N-(2-diethylamino-ethyl)-2-(4-trifluoromethoxy-phenylamino)-benzamide | 1173002-43-1

• 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: N-(2-diethylamino-ethyl)-2-(4-trifluoromethoxy-phenylamino)-benzamide
• 英文别名: N-[2-(diethylamino)ethyl]-2-[4-(trifluoromethoxy)anilino]benzamide
• CAS: 1173002-43-1
• 化学式: C₂₀H₂₄F₃N₃O₂
• 分子量: 395.425
• InChiKey: QOWOCAIBBUSUOK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.3
• 重原子数：
  28
• 可旋转键数：
  9
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.35
• 拓扑面积：
  53.6
• 氢给体数：
  2
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  邻碘苯甲酰氯 在 copper(l) iodide potassium carbonate 、 L-脯氨酸 、 sodium hydroxide 作用下， 以 二氯甲烷 、 水 、 二甲基亚砜 为溶剂， 反应 66.0h， 生成 N-(2-diethylamino-ethyl)-2-(4-trifluoromethoxy-phenylamino)-benzamide
  参考文献：
  名称：

  Compounds for use as therapeutic agents affecting p53 expression and/or activity

  摘要：

  本发明涉及化合物(I)，其中R1和R2分别代表氢原子，(C1-C4)烷氧基，氟代(C1-C4)烷氧基，羟基，苄氧基，二(C1-C4)烷基氨基，吡啶基乙烯基，嘧啶基乙烯基，苯乙烯基，或-NHCO苯基；R3、R4和R5分别代表氢原子，(C1-C4)烷基，CONHR6基团，-CONR7R8基团，-SO2NHR6基团，或杂环烷基，可选择地被卤原子取代，-(CH2)nNR7R8基团或羟基(C1-C4)烷基；R6代表氢原子，-(CHR9)m(CH2)nNR7R8基团或(C1-C6)烷基，可选择地被羟基取代；或其药学上可接受的盐之一，用作预防、抑制或治疗患有该疾病的患者的药剂，所述疾病涉及到p53蛋白的失调。其中一些化合物是新的，也是本发明的一部分。

  公开号：

  EP2505198A1

文献信息

• CHEMICAL MOLECULES THAT INHIBIT THE SLICING MECHANISM FOR TREATING DISEASES RESULTING FROM SPLICING ANOMALIES
  申请人：Tazi Jamal

  公开号：US20110053975A1

  公开（公告）日：2011-03-03

  The present invention relates to a compound of one of the formulas I to XXI; a pharmaceutical composition comprising at least one such compound; and the use of at least one such compound in preparing a drug to treat, in a subject, a genetic disease resulting from at least one splicing anomaly.

  本发明涉及公式I至XXI中的化合物之一；包含至少一种这种化合物的药物组合物；以及使用至少一种这种化合物来制备一种药物，用于治疗主体中由至少一个剪接异常导致的遗传疾病。
• COMPOUNDS FOR USE AS THERAPEUTIC AGENTS AFFECTING P53 EXPRESSION AND/OR ACTIVITY
  申请人：Scherrer Didier

  公开号：US20140206690A1

  公开（公告）日：2014-07-24

  The present invention relates to compound (I) wherein R1 and R2 independently represent a hydrogen atom, a (C 1 -C 4 )alkoxy group, a fluoro(C 1 -C 4 )alkoxy group, a hydroxyl group, a benzyloxy group, a di(C 1 -C 4 )alkylamino group, a pyridyl-vinyl group, a pyrimidinyl-vinyl group, a styryl group, or a —NHCOphenyl group; R3, R4 and R5 independently represent a hydrogen atom, a (C 1 -C 4 )alkyl group, a CONHR6 group, a —CONR7R8 group, a —SO 2 NHR6 group, or a heteroaryl group optionally substituted by a halogen atom, a —(CH 2 ) n NR7R8 group or a hydroxy(C 1 -C 4 )alkyl group; R6 represents a hydrogen atom, a —(CHR9) m (CH 2 ) n NR7R8 group or a (C 1- C 6 )alkyl group optionally substituted by a hydroxyl group; or anyone of its pharmaceutically acceptable salt, for use in a method for preventing, inhibiting or treating a disease in a patient suffering thereof, said disease involving a deregulated p53. Some of said compounds are new and also form part of the invention.

