N-(3-diethylamino-propyl)-3-[3-((E)-2-pyridin-4-yl-vinyl)-phenylamino]-benzamide | 1173003-00-3

• 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-(3-diethylamino-propyl)-3-[3-((E)-2-pyridin-4-yl-vinyl)-phenylamino]-benzamide
• 英文别名: N-(3-diethylaminopropyl)-3-[3-((E)-2-[pyridin-4-yl]vinyl)phenylamino]benzamide；(E)-N-(3-diethylamino-propyl)-3-[3-(2-pyridin-4-ylvinyl)phenylamino]benzamide；N-[3-(diethylamino)propyl]-3-[3-[(E)-2-pyridin-4-ylethenyl]anilino]benzamide
• CAS: 1173003-00-3
• 化学式: C₂₇H₃₂N₄O
• 分子量: 428.577
• InChiKey: YIZJTUSBTZHCIV-OUKQBFOZSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.1
• 重原子数：
  32
• 可旋转键数：
  11
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.26
• 拓扑面积：
  57.3
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  3-溴苯甲酰氯 在 tris-(dibenzylideneacetone)dipalladium(0) 、 2-二环己基磷-2,4,6-三异丙基联苯 potassium carbonate 、 sodium hydroxide 作用下， 以 二氯甲烷 、 水 、 叔丁醇 为溶剂， 反应 38.0h， 生成 N-(3-diethylamino-propyl)-3-[3-((E)-2-pyridin-4-yl-vinyl)-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。
• NEW ANTI-INVASIVE COMPOUNDS
  申请人：ABIVAX

  公开号：US20150315173A1

  公开（公告）日：2015-11-05

  The present invention relates to a compound of formula (I): wherein A and A′ independently represent a phenylene group or a pyridylene group; R 2 is a hydrogen atom or a (C 1 -C 4 )alkyl group; R 3 is a 2-pyridyl group, 3-pyridyl group, a 4-pyridyl group, a 2-pyrimidinyl group, a 4-pyrimidinyl group or a 5-pyrimidinyl group; R 4 is a carbonyl group or a sulfonyl group; and R 5 is a —NH—(CH 2 ) a —NR 6 R 7 group or a 4-methylpiperazinyl group, with a being an integer from 1 to 4, R 6 and R 7 representing independently a (C 1 -C 4 )alkyl group, or R 6 and R 7 together with the nitrogen atom to which they are linked forming a heterocycle group which is chosen among a 4-methylpiperazinyl group, a morpholino group, a pyrrolidinyl group and a piperidino group; or any one of its pharmaceutically acceptable salt.

  本发明涉及一种化合物，其化学式为（I）：其中A和A'分别表示苯基或吡啶基；R2为氢原子或（C1-C4）烷基；R3为2-吡啶基、3-吡啶基、4-吡啶基、2-嘧啶基、4-嘧啶基或5-嘧啶基；R4为羰基或磺酰基；R5为-NH-(CH2)a-NR6R7基团或4-甲基哌嗪基团，其中a为1至4的整数，R6和R7分别表示独立的（C1-C4）烷基，或者R6和R7与它们连接的氮原子一起形成杂环基团，所述杂环基团选择自4-甲基哌嗪基团、吗啡啉基团、吡咯烷基团和哌啶基团；或其药学上可接受的盐之一。
• 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。