methyl 4-[methoxy(phenyl)phosphoryl]benzoate | 1003313-68-5

• 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: methyl 4-[methoxy(phenyl)phosphoryl]benzoate
• CAS: 1003313-68-5
• 化学式: C₁₅H₁₅O₄P
• 分子量: 290.255
• InChiKey: ZSZTXXXGKPGZCM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  20
• 可旋转键数：
  5
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.13
• 拓扑面积：
  52.6
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  methyl 4-[methoxy(phenyl)phosphoryl]benzoate 在 lithium hydroxide 、 水 作用下， 以 四氢呋喃 、 甲醇 为溶剂， 生成 4-[甲氧基(苯基)磷酰基]苯甲酸
  参考文献：
  名称：

  Exploring the pharmacokinetic properties of phosphorus-containing selective HDAC 1 and 2 inhibitors (SHI-1:2)

  摘要：

  We report the preparation and structure-activity relationships of phosphorus-containing histone deacetylase inhibitors. A strong trend between decreasing phosphorus functional group size and superior mouse pharmacokinetic properties was identified. In addition, optimized candidates showed tumor growth inhibition in xenograft studies. (C) 2009 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2009.02.009
• 作为产物：
  描述：

  对溴苯甲酸甲酯 、 hydrogen methyl phenylphosphonate 在 nickel dibromide 作用下， 生成 methyl 4-[methoxy(phenyl)phosphoryl]benzoate
  参考文献：
  名称：

  Exploring the pharmacokinetic properties of phosphorus-containing selective HDAC 1 and 2 inhibitors (SHI-1:2)

  摘要：

  We report the preparation and structure-activity relationships of phosphorus-containing histone deacetylase inhibitors. A strong trend between decreasing phosphorus functional group size and superior mouse pharmacokinetic properties was identified. In addition, optimized candidates showed tumor growth inhibition in xenograft studies. (C) 2009 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2009.02.009

文献信息

• PHOSPHORUS DERIVATIVES AS HISTONE DEACETYLASE INHIBITORS
  申请人：Close Joshua

  公开号：US20090270351A1

  公开（公告）日：2009-10-29

  The present invention relates to a novel class of phosphorus derivatives. The phosphorus compounds can be used to treat cancer. The phosphorus 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 phosphorus derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the phosphorus derivatives in vivo.

  本发明涉及一种新型的磷衍生物。这些磷化合物可以用于治疗癌症。这些磷化合物还可以抑制组蛋白去乙酰化酶，适用于选择性诱导终末分化，并阻止肿瘤细胞的生长和/或凋亡，从而抑制这些细胞的增殖。因此，本发明的化合物对于治疗具有肿瘤细胞增殖特征的患者非常有用。本发明的化合物还可以用于预防和治疗TRX介导的疾病，例如自身免疫、过敏和炎症性疾病，以及预防和/或治疗中枢神经系统（CNS）疾病，例如神经退行性疾病。本发明还提供了包含这些磷衍生物的药物组合物和这些药物组合物的安全剂量方案，这些方案易于遵循，并在体内产生治疗有效量的磷衍生物。
• Phosphorus derivatives as histone deacetylase inhibitors
  申请人：Merck Sharp & Dohme Corp.

  公开号：US07981874B2

  公开（公告）日：2011-07-19

  The present invention relates to a novel class of phosphorus derivatives. The phosphorus compounds can be used to treat cancer. The phosphorus 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 phosphorus derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the phosphorus derivatives in vivo.

  本发明涉及一类新型的磷衍生物。这些磷化合物可用于治疗癌症。这些磷化合物还可以抑制组蛋白去乙酰化酶，适用于选择性诱导末端分化，阻止肿瘤细胞的生长和/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。本发明的化合物还可以用于预防和治疗TRX介导的疾病，如自身免疫性、过敏性和炎症性疾病，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这些磷衍生物的药物组合物和这些药物组合物的安全剂量方案，易于遵循，并且在体内产生治疗有效量的磷衍生物。
• POLYMERIZATION CATALYST FOR POLYESTER PRODUCTION, POLYESTER, AND PROCESS FOR PRODUCING POLYESTER
  申请人：Toyo Boseki Kabushiki Kaisha

  公开号：EP1153953A1

  公开（公告）日：2001-11-14

  A polyester polymerization catalyst consisting mainly of components except for antimony compounds or germanium compounds which exhibits an excellent catalyst activity and yields a highly thermally stable polyester whose thermal degradation upon a melt process is suppressed efficiently without any need of an inactivation or a removal of the catalyst, a polyester obtained using said polyester polymerization catalyst, and a method for producing a polyester using said polyester polymerization catalyst are provided. A polyester polymerization catalyst is one which contains no antimony or germanium, whose activity parameter (AP) fulfills the relationship: AP(min)<2T (min), which gives, when used in a polymerization, a thermal stability degree (TD) of a resultant polyethylene terephthalate fulfilling the requirement: TD (%)<25, and which comprises a metal-containing component and an organic compound component having an Ar-O- and/or an Ar-N< unit. A polyester can be used in various molded articles such as a fiber, a film, a sheet and a hollow article.

  本发明提供了一种主要由锑化合物或锗化合物以外的组分组成的聚酯聚合催化剂，该催化剂具有优异的催化剂活性，并能产生热稳定性极高的聚酯，其在熔融过程中的热降解被有效地抑制，而无需对催化剂进行失活或移除处理；还提供了一种使用所述聚酯聚合催化剂获得的聚酯，以及一种使用所述聚酯聚合催化剂生产聚酯的方法。聚酯聚合催化剂是不含锑或锗的催化剂，其活性参数（AP）符合以下关系：AP(min)<2T(min)，当用于聚合时，生成的聚对苯二甲酸乙二酯的热稳定性度(TD)符合要求：TD(%)<25，它由含金属成分和具有 Ar-O- 和/或 Ar-N< 单元的有机化合物成分组成。聚酯可用于各种成型制品，如纤维、薄膜、片材和中空制品。
• WO2008/10985
  申请人：——

  公开号：——

  公开（公告）日：——
• PROCESSING AGENT FOR POLYESTER FIBER STRUCTURE AND PRODUCTION METHOD FOR POLYESTER FIBER STRUCTURE USING SAME
  申请人：Toray Industries, Inc.

  公开号：EP2653605B1

  公开（公告）日：2018-12-05