2-bromo-N-(2-hydroxyphenyl)-2-methylpropanamide | 129339-29-3

• 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: 2-bromo-N-(2-hydroxyphenyl)-2-methylpropanamide
• 英文别名: 2-bromo-N-(2-hydroxyphenyl)-2-methylpropionamide
• CAS: 129339-29-3
• 化学式: C₁₀H₁₂BrNO₂
• 分子量: 258.115
• InChiKey: YKFWWTRUDVYUKO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.1
• 重原子数：
  14
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  49.3
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  2-bromo-N-(2-hydroxyphenyl)-2-methylpropanamide 在 potassium carbonate 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 3.0h， 生成 2,2-二甲基-2H-1,4-苯并恶唑-3(4H)-酮
  参考文献：
  名称：

  新的1，4-苯并恶嗪衍生物钾通道开放剂的合成及其血管舒张活性。

  摘要：

  作为寻找新的钾通道开放剂的一部分，描述了衍生自克罗马卡林的苯并吡喃骨架的新的1,4-苯并恶嗪衍生物的合成和血管舒张活性。几种新的1,4-苯并恶嗪衍生物具有明显的血管舒张活性，其总体药理行为类似于CRK（1f，1i，2d，2e，2f和2i）。

  DOI：

  10.1016/s0968-0896(02)00091-3
• 作为产物：
  描述：

  2-溴-2-甲基丙酰溴 、 2-氨基苯酚 在 sodium carbonate 作用下， 以 氯仿 为溶剂， 反应 3.0h， 生成 2-bromo-N-(2-hydroxyphenyl)-2-methylpropanamide
  参考文献：
  名称：

  新的1，4-苯并恶嗪衍生物钾通道开放剂的合成及其血管舒张活性。

  摘要：

  作为寻找新的钾通道开放剂的一部分，描述了衍生自克罗马卡林的苯并吡喃骨架的新的1,4-苯并恶嗪衍生物的合成和血管舒张活性。几种新的1,4-苯并恶嗪衍生物具有明显的血管舒张活性，其总体药理行为类似于CRK（1f，1i，2d，2e，2f和2i）。

  DOI：

  10.1016/s0968-0896(02)00091-3

文献信息

• NEW PHENYLAZETIDINECARBOXYLATE OR -CARBOXAMIDE COMPOUNDS
  申请人：INVENTIVA

  公开号：US20170066717A1

  公开（公告）日：2017-03-09

  The invention relates to compounds of formula (I). where R, R 1 , R 2 , n, A and Cy have the meanings indicated in the description. The compounds of formula (I) are Nurr-1 modulators.

  这项发明涉及式(I)的化合物。 其中R、R1、R2、n、A和Cy的含义如描述中所示。 式(I)的化合物是Nurr-1调节剂。
• CYCLIC AMIDE DERIVATIVES AS INHIBITORS OF 11 - BETA - HYDROXYSTEROID DEHYDROGENASE AND USES THEREOF
  申请人：CONNEXIOS LIFE SCIENCES PVT. LTD.

  公开号：US20150158860A1

  公开（公告）日：2015-06-11

  The present invention relates to certain amide derivatives that have the ability to inhibit 11-β-hydroxysteroid dehydrogenase type 1 (11β-HSD-1) and which are therefore useful in the treatment of certain disorders that can be prevented or treated by inhibition of this enzyme. In addition the invention relates to the compounds, methods for their preparation, pharmaceutical compositions containing the compounds and the uses of these compounds in the treatment of certain disorders. It is expected that the compounds of the invention will find application in the treatment of conditions such as non-insulin dependent type 2 diabetes mellitus (NIDDM), insulin resistance, obesity, impaired fasting glucose, impaired glucose tolerance, lipid disorders such as dyslipidemia, hypertension and as well as other diseases and conditions.

  本发明涉及某些酰胺衍生物，这些衍生物具有抑制11-β-羟基类固醇脱氢酶1型（11β-HSD-1）的能力，因此在预防和治疗可以通过抑制该酶来预防或治疗的某些疾病中是有用的。此外，发明还涉及这些化合物的制备方法、含有这些化合物的药物组合物以及这些化合物在治疗某些疾病中的用途。预计本发明的化合物将在治疗非胰岛素依赖型2型糖尿病（NIDDM）、胰岛素抵抗、肥胖、空腹血糖受损、葡萄糖耐量受损、脂质紊乱（如血脂异常）、高血压以及其他疾病和状况中找到应用。
• Carboxylic Acid Compounds and Use Thereof
  申请人：Inoue Teruhiko

  公开号：US20070197512A1

  公开（公告）日：2007-08-23

  Provision of a superior URAT1 activity inhibitor effective for the treatment and the like of a pathology involving uric acid, such as hyperuricemia, gouty tophus, acute gouty arthritis, chronic gouty arthritis, gouty kidney, urinary lithiasis, renal dysfunction, coronary heart disease, ischemic cardiac diseases and the like. A URAT1 activity inhibitor containing a compound represented by the following formula [1] or a pharmaceutically acceptable salt thereof, or a solvate thereof as an active ingredient: wherein each symbol is as defined in the specification.

