N-ethyl-N-methyl-2-nitrobenzenesulfonamide | 1097920-41-6

• 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-ethyl-N-methyl-2-nitrobenzenesulfonamide
• CAS: 1097920-41-6
• 化学式: C₉H₁₂N₂O₄S
• 分子量: 244.271
• InChiKey: RMWUFJXWGLQJDI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.3
• 重原子数：
  16
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  91.6
• 氢给体数：
  0
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  N-乙基甲基胺 、 邻硝基苯磺酰氯 在 三乙胺 作用下， 以 氯仿 为溶剂， 生成 N-ethyl-N-methyl-2-nitrobenzenesulfonamide
  参考文献：
  名称：

  EP2172461

  摘要：

  公开号：

文献信息

• DI(ARYLAMINO)ARYL COMPOUND
  申请人：Kondoh Yutaka

  公开号：US20100099658A1

  公开（公告）日：2010-04-22

  The present invention provides a compound which is useful as an inhibitor against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins. As a result of extensive and intensive studies on compounds having an inhibitory effect against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins, the inventors of the present invention have found that the di(arylamino)aryl compound of the present invention has inhibitory activity against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins. This finding led to the completion of the present invention. The compound of the present invention can be used as a pharmaceutical composition for preventing and/or treating cancer, lung cancer, non-small cell lung cancer, small cell lung cancer, EML4-ALK fusion polynucleotide-positive and/or mutant EGFR polynucleotide-positive cancer, EML4-ALK fusion polynucleotide-positive and/or mutant EGFR polynucleotide-positive lung cancer, or EML4-ALK fusion polynucleotide-positive and/or mutant EGFR polynucleotide-positive non-small cell lung cancer, etc.

  本发明提供了一种化合物，可用作抑制EML4-ALK融合蛋白和突变EGFR蛋白的激酶活性的抑制剂。在广泛而深入的研究EML4-ALK融合蛋白和突变EGFR蛋白的激酶活性的化合物的基础上，本发明的发明人发现本发明的二(芳基氨基)芳基化合物具有抑制EML4-ALK融合蛋白和突变EGFR蛋白的激酶活性的活性。这一发现导致了本发明的完成。本发明的化合物可用作预防和/或治疗癌症、肺癌、非小细胞肺癌、小细胞肺癌、EML4-ALK融合多核苷酸阳性和/或突变EGFR多核苷酸阳性癌症、EML4-ALK融合多核苷酸阳性和/或突变EGFR多核苷酸阳性肺癌，或EML4-ALK融合多核苷酸阳性和/或突变EGFR多核苷酸阳性非小细胞肺癌等的药物组合物。
• Di(arylamino)aryl compounds
  申请人：Astellas Pharma Inc.

  公开号：US08318702B2

  公开（公告）日：2012-11-27

  The present invention provides a compound which is useful as an inhibitor against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins. As a result of extensive and intensive studies on compounds having an inhibitory effect against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins, the inventors of the present invention have found that the di(arylamino)aryl compound of the present invention has inhibitory activity against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins. This finding led to the completion of the present invention. The compound of the present invention can be used as a pharmaceutical composition for preventing and/or treating cancer, lung cancer, non-small cell lung cancer, small cell lung cancer, EML4-ALK fusion polynucleotide-positive and/or mutant EGFR polynucleotide-positive cancer, EML4-ALK fusion polynucleotide-positive and/or mutant EGFR polynucleotide-positive lung cancer, or EML4-ALK fusion polynucleotide-positive and/or mutant EGFR polynucleotide-positive non-small cell lung cancer, etc.

  本发明提供了一种化合物，可作为抑制EML4-ALK融合蛋白和突变EGFR蛋白激酶活性的抑制剂。通过对具有抑制EML4-ALK融合蛋白和突变EGFR蛋白激酶活性的化合物进行广泛和深入的研究，本发明的发明人发现了本发明的二(芳基氨基)芳基化合物具有抑制EML4-ALK融合蛋白和突变EGFR蛋白激酶活性的活性。这一发现促成了本发明的完成。本发明的化合物可用作预防和/或治疗癌症、肺癌、非小细胞肺癌、小细胞肺癌、EML4-ALK融合多核苷酸阳性和/或突变EGFR多核苷酸阳性癌症、EML4-ALK融合多核苷酸阳性和/或突变EGFR多核苷酸阳性肺癌或EML4-ALK融合多核苷酸阳性和/或突变EGFR多核苷酸阳性非小细胞肺癌等的药物组合物。
• Somatostatin antagonists
  申请人：Coy H. David

  公开号：US20080020970A1

  公开（公告）日：2008-01-24

  A 1 -cycloD-Cys-A 2 -D-Trp-A 3 -A 4 -Cys}-A 5 -Y 1 (I) The present invention is directed to a somatostatin antagonist according to formula (I), wherein A 1 is an optionally substituted aromatic ax-amino acid; A 2 is an optionally substituted aromatic α-amino acid; A 3 is Dab, Dap, Lys or Orn; A 4 is β-Hydroxyvaline, Ser, Hser, or Thr; A 5 is an optionally substituted D- or L-aromatic-amino acid; and Y 1 is OH, NH 2 or NHR 1 , where R 1 is (C 1-6 )alkyl; wherein each said optionally substituted aromatic-amino acid is optionally substituted with one or more substituents each independently selected from the group consisting of halogen, NO 2 , OH, CN, (C 1-6 )alkyl, (C 2-6 )alkenyl, (C 2-6 )alkynyl, (C 1-6 )alkoxy, Bzl, O-Bzl, and NR 9 R 10 , where R 9 ad R 10 each is independently H, O, or (C 1-6 )alkyl; and wherein the amine nitrogen of each of amide peptide bond and the amino group of A 1 of formula (I) is optionally substituted with a methyl group, provided that there is at least one said methyl group; or a pharmaceutically acceptable salt thereof, and to uses thereof.
• US7378488B2
  申请人：——

  公开号：US7378488B2

  公开（公告）日：2008-05-27
• US7408024B2
  申请人：——

  公开号：US7408024B2

  公开（公告）日：2008-08-05