2-[4-(dimethylsulfamoyl)piperazin-1-yl]-N-hydroxypyrimidine-5-carboxamide | 603991-92-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 英文名称: 2-[4-(dimethylsulfamoyl)piperazin-1-yl]-N-hydroxypyrimidine-5-carboxamide
• CAS: 603991-92-0
• 化学式: C₁₁H₁₈N₆O₄S
• 分子量: 330.368
• InChiKey: MYNPXCWMJRITGC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.6
• 重原子数：
  22
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.55
• 拓扑面积：
  127
• 氢给体数：
  2
• 氢受体数：
  9

反应信息

• 作为产物：
  描述：

  2-甲砜基-5-嘧啶甲酸乙酯 在 palladium 10% on activated carbon 、 氢气 、 potassium carbonate 、 1-羟基苯并三唑 、 盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺 、 三乙胺 、 三氟乙酸 、 sodium hydroxide 作用下， 以 四氢呋喃 、 甲醇 、 乙醇 、 二氯甲烷 、 乙腈 为溶剂， 反应 206.75h， 生成 2-[4-(dimethylsulfamoyl)piperazin-1-yl]-N-hydroxypyrimidine-5-carboxamide
  参考文献：
  名称：

  Inhibitors of histone deacetylase

  摘要：

  这项发明包括具有组合式(I)的新化合物，其中n、R1、R2、R3、R4、Q、X、Y、Z具有定义的含义，具有组蛋白去乙酰化酶抑制酶活性；它们的制备、含有它们的组合物以及它们作为药物的用途。

  公开号：

  US09150560B2

文献信息

• Inhibitors of Histone Deacetylase
  申请人：Moradei Oscar

  公开号：US20080132459A1

  公开（公告）日：2008-06-05

  The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.

  本发明涉及抑制组蛋白去乙酰化酶的方法。本发明提供了抑制组蛋白去乙酰化酶酶活性的化合物和方法。本发明还提供了用于治疗细胞增殖性疾病和病状的组合物和方法。
• INHIBITORS OF HISTONE DEACETYLASE
  申请人：VAN EMELEN Kristof

  公开号：US20100010004A1

  公开（公告）日：2010-01-14

  This invention comprises the novel compounds of formula (I) wherein n, R 1 , R 2 , R 3 , R 4 , Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.
• Inhibitors Of Histone Deacetylase
  申请人：JANSSEN PHARMACEUTICA, N.V.

  公开号：US20130245034A1

  公开（公告）日：2013-09-19

  This invention comprises the novel compounds of formula (I) wherein n, R 1 , R 2 , R 3 , R 4 , Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.
• COMPOUNDS AND METHODS FOR IMPROVING IMPAIRED ENDOGENOUS FIBRINOLYSIS USING HISTONE DEACETYLASE INHIBITORS
  申请人：Larsson Pia

  公开号：US20140051716A1

  公开（公告）日：2014-02-20

  There is provided a compound which is a histone deacetylase (HDAC) inhibitor, or a pharmaceutically acceptable ester, amide, solvate or salt thereof, for use in: (I) treating or preventing a pathological condition associated with excess fibrin deposition and/or thrombus formation; and/or (II) potentiating the degradation of fibrin deposits and preventing such deposits associated with pathological conditions or which may lead to such conditions, wherein the HDAC inhibitor, and the dose thereof, is as described in the description. There is also provided valproic acid, or a pharmaceutically acceptable salt thereof, for use in improving or normalizing endogenous fibrinolysis impaired by local or systemic inflammation.
• US7615553B2
  申请人：——

  公开号：US7615553B2

  公开（公告）日：2009-11-10