(Z)-3-{1-[4-(N-(2-dimethylamino-ethyl)-N-methylsulphonylamino)-phenylamino]-1-phenyl-methylidene}-2-indolinone | 262367-70-4

• 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: (Z)-3-{1-[4-(N-(2-dimethylamino-ethyl)-N-methylsulphonylamino)-phenylamino]-1-phenyl-methylidene}-2-indolinone
• 英文别名: (Z)-3-(1-(4-(N-(2-dimethylamino-ethyl)-N-methylsulfonyl-amino)-phenyl-amino)-1-phenyl-methylene)-2-indolinone；N-[2-(dimethylamino)ethyl]-N-[4-[[(Z)-(2-oxo-1H-indol-3-ylidene)-phenylmethyl]amino]phenyl]methanesulfonamide
• CAS: 262367-70-4
• 化学式: C₂₆H₂₈N₄O₃S
• 分子量: 476.599
• InChiKey: SGVAUCIEUYKEQF-IZHYLOQSSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.4
• 重原子数：
  34
• 可旋转键数：
  8
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.19
• 拓扑面积：
  90.1
• 氢给体数：
  2
• 氢受体数：
  6

文献信息

• 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。
• Novel substituted indolines with an inhibitory effect on various kinases and complexes of CDKs
  申请人：Boehringer Ingelheim Pharma KG

  公开号：US20040058978A1

  公开（公告）日：2004-03-25

  The present invention relates to new substituted indolinones of general formula 1 wherein X and R 1 to R 5 are defined as in claim 1, the isomers and the salts thereof which have valuable properties. The above compounds of general formula I wherein R 1 denotes a hydrogen atom, a C 1-3 -alkyl group or a prodrug group have valuable pharmacological properties, particularly an inhibiting effect on various kinases, on viral cyclin and on receptor tyrosine kinases, and the other compounds of the above general formula I wherein R 1 does not represent a hydrogen atom, a C 1-3 -alkyl group or a prodrug group are valuable intermediate products for the preparation of the abovementioned compounds.

  本发明涉及一种新的通式1的取代吲哚酮，其中X和R1至R5的定义如权利要求书1中所述，其异构体和盐具有有价值的性质。通式I中的上述化合物，其中R1表示氢原子，C1-3-烷基或前药基，具有有价值的药理学性质，特别是对多种激酶、病毒细胞周期蛋白和受体酪氨酸激酶具有抑制作用，上述通式I中R1不表示氢原子、C1-3-烷基或前药基的其他化合物是制备上述化合物的有价值中间体。
• 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。
• Combinations for the treatment of diseases involving cell proliferation, migration or apoptosis of myeloma cells, or angiogenesis
  申请人：BOEHRINGER INGELHEIM INTERNATIONAL GMBH

  公开号：EP2361626A1

  公开（公告）日：2011-08-31

  The present invention relates to a pharmaceutical combination for the treatment of diseases which involves cell proliferation, migration or apoptosis of myeloma cells, or angiogenesis. The invention also relates to a method for the treatment of said diseases, comprising co-administration of effective amounts of specific active compounds and/or co-treatment with radiation therapy, in a ratio which provides an additive and synergistic effect, and to the combined use of these specific compounds and/or radiotherapy for the manufacture of corresponding pharmaceutical combination preparations.

  本发明涉及一种药物组合，用于治疗涉及骨髓瘤细胞增殖、迁移或凋亡或血管生成的疾病。本发明还涉及一种治疗上述疾病的方法，包括以提供相加和协同效应的比例联合给药有效量的特定活性化合物和/或联合放射治疗，以及联合使用这些特定化合物和/或放射治疗来制造相应的药物组合制剂。
• Combinations for the treatment of diseases involving cell proliferation, migration or apoptosis of myeloma cells or angiogenesis
  申请人：BOEHRINGER INGELHEIM INTERNATIONAL GMBH

  公开号：EP2409705A1

  公开（公告）日：2012-01-25

  The present invention relates to a pharmaceutical combination for the treatment of diseases which involves cell proliferation, migration or apoptosis of myeloma cells, or angiogenesis. The invention also relates to a method for the treatment of said diseases, comprising co-administration of effective amounts of specific active compounds and/or co-treatment with radiation therapy, in a ratio which provides an additive and synergistic effect, and to the combined use of these specific compounds and/or radiotherapy for the manufacture of corresponding pharmaceutical combination preparations.

  本发明涉及一种药物组合，用于治疗涉及骨髓瘤细胞增殖、迁移或凋亡或血管生成的疾病。本发明还涉及一种治疗上述疾病的方法，包括以提供相加和协同效应的比例联合给药有效量的特定活性化合物和/或联合放射治疗，以及联合使用这些特定化合物和/或放射治疗来制造相应的药物组合制剂。