  本发明涉及化合物(I)，其中R1和R2分别表示氢原子，(C1-C4)烷氧基，氟(C1-C4)烷氧基，羟基，苄氧基，二(C1-C4)烷基氨基，吡啶基乙烯基，嘧啶基乙烯基，苯乙烯基或—NHCO苯基；R3，R4和R5分别表示氢原子，(C1-C4)烷基，CONHR6基，—CONR7R8基，—SO2NHR6基或杂环基，所述杂环基可选地被卤原子，—(CH2)nNR7R8基或羟基(C1-C4)烷基取代；R6表示氢原子，—(CHR9)m(CH2)nNR7R8基或(C1-C6)烷基，可选地被羟基取代；或其药学上可接受的盐之一，用于预防，抑制或治疗患有p53失调的患者的疾病的方法。其中一些化合物是新的，也是本发明的一部分。
• CHEMICAL MOLECULES THAT INHIBIT THE SPLICING MECHANISM FOR TREATING DISEASES RESULTING FROM SPLICING ANOMALIES
  申请人：CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE - CNRS

  公开号：EP3536691A1

  公开（公告）日：2019-09-11

  The present invention relates to specific compounds; pharmaceutical composition comprising at least one of said compounds; and the use of at least one of said compounds in preparing a drug to treat, in a subject, a genetic disease resulting from at least one splicing anomaly.

  本发明涉及特定化合物；包含至少一种所述化合物的药物组合物；以及使用至少一种所述化合物制备药物，以治疗受试者因至少一种剪接异常导致的遗传疾病。
• Chemical molecules that inhibit the slicing mechanism for treating diseases resulting from splicing anomalies
  申请人：CENTRE NATIONALE DE RECHERCHE SCIENTIFIQUE

  公开号：US10130595B2

  公开（公告）日：2018-11-20

  A method of treating a disease selected from the group consisting of cancer, Duchenne muscular dystrophy, AIDS, and progeria, that includes administering to a patient in need thereof an effective quantity of at least one compound of formula (IV) or a pharmaceutically acceptable salt thereof.

  一种治疗选自癌症、杜氏肌营养不良症、艾滋病和早衰症的疾病的方法，包括向有需要的患者施用有效量的至少一种式（IV）化合物或其药学上可接受的盐。
• Compounds for use as therapeutic agents affecting P53 expression and/or activity
  申请人：ABIVAX

  公开号：US10538485B2

  公开（公告）日：2020-01-21

  The present disclosure relates to compound (I) wherein R1 and R2 independently represent a hydrogen atom, a (C1-C4)alkoxy group, a fluoro(C1-C4)alkoxy group, a hydroxyl group, a benzyloxy group, a di(C1-C4)alkylamino group, a pyridyl-vinyl group, a pyrimidinyl-vinyl group, a styryl group, or a —NHCOphenyl group; R3, R4 and R5 independently represent a hydrogen atom, a (C1-C4)alkyl group, a CONHR6 group, a —CONR7R8 group, a —SO2NHR6 group, or a heteroaryl group optionally substituted by a halogen atom, a —(CH2)nNR7R8 group or a hydroxy(C1-C4)alkyl group; R6 represents a hydrogen atom, a —(CHR9)m(CH2)nNR7R8 group or a (C1-C6)alkyl group optionally substituted by a hydroxyl group; or anyone of its pharmaceutically acceptable salt, for use in a method for preventing, inhibiting or treating a disease in a patient suffering thereof, said disease involving a deregulated p53. Some of said compounds are new and also form part of the disclosure.

  本公开涉及化合物 (I) 其中 R1 和 R2 独立地代表氢原子、(C1-C4)烷氧基、氟(C1-C4)烷氧基、羟基、苄氧基、二(C1-C4)烷基氨基、吡啶基乙烯基、嘧啶基乙烯基、苯乙烯基或 -NHCOphenyl 基；R3、R4 和 R5 各自代表氢原子、(C1-C4)烷基、CONHR6 基团、-CONR7R8 基团、-SO2NHR6 基团或任选被卤素原子、-(CH2)nNR7R8 基团或羟基(C1-C4)烷基取代的杂芳基；R6代表氢原子、-(CHR9)m(CH2)nNR7R8基团或任选被羟基取代的(C1-C6)烷基；或其任何药学上可接受的盐，用于预防、抑制或治疗患者的疾病，所述疾病涉及p53失调。其中一些化合物是新化合物，也是本公开的一部分。