(+/-)-2-(Ethoxymethyl)-1,2,3,6-tetrahydro-1-(2,2,2-trifluoroethyl)-9-(trifluoromethyl)-7H-[1,4]oxazino[3,2-g]quinolin-7-one | 329228-85-5

• 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
• 英文名称: (+/-)-2-(Ethoxymethyl)-1,2,3,6-tetrahydro-1-(2,2,2-trifluoroethyl)-9-(trifluoromethyl)-7H-[1,4]oxazino[3,2-g]quinolin-7-one
• 英文别名: 2-(ethoxymethyl)-1-(2,2,2-trifluoroethyl)-9-(trifluoromethyl)-3,6-dihydro-2H-pyrido[3,2-g][1,4]benzoxazin-7-one
• CAS: 329228-85-5
• 化学式: C₁₇H₁₆F₆N₂O₃
• 分子量: 410.316
• InChiKey: LGNNPMLVSVGWSH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  28
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.47
• 拓扑面积：
  50.8
• 氢给体数：
  1
• 氢受体数：
  10

反应信息

• 作为产物：
  描述：

  (+/-)-2-(ethoxymethyl)-2,3-dihydro-7-isopropoxy-1-(2,2,2-trifluoroethyl)-9-(trifluoromethyl)-1H-[1,4]oxazino[3,2-g]quinoline 在 盐酸 、 溶剂黄146 作用下， 生成 (+/-)-2-(Ethoxymethyl)-1,2,3,6-tetrahydro-1-(2,2,2-trifluoroethyl)-9-(trifluoromethyl)-7H-[1,4]oxazino[3,2-g]quinolin-7-one
  参考文献：
  名称：

  Selective androgen receptor modulators based on a series of 7H-[1,4]oxazino[3,2-g]quinolin-7-ones with improved in vivo activity

  摘要：

  Modification on a lead series of [1,4] oxazino[3,2-g] quinolin-7-ones at the 2-position led to selective androgen receptor modulators with improved in vivo activity. The most potent analog (-)-33a exhibited full maintenance of levator ani muscle at 3 mg/kg and reduced activity on ventral prostate weight in a 2-week orally-dosed and orchidectomized rat maintenance assay. (C) 2008 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2008.03.062

文献信息

• Androgen receptor modulator compounds and methods
  申请人：Ligand Pharmaceuticals, Inc.

  公开号：US06462038B1

  公开（公告）日：2002-10-08

  Compounds, pharmaceutical compositions, and methods for modulating processes mediated by steroid receptors. In particular, preparation and methods of use of non-steroidal compounds and compositions that are agonists, partial agonists, and antagonists for the androgen receptor (AR) are described. Further, described are the methods of making and use of critical intermediates including a stereoselective synthetic route to intermediates for the AR modulators.

  化合物、药物组合物和调节类固醇受体介导过程的方法。具体描述了非类固醇化合物和组合物的制备和使用方法，这些化合物和组合物是雄激素受体（AR）的激动剂、部分激动剂和拮抗剂。此外，还描述了制备和使用关键中间体的方法，包括用于AR调节剂的立体选择性合成路线。
• Androgen Receptor Modulator Compounds and Methods
  申请人：Loren Jon C.

  公开号：US20090227571A1

  公开（公告）日：2009-09-10

  Provided herein are compounds that bind to androgen receptors and modulate the activity and/or the amount of androgen receptors and to methods for making and using such compounds. Also provided are compositions including such compounds and methods for making and using such compositions.

  本文提供了一些结合雄激素受体并调节雄激素受体的活性和/或数量的化合物，以及制备和使用这些化合物的方法。还提供了包括这些化合物的组合物以及制备和使用这些组合物的方法。
• PHARMACEUTICAL COMPOSITION FOR INHIBITING ACCUMULATION OF AMYLOID- BETA PROTEIN
  申请人：Sumitomo Chemical Company, Limited

  公开号：EP2199284A1

  公开（公告）日：2010-06-23

  The present invention provides: a pharmaceutical composition for inhibiting amyloid-β protein accumulation comprising a compound represented by the formulas including (I) or a pharmaceutically acceptable salt thereof; a method for inhibiting amyloid-β protein accumulation, comprising a step of administering an effective amount of the compound represented by the formulas including (I) or a pharmaceutically acceptable salt thereof to a mammal which may be diagnosed with an amyloid-β protein-related disease; and so on.

  本发明提供了：一种用于抑制淀粉样蛋白-β蛋白积累的药物组合物，该组合物由包括（I）在内的式子所代表的化合物或其药学上可接受的盐；一种抑制淀粉样蛋白-β蛋白积累的方法，该方法包括向可能被诊断患有淀粉样蛋白-β蛋白相关疾病的哺乳动物施用有效量的包括（I）在内的式子所代表的化合物或其药学上可接受的盐的步骤；等等。
• ANDROGEN RECEPTOR MODULATOR COMPOUNDS AND METHODS
  申请人：LIGAND PHARMACEUTICALS INCORPORATED

  公开号：EP1212330B1

  公开（公告）日：2006-04-19
• PHARMACEUTICAL COMPOSITION FOR INHIBITING AMYLOID-beta PROTEIN ACCUMULATION
  申请人：Motonaga Kozo

  公开号：US20100204216A1

  公开（公告）日：2010-08-12

  The present invention provides: a pharmaceutical composition for inhibiting amyloid-β protein accumulation comprising a compound represented by the formulas including (I) or a pharmaceutically acceptable salt thereof; a method for inhibiting amyloid-β protein accumulation, comprising a step of administering an effective amount of the compound represented by the formulas including (I) or a pharmaceutically acceptable salt thereof to a mammal which may be diagnosed with an amyloid-β protein-related disease; and so on.