N-(cyclopropylmethyl)-N'-hydroxynaphthalene-2,6-dicarboxamide | 1141942-36-0

• 分子结构分类: 有机化合物 - 苯类化合物 - 萘
• 英文名称: N-(cyclopropylmethyl)-N'-hydroxynaphthalene-2,6-dicarboxamide
• 英文别名: 6-N-(cyclopropylmethyl)-2-N-hydroxynaphthalene-2,6-dicarboxamide
• CAS: 1141942-36-0
• 化学式: C₁₆H₁₆N₂O₃
• 分子量: 284.315
• InChiKey: XNLDKTXJHNWUBR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2
• 重原子数：
  21
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  78.4
• 氢给体数：
  3
• 氢受体数：
  3

文献信息

• [EN] N-HYDROXY-NAPHTHALENE DICARBOXAMIDE AND N-HYDROXY-BIPHENYL-DICARBOXAMIDE COMPOUNDS AS HISTONE DEACETYLASE INHIBITORS<br/>[FR] COMPOSÉS N-HYDROXY-NAPHTALÈNE DICARBOXAMIDE ET N-HYDROXY-BIPHÉNYL-DICARBOXAMIDE COMME INHIBITEURS DE L'HISTONE DÉSACÉTYLASE
  申请人：MERCK & CO INC

  公开号：WO2009045385A1

  公开（公告）日：2009-04-09

  The present invention relates to a novel class of N-hydroxy-naphthalene dicarboxamide and N-hydroxy-biphenyl-dicarboxamide derivatives. The N-hydroxy-naphthalene dicarboxamide and N-hydroxy-biphenyl-dicarboxamide compounds can be used to treat cancer. The N-hydroxy-naphthalene dicarboxamide and N-hydroxy-biphenyl-dicarboxamide compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the N-hydroxy-naphthalene dicarboxamide and N-hydroxy-biphenyl-dicarboxamide derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the N-hydroxy-naphthalene dicarboxamide and N-hydroxy-biphenyl-dicarboxamide derivatives in vivo.

  本发明涉及一类新型的N-羟基-萘二甲酰胺和N-羟基联苯二甲酰胺衍生物。N-羟基-萘二甲酰胺和N-羟基联苯二甲酰胺化合物可用于治疗癌症。N-羟基-萘二甲酰胺和N-羟基联苯二甲酰胺化合物还可以抑制组蛋白去乙酰化酶，并适用于选择性诱导末端分化、阻止肿瘤细胞生长和/或凋亡，从而抑制这些细胞的增殖。因此，本发明的化合物可用于治疗具有肿瘤细胞增殖特征的患者。本发明的化合物也可用于预防和治疗TRX介导的疾病，如自身免疫、过敏和炎症性疾病，以及中枢神经系统（CNS）疾病的预防和/或治疗，如神经退行性疾病。本发明还提供包含N-羟基-萘二甲酰胺和N-羟基联苯二甲酰胺衍生物的制药组合物和这些制药组合物的安全用量方案，易于遵循，并在体内产生治疗有效量的N-羟基-萘二甲酰胺和N-羟基联苯二甲酰胺衍生物。
• N-HYDROXY-NAPHTHALENE DICARBOXAMIDE AND N-HYDROXY-BIPHENYL-DICARBOXAMIDE COMPOUNDS AS HISTONE DEACETYLASE INHIBITORS
  申请人：Kattar Solomon

  公开号：US20100216796A1

  公开（公告）日：2010-08-26

  The present invention relates to a novel class of N-hydroxy-naphthalene dicarboxamide and N-hydroxy-biphenyl-dicarboxamide derivatives. The N-hydroxy-naphthalene dicarboxamide and N-hydroxy-biphenyl-dicarboxamide compounds can be used to treat cancer. The N-hydroxy-naphthalene dicarboxamide and N-hydroxy-biphenyl-dicarboxamide compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the N-hydroxy-naphthalene dicarboxamide and N-hydroxy-biphenyl-dicarboxamide derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the N-hydroxy-naphthalene dicarboxamide and N-hydroxy-biphenyl-dicarboxamide derivatives in vivo.

  本发明涉及一种新的N-羟基萘二甲酰胺和N-羟基联苯二甲酰胺衍生物。N-羟基萘二甲酰胺和N-羟基联苯二甲酰胺化合物可用于治疗癌症。N-羟基萘二甲酰胺和N-羟基联苯二甲酰胺化合物还可抑制组蛋白去乙酰化酶，并适用于选择性诱导末端分化，抑制肿瘤细胞的增殖和/或凋亡，从而抑制这些细胞的增殖。因此，本发明的化合物适用于治疗具有肿瘤细胞增殖特征的患者。本发明的化合物也可用于预防和治疗TRX介导的疾病，如自身免疫、过敏和炎症性疾病，以及中枢神经系统（CNS）疾病的预防和/或治疗，如神经退行性疾病。本发明还提供了包含N-羟基萘二甲酰胺和N-羟基联苯二甲酰胺衍生物的药物组合物和这些药物组合物的安全给药方案，易于遵循，并在体内产生治疗有效量的N-羟基萘二甲酰胺和N-羟基联苯二甲酰胺衍生物。