4-[({[4-(1H-pyrazol-1-yl)phenyl]sulfonyl}amino)methyl]-N-(3-pyridinyl)benzamide | 1262990-41-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 4-[({[4-(1H-pyrazol-1-yl)phenyl]sulfonyl}amino)methyl]-N-(3-pyridinyl)benzamide
• 英文别名: 4-[[(4-pyrazol-1-ylphenyl)sulfonylamino]methyl]-N-pyridin-3-ylbenzamide
• CAS: 1262990-41-9
• 化学式: C₂₂H₁₉N₅O₃S
• 分子量: 433.491
• InChiKey: FXDAFTAUAILJQH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.1
• 重原子数：
  31
• 可旋转键数：
  7
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.05
• 拓扑面积：
  114
• 氢给体数：
  2
• 氢受体数：
  6

文献信息

• [EN] HETEROARYL BENZAMIDES, COMPOSITIONS AND METHODS OF USE<br/>[FR] HÉTÉROARYL BENZAMIDES, COMPOSITIONS ET PROCÉDÉS D'UTILISATION
  申请人：UNIV LELAND STANFORD JUNIOR

  公开号：WO2011011514A1

  公开（公告）日：2011-01-27

  Provided are certain heteroaryl benzamides, compositions, and methods of their manufacture and use.

  提供了某些杂环芳酰苯胺、组合物及其制备和使用方法。
• COMPOSITIONS AND METHODS USEFUL FOR TREATING DISEASES
  申请人：Cardone Michael H.

  公开号：US20120225851A1

  公开（公告）日：2012-09-06

  The present invention relates to a chemotherapeutic cancer treatment in which compounds of Formula Ia′, Ib′, Ic′, or II′ (referred to as a group as BH3Is) are administered to a mammal for the treatment of B-cell Lymphoma or other hematopoietic cancers, including diseases associated with MCL-1. In another aspect, the invention provides a method for treating particular types of hematopoietic cancers, such as B-cell lymphoma, using a combination of one or more compounds selected from the group consisting of compounds or Formula Ia, Ib, Ic, or II in combination with other therapies, for example, a class of therapeutics known as 26S proteosome inhibitors, such as, for example, Bortezomib. In another aspect the present invention relates to autoimmune treatment with pharmaceutical compositions comprising one or more compounds of Formula Ia′, Ib′, Ic′, or II′. In another aspect, this invention relates to methods for identifying compounds, for example, compounds of the BH3 mimic class, that have unique in vitro properties that predict in vivo efficacy against B-cell lymphoma tumors and other cancers as well as autoimmune disease.

  本发明涉及一种化疗癌症的治疗方法，其中将Ia'、Ib'、Ic'或II'的化合物（作为一组称为 Is）用于治疗哺乳动物的B细胞淋巴瘤或其他造血系统癌症，包括与MCL-1相关的疾病。在另一方面，本发明提供了一种治疗特定类型的造血系统癌症，例如B细胞淋巴瘤的方法，使用从由Ia、Ib、Ic或II的化合物中选择的一种或多种化合物与其他治疗方法，例如一类被称为26S蛋白酶体抑制剂的治疗剂的组合，例如Bortezomib。在另一方面，本发明涉及使用包括Ia'、Ib'、Ic'或II'的一种或多种化合物的药物组合物进行自身免疫治疗。在另一方面，本发明涉及识别化合物的方法，例如BH3类似物类的化合物，具有预测体内对B细胞淋巴瘤肿瘤和其他癌症以及自身免疫疾病的疗效的独特的体外特性。
• HETEROARYL BENZAMIDES, COMPOSITIONS AND METHODS OF USE
  申请人：Sutphin Patrick D.

  公开号：US20120225862A1

  公开（公告）日：2012-09-06

  Provided are certain heteroaryl benzamides, compositions, and methods of their manufacture and use.

  提供了某些杂环芳酰苯胺、组成物及其制造和使用方法。
• 2,2'-BIPHENAZINE COMPOUNDS AND METHODS USEFUL FOR TREATING DISEASES
  申请人：Eutropics Pharmaceuticals, Inc.

  公开号：US20150216862A1

  公开（公告）日：2015-08-06

  The invention relates to a chemotherapeutic cancer treatment in which compounds (BH3Is) are administered to a mammal to treat B-cell Lymphoma or other hematopoietic cancers, including diseases associated with MCL-1. The invention also provides a method for treating types of hematopoietic cancers, such as B-cell lymphoma, using a combination of one or more disclosed compounds in combination with other therapes, for example, 26S proteasome inhibitors, such as, for example, Bortezomib. The invention also relates to autoimmune treatment with pharmaceutical compositions comprising one or more disclosed compounds. The invention also relates to methods for identifying compounds, for example, compounds of the BH3 mimic class, that have unique in vitro properties that predict in vivo efficacy against B-cell lymphoma tumors and other cancers as well as autoimmune disease. Illustrative compounds are those of Formula II:

  本发明涉及一种化疗癌症的治疗方法，其中将化合物（ Is）用于治疗哺乳动物的B细胞淋巴瘤或其他造血系统癌症，包括与MCL-1相关的疾病。本发明还提供了一种治疗造血系统癌症（如B细胞淋巴瘤）的方法，该方法使用一个或多个披露的化合物与其他治疗方法（例如26S蛋白酶抑制剂，例如博来佐米布）的组合。本发明还涉及使用含有一个或多个披露的化合物的制药组合物进行自身免疫治疗。本发明还涉及识别化合物的方法，例如BH3类似物类的化合物，这些化合物具有预测体内对B细胞淋巴瘤肿瘤和其他癌症以及自身免疫疾病有效性的独特体外性质。其中一些示例化合物为II式：
• SYNTHETIC LETHAL TARGETING OF GLUCOSE TRANSPORT
  申请人：Irwin John

  公开号：US20140128397A1

  公开（公告）日：2014-05-08

  The present invention provides methods for inhibiting growth and proliferation of HIF pathway proficient cells by administering GLUT1 inhibitors of the invention to HIF pathway proficient cells.