pyridine-2,5-dicarboxylic acid 5-[(2-amino-phenyl)-amide] 2-[(2-diethylamino-ethyl)-methyl-amide]

• 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: pyridine-2,5-dicarboxylic acid 5-[(2-amino-phenyl)-amide] 2-[(2-diethylamino-ethyl)-methyl-amide]
• 英文别名: 5-N-(2-aminophenyl)-2-N-[2-(diethylamino)ethyl]-2-N-methylpyridine-2,5-dicarboxamide
• 化学式: C₂₀H₂₇N₅O₂
• 分子量: 369.467
• InChiKey: RCFJUQOFYZHFBB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  27
• 可旋转键数：
  8
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.35
• 拓扑面积：
  91.6
• 氢给体数：
  2
• 氢受体数：
  5

文献信息

• Mono-acylated o-phenylendiamines derivatives
  申请人：——

  公开号：US20040162317A1

  公开（公告）日：2004-08-19

  Mono-acylated o-phenylendiamines derivatives of formula A 1 wherein Ar, R 1 , and R 2 are as described herein, have been found useful for the treatment of diseases mediated by the inhibition of histone deacetylase, such as cancer.

  公式A1中的单酰化的邻苯二胺衍生物，其中Ar，R1和R2如此描述，已被发现对于治疗由组蛋白去乙酰化酶抑制剂介导的疾病，如癌症，具有有用的作用。
• NEW MONO-ACYLATED O-PHENYLENDIAMINES DERIVATIVES
  申请人：F. HOFFMANN-LA ROCHE AG

  公开号：EP1592667A2

  公开（公告）日：2005-11-09
• [EN] NEW MONO-ACYLATED O-PHENYLENDIAMINES DERIVATIVES<br/>[FR] NOUVEAUX DÉRIVÉS D'O-PHÉNYLENDIAMINES MONOACYLÉES
  申请人：HOFFMANN LA ROCHE

  公开号：WO2004069803A2

  公开（公告）日：2004-08-19

  Objects of the present invention are new mono-acylated o-phenylendiamines derivatives of formula (A) wherein Ar is thiophen-2,5-diyl, pyridine-2,5-diyl, pyridine-5,2-diyl, pyridine-2,6-diyl, pyridine-2,4-diyl or 1,4-phenylene, R1, R2 independently from each other represent hydrogen, C1-12-alkyl, C2-12-alkenyl, C2-12-alkynyl, C3-12-cycloalkyl, the alkyl, alkenyl, alkynyl and cycloalkyl groups being optionally mono or multiple substituted by hydroxy, halogen, C3-12-cycloalkyl, alkoxy, alkylsulfanyl, acyloxy, alkoxycarbonyl, acyl, C1-6-alkyl-NH-C(O)-, C1-6-alkyl-C(O)NH- or -NR3R4, or alternatively R1 is hydrogen, and R2 is hydroxyl, alkoxy, C2-C12-alkenyloxy or phenoxy, which phenoxy group is optionally substituted with methyl, methoxy, halogen, nitro, cyano, trifluoromethyl, ethenyl or -C(O)-O-CH3, provided that if R2 is hydroxy, Ar is not thiophen-2,5-diyl; and R3 and R4 independently from each other represent hydrogen or C1-6-alkyl, or wherein R3 and R4 together with the nitrogen-atom to which they are attached form a ring, which ring is monosubstituted by oxo and which ring may contain a further heteroatom, and pharmaceutically acceptable salts thereof, as well as processes for the manufacturing of these compounds, pharmaceutical compositions containing such compounds and their use in the manufacture of drugs for the treatment of diseases such as cancer.