2-(cyclopropyloxy)benzene-1-sulfonamide | 1243451-33-3

• 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: 2-(cyclopropyloxy)benzene-1-sulfonamide
• 英文别名: 2-Cyclopropoxybenzenesulfonamide；2-cyclopropyloxybenzenesulfonamide
• CAS: 1243451-33-3
• 化学式: C₉H₁₁NO₃S
• 分子量: 213.257
• InChiKey: FAAFPHPEBJIHFE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1
• 重原子数：
  14
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  77.8
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  2-(cyclopropyloxy)benzene-1-sulfonamide 、 5-bromo-6-(dimethylamino)-1-benzofuran-2-carboxylic acid 在 benzotriazol-1-yloxyl-tris-(pyrrolidino)-phosphonium hexafluorophosphate 、 N,N-二异丙基乙胺 作用下， 以 二氯甲烷 为溶剂， 以56%的产率得到5-bromo-N-[2-(cyclopropyloxy)benzene-1-sulfonyl]-6-(dimethylamino)-1-benzofuran-2-carboxamide
  参考文献：
  名称：

  [EN] ACYL SULFONAMIDES FOR TREATING CANCER
  [FR] ACYLSULFONAMIDES POUR LE TRAITEMENT DU CANCER

  摘要：

  本发明提供了一般式(I)的酰基磺酰胺化合物：其中X、R1、R2、R3、R4、R5、R6、Ra和Rb如本文所述和定义的那样，制备所述化合物的方法，用于制备所述化合物的有用中间体化合物，包含所述化合物的药物组合物和组合物，以及利用所述化合物制造用于治疗或预防疾病的药物组合物，特别是治疗或预防过度增殖性疾病的药物组合物，作为唯一药剂或与其他活性成分结合使用，以及治疗和/或预防疾病的方法，特别是癌症，更特别是KAT6A和/或KAT6B在局部扩增的癌症，所述方法包括向需要的受试者施用至少一种式(I)化合物的有效量。

  公开号：

  WO2020216701A1

文献信息

• [EN] SUBSTITUTED ACYL SULFONAMIDES FOR TREATING CANCER<br/>[FR] ACYLSULFONAMIDES SUBSTITUÉS POUR LE TRAITEMENT DU CANCER
  申请人：BROAD INST INC

  公开号：WO2022081842A1

  公开（公告）日：2022-04-21

  The present invention provides acyl sulfonamide compounds of general formula (I): (I) in which R1, R2, R3, R4, R5 and R6 are as described and defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds, and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative disorders, as a sole agent or in combination with other active ingredients as well as methods of treatment and/or prophylaxis of diseases, particularly cancer, more particularly cancer in which KAT6A and/or KAT6B is focally amplified, said method comprising administering an effective amount of at least one compound of formula (I) to a subject in need thereof.

  本发明提供了一般式(I)的酰基磺酰胺化合物：(I)其中R1、R2、R3、R4、R5和R6如本文所述和定义的，制备所述化合物的方法，用于制备所述化合物的有用中间体化合物，包含所述化合物的药物组合物和配方，以及利用所述化合物制造用于治疗或预防疾病的药物组合物，特别是用作唯一药剂或与其他活性成分结合的方法，以及治疗和/或预防疾病的方法，特别是癌症，更具体地说是KAT6A和/或KAT6B局部扩增的癌症，所述方法包括向需要的受试者投与至少一种式(I)化合物的有效剂量。
• ACYL SULFONAMIDES FOR TREATING CANCER
  申请人：Bayer Aktiengesellschaft

  公开号：US20220226279A1

  公开（公告）日：2022-07-21

  The present invention provides acyl sulfonamide compounds of general formula (I): in which X, R 1 , R 2 , R 3 , R 4 , R 5 , R 6′ R a and R b are as described and defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds, and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative disorders, as a sole agent or in combination with other active ingredients as well as methods of treating and/or prophylaxing diseases, particularly cancer, more particularly cancer in which KAT6A and/or KAT6B is focally amplified, said method comprising administering an effective amount of at least one compound of formula (I) to a subject in need thereof.