5-bromo-4-chloro-2-fluorobenzamide

• 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: 5-bromo-4-chloro-2-fluorobenzamide
• 英文别名: 5-Bromo-4-chloro-2-fluorobenzamide
• 化学式: C₇H₄BrClFNO
• 分子量: 252.47
• InChiKey: CYAYBPWXTDFNIJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  12
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  43.1
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  5-bromo-4-chloro-2-fluorobenzamide 在 tris-(dibenzylideneacetone)dipalladium(0) 、 N-氯代丁二酰亚胺 、 碳酸氢钠 、 溶剂黄146 、 N,N-二异丙基乙胺 、 4,5-双二苯基膦-9,9-二甲基氧杂蒽 作用下， 以 四氢呋喃 、 1,4-二氧六环 、 水 为溶剂， 反应 5.1h， 生成 4-chloro-2-fluoro-5-(N-(1-methylcyclopropyl)sulfamoyl)benzamide
  参考文献：
  名称：

  [EN] 2,4-DIOXO-1,4-DIHYDROQUINAZOLINE DERIVATIVES AS PARG INHIBITORS FOR THE TREATMENT OF CANCER
  [FR] DÉRIVÉS DE 2,4-DIOXO-1,4-DIHYDROQUINAZOLINE UTILISÉS COMME INHIBITEURS DE PARG POUR LE TRAITEMENT DU CANCER

  摘要：

  The present invention relates to a compound of formula (I) or an enantiomer, diastereoisomer, tautomer, pharmaceutically acceptable solvate, pharmaceutically acceptable crystal form, or pharmaceutically acceptable salt thereof. The present invention further relates to the compound of formula (I) of the present invention for use in therapy. Instant compounds are particularly useful as PARG inhibitors, preferably as covalent PARG inhibitors, and can be used in a method of treatment of a proliferative disorder, preferably of cancer.

  公开号：

  WO2023175184A1
• 作为产物：
  描述：

  5-溴-4-氯-2-氟苯甲酸 在 氯化铵 、 N,N-二异丙基乙胺 、 Methanaminium,N-[(dimethylamino)(3H-1,2,3-triazolo[4,5-b]pyridin-3-yloxy)methylene]-N-methyl-, hexafluorophosphate(1-) 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 以85.33 %的产率得到5-bromo-4-chloro-2-fluorobenzamide
  参考文献：
  名称：

  [EN] 2,4-DIOXO-1,4-DIHYDROQUINAZOLINE DERIVATIVES AS PARG INHIBITORS FOR THE TREATMENT OF CANCER
  [FR] DÉRIVÉS DE 2,4-DIOXO-1,4-DIHYDROQUINAZOLINE UTILISÉS COMME INHIBITEURS DE PARG POUR LE TRAITEMENT DU CANCER

  摘要：

  The present invention relates to a compound of formula (I) or an enantiomer, diastereoisomer, tautomer, pharmaceutically acceptable solvate, pharmaceutically acceptable crystal form, or pharmaceutically acceptable salt thereof. The present invention further relates to the compound of formula (I) of the present invention for use in therapy. Instant compounds are particularly useful as PARG inhibitors, preferably as covalent PARG inhibitors, and can be used in a method of treatment of a proliferative disorder, preferably of cancer.

  公开号：

  WO2023175184A1

文献信息

• [EN] BIARYL-CONTAINING COMPOUNDS AS INVERSE AGONISTS OF ROR-GAMMA RECEPTORS<br/>[FR] COMPOSÉS CONTENANT BIARYLE COMME AGONISTES INVERSES DE RÉCEPTEURS ROR-GAMMA
  申请人：BIOGEN IDEC INC

  公开号：WO2014008214A1

  公开（公告）日：2014-01-09

  The present invention relates to biaryl-containing inverse agonists of ROR-gamma receptors. The invention also provides pharmaceutical compositions comprising these biaryl- containing inverse agonists, and methods of modulating ROR-gamma receptors using these inverse agonists. Also provided are methods of using biaryl-containing inverse agonists to treat ROR-gamma mediated diseases.

  本发明涉及含有联苯基的ROR-gamma受体的逆激动剂。该发明还提供了包含这些含有联苯基的逆激动剂的药物组合物，以及使用这些逆激动剂调节ROR-gamma受体的方法。同时提供了使用含有联苯基的逆激动剂治疗ROR-gamma介导疾病的方法。
• [EN] 2,4-DIOXO-1,4-DIHYDROQUINAZOLINE DERIVATIVES AS PARG INHIBITORS FOR THE TREATMENT OF CANCER<br/>[FR] DÉRIVÉS DE 2,4-DIOXO-1,4-DIHYDROQUINAZOLINE UTILISÉS COMME INHIBITEURS DE PARG POUR LE TRAITEMENT DU CANCER
  申请人：[en]FORX THERAPEUTICS AG

  公开号：WO2023175184A1

  公开（公告）日：2023-09-21

  The present invention relates to a compound of formula (I) or an enantiomer, diastereoisomer, tautomer, pharmaceutically acceptable solvate, pharmaceutically acceptable crystal form, or pharmaceutically acceptable salt thereof. The present invention further relates to the compound of formula (I) of the present invention for use in therapy. Instant compounds are particularly useful as PARG inhibitors, preferably as covalent PARG inhibitors, and can be used in a method of treatment of a proliferative disorder, preferably of cancer.