6-[Amino-(4-chloro-phenyl)-(3-methyl-3H-imidazol-4-yl)-methyl]-4-(3-chloro-phenyl)-1-cyclopropylmethyl-1H-quinolin-2-one | 260052-37-7

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 二芳基庚烷
• 英文名称: 6-[Amino-(4-chloro-phenyl)-(3-methyl-3H-imidazol-4-yl)-methyl]-4-(3-chloro-phenyl)-1-cyclopropylmethyl-1H-quinolin-2-one
• 英文别名: 6-[amino-(4-chlorophenyl)-(3-methylimidazol-4-yl)methyl]-4-(3-chlorophenyl)-1-(cyclopropylmethyl)quinolin-2-one
• CAS: 260052-37-7
• 化学式: C₃₀H₂₆Cl₂N₄O
• 分子量: 529.469
• InChiKey: MKUBQPBXFQCRND-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.9
• 重原子数：
  37
• 可旋转键数：
  6
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.2
• 拓扑面积：
  64.2
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  6-[Chloro-(4-chloro-phenyl)-(3-methyl-3H-imidazol-4-yl)-methyl]-4-(3-chloro-phenyl)-1-cyclopropylmethyl-1H-quinolin-2-one 、 盐酸 、 铵 在 water-ethyl acetate 、 乙酸乙酯 、 Brine 、 magnesium sulfate 、 silica 、 Ethyl acetate methanol triethylamine 作用下， 以 四氢呋喃 为溶剂， 反应 2.0h， 以gave 6-[Amino-(4-chloro-phenyl)-(3-methyl-3H-imidazol-4-yl)-methyl]-4-(3-chloro-phenyl)-1-cyclopropylmethyl-1H-quinolin-2-one (1.54 g, 79%) as a yellow foam的产率得到6-[Amino-(4-chloro-phenyl)-(3-methyl-3H-imidazol-4-yl)-methyl]-4-(3-chloro-phenyl)-1-cyclopropylmethyl-1H-quinolin-2-one
  参考文献：
  名称：

  Quinolin-2-one derivatives useful as anticancer agents

  摘要：

  本发明涉及公式1的化合物及其药学上可接受的盐、前药和溶剂化物，其中R1、R2、R3、R4、R5、R6、R7、R8、R9、R10和R11如本文所定义。公式1的上述化合物在哺乳动物的高增殖性疾病治疗中有用，例如癌症。本发明还涉及含有公式1化合物的制药组合物，以及通过向需要此类治疗的哺乳动物注射公式1化合物来抑制异常细胞生长，包括癌症的方法。

  公开号：

  US06495564B1

文献信息

• QUINOLIN-2-ONE DERIVATIVES USEFUL AS ANTICANCER AGENTS
  申请人：Pfizer Products Inc.

  公开号：EP1107962A1

  公开（公告）日：2001-06-20
• US6495564B1
  申请人：——

  公开号：US6495564B1

  公开（公告）日：2002-12-17
• [EN] QUINOLIN-2-ONE DERIVATIVES USEFUL AS ANTICANCER AGENTS<br/>[FR] DERIVES DE QUINOLIN-2-ONE UTILES EN TANT QU'AGENTS ANTICANCEREUX
  申请人：PFIZER PROD INC

  公开号：WO2000012498A1

  公开（公告）日：2000-03-09

  Compounds of formula (1) and pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R8 is H, -OR?12, -NR12R13, -NR12C(O)R13¿, cyano, -C(O)OR?13, -SR12, -(CR13R14)¿t(4-10 membered heterocyclic), wherein t is an integer from 0 to 5, or C1-C6 alkyl, wherein said heterocyclic and alkyl moieties are optionally substituted by 1 to 3 R6 substituents; R9 is -(CR13R14)t(imidazolyl) wherein t is an integer from 0 to 5 and said imidazolyl moiety is optionally substituted by 1 or 2 R6 substituents; provided that where R1 is not -(CR13R14)t(C3-C10 cycloalkyl), wherein t is an integer from 0 to 5, then R8 is triazolyl optionally substituted by 1 or 2 R6 groups, or at least one of R?3, R4 and R5¿ is -CH=NOR12 or -S(O)¿jR?12 wherein j is an integer from 0 to 2. The compounds of formula (1) are useful in the treatment of hyperproliferative disorders, such as cancer, in mammals. The invention also relates to pharmaceutical compositions containing the compounds of formula (1) and to methods of inhibiting abnormal cell growth, including cancer, in a mammal by administering the compounds of formula (1) to a mammal requiring such treatment.
• Quinolin-2-one derivatives useful as anticancer agents
  申请人：Pfizer Inc.

  公开号：US06495564B1

  公开（公告）日：2002-12-17

  The present invention relates to compounds of formula 1 and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, and R11 are as defined herein. The above compounds of formula 1 are useful in the treatment of hyperproliferative disorders, such as cancer, in mammals. The invention also relates to pharmaceutical compositions containing the compounds of formula 1 and to methods of inhibiting abnormal cell growth, including cancer, in a mammal by administering the compounds of formula 1 to a mammal requiring such treatment.

  本发明涉及公式1的化合物及其药学上可接受的盐、前药和溶剂化物，其中R1、R2、R3、R4、R5、R6、R7、R8、R9、R10和R11如本文所定义。公式1的上述化合物在哺乳动物的高增殖性疾病治疗中有用，例如癌症。本发明还涉及含有公式1化合物的制药组合物，以及通过向需要此类治疗的哺乳动物注射公式1化合物来抑制异常细胞生长，包括癌症的方法。