4-oxo-2,3,4,5-tetrahydro-1H-naphtho[2,1-b]azepine | 178201-77-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯氮卓类
• 英文名称: 4-oxo-2,3,4,5-tetrahydro-1H-naphtho[2,1-b]azepine
• 英文别名: 1,2,3,5-tetrahydrobenzo[g][1]benzazepin-4-one
• CAS: 178201-77-9
• 化学式: C₁₄H₁₃NO
• 分子量: 211.263
• InChiKey: JQFNQEHAIUGKPJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  16
• 可旋转键数：
  0
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.21
• 拓扑面积：
  29.1
• 氢给体数：
  1
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  4-oxo-2,3,4,5-tetrahydro-1H-naphtho[2,1-b]azepine 在 三甲基氯硅烷 、 氨 、 碘 、 sodium iodide 作用下， 以 甲醇 为溶剂， 生成 3-amino-4-oxo-2,3,4,5-tetrahydro-1H-naphtho [2,1-b]azepine
  参考文献：
  名称：

  Naphtho-fused azepines as potent growth hormone secretagogues

  摘要：

  Computerguided improvements of known growth hormone secretagogues are reported. These are a new series of napthofused azepines. Structure-activity relationships are different than in the corresponding benzo-fused azepines. (C) 1997 Eisevier Science Ltd.

  DOI：

  10.1016/s0960-894x(97)10115-9
• 作为产物：
  描述：

  (NE)-N-(3,4-dihydro-2H-phenanthren-1-ylidene)hydroxylamine 在 甲烷磺酸 作用下， 生成 4-oxo-2,3,4,5-tetrahydro-1H-naphtho[2,1-b]azepine
  参考文献：
  名称：

  Naphtho-fused azepines as potent growth hormone secretagogues

  摘要：

  Computerguided improvements of known growth hormone secretagogues are reported. These are a new series of napthofused azepines. Structure-activity relationships are different than in the corresponding benzo-fused azepines. (C) 1997 Eisevier Science Ltd.

  DOI：

  10.1016/s0960-894x(97)10115-9

文献信息

• N-substituted naphthofused lactams
  申请人：Novo Nordisk A/S

  公开号：US05817654A1

  公开（公告）日：1998-10-06

  The present invention relates to novel N-substituted naphthofused lactams and salts thereof of the formula ##STR1## Compounds of the general formula I possess the ability to stimulate the release of endogenous growth hormone. Thus, these compounds may be used in the treatment of conditions which require stimulation of growth hormone production or secretion such as in humans with growth hormone deficiency or where increased growth hormone plasma levels are desired, for instance in elderly patients or in livestock.

  本发明涉及新型N-取代的萘并噁唑内酰胺及其盐，化学式如下：化合物的一般式I具有刺激内源性生长激素释放的能力。因此，这些化合物可用于治疗需要刺激生长激素产生或分泌的病症，例如对于生长激素缺乏症或需要增加生长激素血浆水平的人类，例如老年患者或家畜。
• TRIAZOLE DERIVATIVES FOR TREATING ALZHEIMER'S DISEASE AND RELATED CONDITIONS
  申请人：Fischer Christian

  公开号：US20100222320A1

  公开（公告）日：2010-09-02

  Compounds of formula I: Selectively attenuate production of Aβ(1-42) and hence find use in treatment or prevention of diseases associated with deposition of Aβ in the brain, in particular Alzheimer's disease.

  公式为I的化合物：选择性地减弱Aβ（1-42）的产生，因此可用于治疗或预防与Aβ在大脑中沉积相关的疾病，特别是阿尔茨海默病。
• Discovery of novel triazolobenzazepinones as γ-secretase modulators with central Aβ42 lowering in rodents and rhesus monkeys
  作者：Christian Fischer、Susan L. Zultanski、Hua Zhou、Joey L. Methot、Sanjiv Shah、Ikuo Hayashi、Bethany L. Hughes、Christopher M. Moxham、Nathan W. Bays、Nadya Smotrov、Armetta D. Hill、Bo-Sheng Pan、Zhenhua Wu、Lily Y. Moy、Flobert Tanga、Candia Kenific、Jonathan C. Cruz、Deborah Walker、Melanie Bouthillette、George N. Nikov、Sujal V. Deshmukh、Valentina V. Jeliazkova-Mecheva、Damaris Diaz、Maria S. Michener、Jacquelynn J. Cook、Benito Munoz、Mark S. Shearman

  DOI：10.1016/j.bmcl.2015.07.003

  日期：2015.9

  Synthesis and SAR studies of novel triazolobenzazepinones as gamma secretase modulators (GSMs) are presented in this communication. Starting from our azepinone leads, optimization studies toward improving central lowering of A beta 42 led to the discovery of novel benzo-fused azepinones. Several benzazepinones were profiled in vivo and found to lower brain A beta 42 levels in Sprague Dawley rats and transgenic APP-YAC mice in a dose-dependent manner after a single oral dose. Compound 34 was further progressed into a pilot study in our cisterna-magna-ported rhesus monkey model, where we observed robust lowering of CSF A beta 42 levels. (C) 2015 Elsevier Ltd. All rights reserved.
• NOVEL N-SUBSTITUTED NAPHTHOFUSED LACTAMS
  申请人：NOVO NORDISK A/S

  公开号：EP0777668A1

  公开（公告）日：1997-06-11
• US5817654A
  申请人：——

  公开号：US5817654A

  公开（公告）日：1998-10-06