3,4-二甲基-10-(3-氨基丙基)-9-吖啶酮草酸盐 | 201010-95-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 中文名称: 3,4-二甲基-10-(3-氨基丙基)-9-吖啶酮草酸盐
• 英文名称: ER-27319
• 英文别名: 3,4-Dimethyl-10-(3-aminopropyl)-9-acridone oxalate；9(10H)-Acridinone, 10-(3-aminopropyl)-3,4-dimethyl-, ethanedioate (1:1)；10-(3-aminopropyl)-3,4-dimethylacridin-9-one;oxalic acid
• CAS: 201010-95-9
• 化学式: C₂H₂O₄*C₁₈H₂₀N₂O
• 分子量: 370.405
• InChiKey: IIELZHYJYZBSGG-UHFFFAOYSA-N

物化性质

• 熔点：
  135 - 137°C
• 溶解度：
  在DMSO中的溶解度为28 毫克/毫升

计算性质

• 辛醇/水分配系数(LogP)：
  2.28
• 重原子数：
  27
• 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：
  121
• 氢给体数：
  3
• 氢受体数：
  7

制备方法与用途

ER-27319是一种吖啶酮衍生物，是一种强效且选择性的SYK抑制剂，能够抑制SYK的酪氨酸磷酸化及其活性。研究表明，ER-27319在浓度为10μM时，可有效抑制人类和大鼠肥大细胞中抗原诱导的过敏介质释放，因此它在过敏性疾病的研究中具有潜在应用价值。

文献信息

• 1,6 Naphthyridines useful as inhibitors of SYK kinase
  申请人：Boehringer Ingelheim Pharmaceuticals, Inc.

  公开号：US20030229090A1

  公开（公告）日：2003-12-11

  Disclosed are compounds of formula (I): 1 wherein R 3 , R 5 , R 7 and R 8 are defined herein, which are useful as inhibitors SYK kinase and are thus useful for treating diseases resulting from inappropriate mast cell activation, which include allergic and inflammatory diseases. Also disclosed are pharmaceutical compositions comprising these compounds and processes for preparing these compounds.

  公开了式(I)的化合物：其中R3、R5、R7和R8如此定义，它们有用作SYK激酶抑制剂，并因此有用于治疗由不适当的肥大细胞活化引起的疾病，包括过敏和炎症性疾病。还公开了包含这些化合物的制药组合物和制备这些化合物的方法。
• 1,6 NAPHTHYRIDINES USEFUL AS INHIBITORS OF SYK KINASE
  申请人：CYWIN L. Charles

  公开号：US20080114024A1

  公开（公告）日：2008-05-15

  Disclosed are compounds of formula (I): wherein R 3 , R 5 , R 7 and R 8 are defined herein, which are useful as inhibitors SYK kinase and are thus useful for treating diseases resulting from inappropriate mast cell activation, which include allergic and inflammatory diseases. Also disclosed are pharmaceutical compositions comprising these compounds and processes for preparing these compounds.

  本发明涉及式(I)的化合物：其中R3、R5、R7和R8如本文所定义，其可用作抑制SYK激酶的抑制剂，因此可用于治疗由不恰当的肥大细胞激活引起的疾病，包括过敏和炎症性疾病。本发明还涉及包含这些化合物的制药组合物和制备这些化合物的方法。
• QUINOLINE DERIVATIVES FOR MODULATING DNA METHYLATION
  申请人：Phiasivongsa Pasit

  公开号：US20090285772A1

  公开（公告）日：2009-11-19

  Quinoline derivatives, particularly 4-anilinoquinoline derivatives, are provided. Such quinoline derivatives can be used for modulation of DNA methylation, such as effective inhibition of methylation of cytosine at the C-5 position, for example via selective inhibition of DNA methyltransferase DNMT1. Methods for synthesizing numerous 4-anilinoquinoline derivatives and for modulating DNA methylation are provided. Also provided are methods for formulating and administering these compounds or compositions to treat conditions such as cancer and hematological disorders.

  提供了喹啉衍生物，特别是4-苯胺基喹啉衍生物。这样的喹啉衍生物可用于调节DNA甲基化，例如通过选择性抑制DNA甲基转移酶DNMT1，有效抑制C-5位置的胞嘧啶甲基化。提供了合成多种4-苯胺基喹啉衍生物和调节DNA甲基化的方法。还提供了制剂和给药这些化合物或组合物以治疗癌症和血液疾病的方法。
• 1,6 NAPHTHRIDINES USEFUL AS INHIBITORS OF SYK KINASE
  申请人：CYWIN Charles L.

  公开号：US20090171089A1

  公开（公告）日：2009-07-02

  Disclosed are compounds of formula (I): wherein R 3 , R 5 , R 7 and R 8 are defined herein, which are useful as inhibitors SYK kinase and are thus useful for treating diseases resulting from inappropriate mast cell activation, which include allergic and inflammatory diseases. Also disclosed are pharmaceutical compositions comprising these compounds and processes for preparing these compounds.

  本发明涉及一种化合物，其化学式为（I）：其中R3，R5，R7和R8如本文所定义，这些化合物可用作SYK激酶抑制剂，因此可用于治疗由不适当的肥大细胞激活引起的疾病，包括过敏性和炎症性疾病。本发明还涉及包含这些化合物的制药组合物以及制备这些化合物的过程。
• ACRIDONE DERIVATIVE
  申请人：Eisai Co., Ltd.

  公开号：EP0877020A1

  公开（公告）日：1998-11-11

  An acridone derivative represented by the following formula (I) and a pharmacologically acceptable salt thereof are effective in preventing and curing diseases which are associable with histamine, leucotriene, etc. and in preventing and curing allergic diseases such as asthma, allergic rhinitis, atopic dermatitis, urticaria, valerian fever, digestive tract allergy, or food allergy. wherein R1 - R8 severally represent a hydrogen atom, a lower alkyl group, etc. and n represents an integer of 1 - 6.

  下式(I)代表的吖啶酮衍生物及其药理上可接受的盐可有效预防和治疗与组胺、白三烯等有关的疾病，以及预防和治疗过敏性疾病，如哮喘、过敏性鼻炎、特应性皮炎、荨麻疹、缬草热、消化道过敏或食物过敏。 其中 R1 - R8 分别代表氢原子、低级烷基等，n 代表 1 - 6 的整数。