4-oxiranylmethoxy-benzamide | 28763-58-8

• 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: 4-oxiranylmethoxy-benzamide
• 英文别名: 1-(4-aminocarbonyl)phenoxy-2,3-epoxy-propane；4-(2,3-epoxypropoxy)benzamide；4-(oxiran-2-ylmethoxy)benzamide
• CAS: 28763-58-8
• 化学式: C₁₀H₁₁NO₃
• 分子量: 193.202
• InChiKey: KQGBLRILCYSUFE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.6
• 重原子数：
  14
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  64.8
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  4-oxiranylmethoxy-benzamide 在 盐酸 作用下， 以 1,4-二氧六环 、 甲醇 、 DMF (N,N-dimethyl-formamide) 为溶剂， 反应 51.0h， 生成 4-[2-hydroxy-3-(piperidin-4-ylamino)-propoxy]-benzamide hydrogen chloride
  参考文献：
  名称：

  [EN] SUBSTITUTED 3-AMINO-THIENO[2,3-b]PYRIDINE-2-CARBOXYLIC ACID AMIDE COMPOUNDS AND PROCESSES FOR PREPARING AND THEIR USES
  [FR] COMPOSES AMIDE D'ACIDE 3-AMINO-THIENO[2,3-b]PYRIDINE-2-CARBOXYLIQUE SUBSTITUES ET PROCESSUS DE PREPARATION ET D'UTILISATION DE CES COMPOSES

  摘要：

  公开的是式(I)的化合物，其中R1和R2如本文所定义，这些化合物可用作IκB激酶（IKK）复合物激酶活性的抑制剂。因此，这些化合物在治疗IKK介导的疾病，包括自身免疫疾病、炎症性疾病和癌症方面是有用的。还公开了包含这些化合物的药物组合物以及制备这些化合物的方法。

  公开号：

  WO2003103661A1
• 作为产物：
  描述：

  4-羟基苯甲酰胺 生成 4-oxiranylmethoxy-benzamide
  参考文献：
  名称：

  New 8-substituted nucleoside and purine derivatives, the process for the

  摘要：

  新的8-取代核苷和嘌呤衍生物的一般公式为：##STR1##其中R代表氨基团或羟基团，可能以相应的酮式互变形式存在，R.sub.1是氢或氨基团，R.sub.2是氢或一个β-D-核糖呋喃基团，其中主要羟基和/或两个次要羟基可以被衍生，R.sub.3是一个可选择取代的芳基或单环杂芳基团，X是--O--或--S--。这些新化合物具有抗高脂血症活性。

  公开号：

  US04774325A1

文献信息

• Substituted 3-amino-thieno[2,3-b]pyridine-2-carboxylic acid amide compounds and processes for preparing and their uses
  申请人：Cywin L. Charles

  公开号：US20050288285A1

  公开（公告）日：2005-12-29

  Disclosed are compounds of formula (I): wherein R 1 and R 2 are defined herein, which are useful as inhibitors of the kinase activity of the IκB kinase (IKK) complex. The compounds are therefore useful in the treatment of IKK mediated diseases including autoimmune diseases inflammatory diseases and cancer. Also disclosed are pharmaceutical compositions comprising these compounds and processes for preparing these compounds.

  本发明涉及化合物(I)的公开，其中R1和R2在此定义，这些化合物可用作IκB激酶（IKK）复合物的激酶活性抑制剂。因此，这些化合物可用于治疗由IKK介导的疾病，包括自身免疫性疾病、炎症性疾病和癌症。还公开了包含这些化合物的药物组合物和制备这些化合物的过程。
• Substituted 3-amino-thieno [2,3-b]pyridine-2-carboxylic acid amide compounds and processes for preparing and their uses
  申请人：Boehringer Ingelheim Pharmaceuticals, Inc.

  公开号：US20040053957A1

  公开（公告）日：2004-03-18

  Disclosed are compounds of formula (I): 1 wherein R 1 and R 2 are defined herein, which are useful as inhibitors of the kinase activity of the I&kgr;B kinase (IKK) complex. The compounds are therefore useful in the treatment of IKK mediated diseases including autoimmune diseases inflammatory diseases and cancer. Also disclosed are pharmaceutical compositions comprising these compounds and processes for preparing these compounds.

  本发明公开了式(I)的化合物：其中R1和R2在此定义，这些化合物可用作IκB激酶（IKK）复合物的激酶活性抑制剂。因此，这些化合物可用于治疗IKK介导的疾病，包括自身免疫性疾病、炎症性疾病和癌症。本发明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过程。
• 3-amino-thieno[2,3-b]pyridine-2-carboxylic acid amides
  申请人：Boehringer Ingelheim Pharmaceuticals, Inc.

  公开号：EP2008654A1

  公开（公告）日：2008-12-31

  Disclosed are compounds of formula (I): wherein R1 and R2 are defined herein, which are useful as inhibitors of the kinase activity of the IκB kinase (IKK) complex. The compounds are therefore useful in the treatment of IKK mediated diseases including autoimmune diseases inflammatory diseases and cancer. Also disclosed are pharmaceutical compositions comprising these compounds and processes for preparing these compounds.

  所公开的是式 (I) 化合物： 其中 R1 和 R2 在此定义，可用作 IκB 激酶（IKK）复合物激酶活性的抑制剂。因此，这些化合物可用于治疗 IKK 介导的疾病，包括自身免疫性疾病、炎症性疾病和癌症。此外，还公开了包含这些化合物的药物组合物以及制备这些化合物的工艺。
• 8-Substituted purine derivatives: a new class of lipid-lowering agents
  作者：E Vanotti、M Bani、D Favara、M Gobetti、M Lombroso、S Magnetti、V Olgiati、M Palladino、GC Tonon

  DOI：10.1016/0223-5234(94)90098-1

  日期：1994.1

  A series of purine derivatives have been prepared and their in vivo abilities to lower plasma total cholesterol and triglyceride levels, and to elevate high density lipoprotein (HDL) cholesterol levels in hyperlipemic rats have been tested. Some compounds, among which 8-2-(R)-hydroxy-3-[(p-isobutoxycarbonyl)phenoxy]propylthio}adenosine 31, 8-3-[(p-isobutoxy carbonyl)phenoxy]-2-oxopropylthio} adenosine 33 and 8-3-[(p-isobutoxycarbonyl)phenoxy]-2-hydrazonecarboxamidepropylthio} adenosine 36 appear to be the most interesting, have been found to have both the desired profile of activity and no hepatotoxicity, when administered po at 50, 100 or 300 mg/kg. Compounds 31, 33 and 36, orally tested at the same doses in the 15-d test, lower triglyceride and VLDL/LDL (very low density lipoprotein/low density lipoprotein) cholesterol levels by 10-33% and 13-46%, respectively, and increase HDL-associated cholesterol levels by 10-32%. These molecules have been chosen for further pharmacological and toxicological evaluations.
• New 8-substituted nucleoside and purine derivatives, the process for the preparation thereof and the pharmaceutical compositions containing them
  申请人：Pierrel S.p.A.

  公开号：EP0175325B1

  公开（公告）日：1989-03-15