(E) (Z)-3-(1-(4-(piperidin-1-yl-methyl)-phenylamino)-1-phenyl-methylene)-5-(4-amino-phenylsulfonylamino)-2-indolinone | 422513-50-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: (E) (Z)-3-(1-(4-(piperidin-1-yl-methyl)-phenylamino)-1-phenyl-methylene)-5-(4-amino-phenylsulfonylamino)-2-indolinone
• 英文别名: (Z)-3-(1-(4-(piperidin-1-yl-methyl)-phenylamino)-1-phenyl-methylene)-5-(4-amino-phenylsulfonylamino)-2-indolinone；(Z)-3-[1-(4-piperidinomethyl-phenylamino)-1-phenyl-methylidene]-5-(4-aminophenylsulphonylamino)-2-indolinone；4-amino-N-[(3Z)-2-oxo-3-[phenyl-[4-(piperidin-1-ylmethyl)anilino]methylidene]-1H-indol-5-yl]benzenesulfonamide
• CAS: 422513-50-6
• 化学式: C₃₃H₃₃N₅O₃S
• 分子量: 579.723
• InChiKey: SVBJQIKBRMJODN-MVJHLKBCSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.8
• 重原子数：
  42
• 可旋转键数：
  8
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.18
• 拓扑面积：
  125
• 氢给体数：
  4
• 氢受体数：
  7

文献信息

• Substituted indolinones, preparation thereof and their use as pharmaceutical compositions
  申请人：——

  公开号：US20030069299A1

  公开（公告）日：2003-04-10

  Indolinones of general formula I 1 which are inhibitors of cell proliferation, particularly of tumour cells, and inhibitors of protein kinases. The following compounds are exemplary: (Z)-3-{1-[4-(N-(2-aminoethyl)-N-methylsulphonyl-amino)-phenylamino]-1-phenyl-methylidene}-5-phenylsulphonylamino-2-indolinone, (Z)-3-{1 -[4-(N-(2-dimethylaminoethyl)-N-phenylsulphonyl-amino)-phenylamino]-1-phenyl-methylidene}-5-phenylsulphonylamino-2-indolinone, and (Z)-3-{1-[4-(4-methylpiperazinomethyl)-phenylamino]-1-phenyl-methylidene}-5-phenylsulphonylamino-2-indolinone.

  通用公式I1的吲哚酮是细胞增殖抑制剂，特别是肿瘤细胞的抑制剂，也是蛋白激酶的抑制剂。以下化合物是示例性的：(Z)-3-1-[4-(N-(2-氨基乙基)-N-甲基磺酰氨基)苯氨基]-1-苯甲基亚甲基}-5-苯磺酰氨基-2-吲哚酮，(Z)-3-1-[4-(N-(2-二甲基氨基乙基)-N-苯磺酰氨基)苯氨基]-1-苯甲基亚甲基}-5-苯磺酰氨基-2-吲哚酮，以及(Z)-3-1-[4-(4-甲基哌嗪甲基)苯氨基]-1-苯甲基亚甲基}-5-苯磺酰氨基-2-吲哚酮。
• Use of Lck inhibitors for treatment of immunologic diseases
  申请人：Boehringer Ingelheim Pharma GmbH & Co. KG

  公开号：US20040204458A1

  公开（公告）日：2004-10-14

  The invention relates to a method of treating immunologic diseases or pathological conditions involving an immunologic component using certain Lck inhibitors already known as kinase inhibitors for therapy in oncology, optionally in combination with one or more other drugs selected from NSAIDs, steroids, DMARDs, immunsuppressives, biologic response modifiers and antinfectives, pharmaceutical compositions comprising said Lck inhibitors together with said other drugs, and the use of the Lck inhibitors for the manufacture of a pharmaceutical composition for the treatment of immunologic diseases or pathological conditions involving an immunologic component.

  该发明涉及一种治疗免疫性疾病或涉及免疫组分的病理条件的方法，使用某些已知为激酶抑制剂的Lck抑制剂进行治疗肿瘤学，可选择与来自NSAIDs、类固醇、DMARDs、免疫抑制剂、生物反应调节剂和抗感染药物中的一个或多个其他药物结合，包括所述Lck抑制剂和所述其他药物的药物组合物，以及利用Lck抑制剂制备用于治疗涉及免疫组分的免疫性疾病或病理条件的制药组合物。
• New substituted indolinones, preparation thereof and their use as pharmaceutical compositions
  申请人：Boehringer Ingelheim Pharma KG

  公开号：US20040044222A1

  公开（公告）日：2004-03-04

  Indolinones of general formula I 1 which are inhibitors of cell proliferation, particularly of tumour cells, and inhibitors of protein kinases.

  通式为I1的吲哚酮类化合物是细胞增殖抑制剂，尤其是肿瘤细胞的抑制剂，同时也是蛋白激酶的抑制剂。
• Use of LCK inhibitors for treatment of immunologic diseases
  申请人：Boehringer Ingelheim Pharma GmbH & Co. KG

  公开号：EP2281561A2

  公开（公告）日：2011-02-09

  The invention relates to a method of treating immunologic diseases or pathological conditions involving an immunologic component using certain Lck inhibitors already known as kinase inhibitors for therapy in oncology, optionally in combination with one or more other drugs selected from NSAIDs, steroids, DMARDs, immunsuppressives, biologic response modifiers and antinfectives, pharmaceutical compositions comprising said Lck inhibitors together with said other drugs, and the use of the Lck inhibitors for the manufacture of a pharmaceutical composition for the treatment of immunologic diseases or pathological conditions involving an immunologic component.

  本发明涉及一种治疗涉及免疫成分的免疫性疾病或病理条件的方法，该方法使用某些已被称为肿瘤学治疗激酶抑制剂的Lck抑制剂，可选择与一种或多种选自非甾体抗炎药、类固醇、DMARDs、免疫抑制剂、生物反应调节剂和抗感染药的其他药物联合使用，药物组合物包含所述Lck抑制剂和所述其他药物，以及使用Lck抑制剂制造用于治疗免疫性疾病或病理条件的药物组合物、生物反应调节剂和抗感染药，由所述 Lck 抑制剂和所述其它药物组成的药物组合物，以及使用 Lck 抑制剂制造用于治疗免疫性疾病或涉及免疫成分的病理状况的药物组合物。
• SULFONYLAMINO SUBSTITUIERTE 3-(AMINOMETHYLIDEN)-2-INDOLINONE ALS INHIBITOREN DER ZELLPROLIFERATION
  申请人：Boehringer Ingelheim Pharma GmbH & Co.KG

  公开号：EP1341760A1

  公开（公告）日：2003-09-10