  提供一种优越的URAT1活性抑制剂，用于治疗与尿酸有关的病理，如高尿酸血症、痛风石、急性痛风性关节炎、慢性痛风性关节炎、痛风性肾病、尿路结石、肾功能障碍、冠心病、缺血性心脏病等。 一种包含下式[1]所表示的化合物或其药学上可接受的盐，或其溶剂化合物的URAT1活性抑制剂作为活性成分： 其中每个符号如规范中定义。
• [EN] CYCLIC AMIDE DERIVATIVES AS INHIBITORS OF 11 - BETA - HYDROXYSTEROID DEHYDROGENASE AND USES THEREOF<br/>[FR] DÉRIVÉS D'AMIDE CYCLIQUES À UTILISER EN TANT QU'INHIBITEURS DE 11-BÊTA-HYDROXYSTÉROÏDE DÉSHYDROGÉNASE ET UTILISATIONS DE CEUX-CI
  申请人：CONNEXIOS LIFE SCIENCES PVT LTD

  公开号：WO2013128465A1

  公开（公告）日：2013-09-06

  The present invention relates to certain amide derivatives that have the ability to inhibit 11-β-hydroxysteroid dehydrogenase type 1 (11β-HSD-1) and which are therefore useful in the treatment of certain disorders that can be prevented or treated by inhibition of this enzyme. In addition the invention relates to the compounds, methods for their preparation, pharmaceutical compositions containing the compounds and the uses of these compounds in the treatment of certain disorders. It is expected that the compounds of the invention will find application in the treatment of conditions such as non-insulin dependent type 2 diabetes mellitus (NIDDM), insulin resistance, obesity, impaired fasting glucose, impaired glucose tolerance, lipid disorders such as dyslipidemia, hypertension and as well as other diseases and conditions.

  本发明涉及某些酰胺衍生物，这些衍生物具有抑制11-β-羟基类固醇脱氢酶1型（11β-HSD-1）的能力，因此在预防或治疗可通过抑制该酶来预防或治疗的某些疾病中是有用的。此外，本发明还涉及这些化合物的制备方法、含有这些化合物的药物组合物以及这些化合物在治疗某些疾病中的用途。预计本发明的化合物将用于治疗非胰岛素依赖型2型糖尿病（NIDDM）、胰岛素抵抗、肥胖、空腹血糖受损、葡萄糖耐量受损、脂质紊乱（如血脂异常）、高血压以及其它疾病和状况。
• Studies on antidiabetic agents. IX. A new aldose reductase inhibitor, AD-5467, and related 1,4-benzoxazine and 1,4-benzothiazine derivatives: Synthesis and biological activity.
  作者：Hiroyuki TAWADA、Yasuo SUGIYAMA、Hitoshi IKEDA、Yujiro YAMAMOTO、Kanji MEGURO

  DOI：10.1248/cpb.38.1238

  日期：——

  N-Acetic acid derivatives (I) of 2-substituted 1, 4-benzoxazines and benzothiazines were designed and synthesized for evaluation as new aldose reductase inhibitors. In general, 3-thioxo derivatives were more potent inhibitors of aldose reductase from human placenta in vitro than the corresponding 3-oxo derivatives. While many compounds (I) were not very effective in inhibiting sorbitol accumulation in the rat sciatic nerve in vivo, the 3-thioxo compounds bearing an isopropyl group at the 2-position showed highly potent activity in the in vivo assay. Compound 46 (AD-5467) was selected from this series as a candidate for further development.

  N-乙酸衍生物（I）的2-取代基1,4-苯并恶嗪和苯并噻嗪被设计合成，以评估其作为新型醛糖还原酶抑制剂的潜力。一般而言，3-硫代羰基衍生物在体外对人胎盘醛糖还原酶的抑制活性比相应的3-氧代衍生物更强。虽然许多化合物（I）在体内对大鼠坐骨神经山梨醇积累的抑制作用并不十分有效，但在体内试验中，2-位带有异丙基的3-硫代羰基化合物显示出极强的活性。从这一系列中选出化合物46（AD-5467）作为进一步开发的候选药物。