMINISTRÉS DE FAÇON SOUS-OPTIMALE
  申请人：BROWN DENNIS M

  公开号：WO2014168986A1

  公开（公告）日：2014-10-16

  The present invention describes methods and compositions for improving the therapeutic efficacy of therapeutic agents previously limited by suboptimal therapeutic performance by either improving efficacy as monotherapy or reducing side effects. Such methods and compositions are particularly applicable to mustard-based alkylating agents such as uracil mustard and analogs, derivatives, or prodrugs thereof, including 6-methyluracil mustard and 6-ethyluracil mustard.
• [EN] USE OF DIANHYDROGALACTITOL OR DERIVATIVES AND ANALOGS THEREOF FOR TREATMENT OF NON-SMALL-CELL LUNG CARCINOMA, GLIOBLASTOMA, AND OVARIAN CARCINOMA BY INDUCTION OF DNA DAMAGE AND STALLING OF CELL CYCLE<br/>[FR] UTILISATION DE DIANHYDROGALACTITOL OU DE DÉRIVÉS ET D'ANALOGUES DE CELUI-CI POUR LE TRAITEMENT D'UN CARCINOME NON À PETITES CELLULES, D'UN GLIOBLASTOME ET D'UN CARCINOME DE L'OVAIRE PAR INDUCTION DE LÉSIONS DE L'ADN ET BLOCAGE DU CYCLE CELLULAIRE
  申请人：DEL MAR PHARMACEUTICALS

  公开号：WO2017042634A2

  公开（公告）日：2017-03-16

  The use of dianhydrogalactitol provides a novel therapeutic modality for the treatment of glioblastoma, non-small-cell lung carcinoma (NSCLC) and ovarian cancer, as well as other types of malignancy, including brain metastases of NSCLC. Dianhydrogalactitol acts as an alkylating agent on DNA that creates N7 methylation and inter-strand crosslinks that can induce double-stranded breaks in DNA. Dianhydrogalactitol is effective in suppressing the growth of cancer stem cells and is active against tumors that are refractory to temozolomide, cisplatin, and tyrosine kinase inhibitors; the drug acts independently of the MGMT repair mechanism. Dianhydrogalactitol can be used together with other anti-neoplastic agents and can possess additive or synergistic effects. Dianhydrogalactitol can be used for treatment of leptomeningeal carcinomatosis.