4-(4-fluoro-benzyloxy)-1-{2-oxo-2-[2-(2,2,2-trifluoro-acetyl)-1,2,3,4-tetrahydro-isoquinolin-7-yl]-ethyl}-1H-pyridin-2-one | 1184950-21-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 四氢异喹啉
• 英文名称: 4-(4-fluoro-benzyloxy)-1-{2-oxo-2-[2-(2,2,2-trifluoro-acetyl)-1,2,3,4-tetrahydro-isoquinolin-7-yl]-ethyl}-1H-pyridin-2-one
• 英文别名: 4-[(4-fluorophenyl)methoxy]-1-[2-oxo-2-[2-(2,2,2-trifluoroacetyl)-3,4-dihydro-1H-isoquinolin-7-yl]ethyl]pyridin-2-one
• CAS: 1184950-21-7
• 化学式: C₂₅H₂₀F₄N₂O₄
• 分子量: 488.438
• InChiKey: MEPYOCKLBDIAJK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.5
• 重原子数：
  35
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.24
• 拓扑面积：
  66.9
• 氢给体数：
  0
• 氢受体数：
  8

文献信息

• [EN] PYRIDONE AND PYRIDAZINONE DERIVATIVES AS MCH ANTAGONISTS<br/>[FR] DÉRIVÉS DE PYRIDONE ET DE PYRIDAZINONE COMME ANTAGONISTES DE LA MCH
  申请人：BOEHRINGER INGELHEIM INT

  公开号：WO2009103478A1

  公开（公告）日：2009-08-27

  The present invention relates to pyridone and pyridazinone derivatives as listed in claim 1 including their salts. Moreover the invention relates to pharmaceutical compositions containing at least one compound according to the invention. By virtue of their MCH- receptor antagonistic activity the pharmaceutical compositions according to the invention are suitable for the treatment of metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia and diabetes.

  本发明涉及权利要求1中所列的吡啶酮和吡啶并二嗪酮衍生物及其盐。此外，本发明还涉及含有至少一种根据本发明的化合物的药物组合物。凭借其黑色素细胞刺激素受体拮抗活性，根据本发明的药物组合物适用于治疗代谢紊乱和/或饮食失调，特别是肥胖、贪食症、厌食症、过食和糖尿病。
• 5-PHENYL-5,6,7,8-HYDROQUINOLINE TACHYKININ RECEPTOR ANTAGONISTS
  申请人：Merck & Co., Inc.

  公开号：EP1819676A2

  公开（公告）日：2007-08-22
• EP1819676A4
  申请人：——

  公开号：EP1819676A4

  公开（公告）日：2009-04-15
• [EN] 5-PHENYL-5,6,7,8-HYDROQUINOLINE TACHYKININ RECEPTOR ANTAGONISTS<br/>[FR] ANTAGONISTES DE RECEPTEURS DE TACHYKININE 5-PHENYL-5,6,7,8-HYDROQUINOLINE
  申请人：MERCK & CO INC

  公开号：WO2006060344A2

  公开（公告）日：2006-06-08

  [EN] The present invention is directed to certain 5-phenyl-5,6,7,8-hydroquinoline compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.
  [FR] L'invention concerne certains composés 5-phényl-5,6,7,8-hydroquinoline utiles en tant qu'antagonistes des récepteurs de la neurokinine-1 (NK-1), et inhibiteurs de la tachykinine, en particulier de la substance P. L'invention concerne également des préparations pharmaceutiques contenant ces composés comme principes actifs, ainsi que l'utilisation desdits composés et préparations dans le traitement de certains troubles, notamment le vomissement, l'incontinence urinaire, la dépression et l'anxiété.