1-(2-{[6-(2-Fluorophenyl)pyridin-3-yl]oxy}ethyl)azetidin-2-one | 918146-02-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 内酰胺类
• 英文名称: 1-(2-{[6-(2-Fluorophenyl)pyridin-3-yl]oxy}ethyl)azetidin-2-one
• 英文别名: 1-[2-[6-(2-fluorophenyl)pyridin-3-yl]oxyethyl]azetidin-2-one
• CAS: 918146-02-8
• 化学式: C₁₆H₁₅FN₂O₂
• 分子量: 286.3
• InChiKey: NGEHZCHNBNMIKO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.8
• 重原子数：
  21
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  42.4
• 氢给体数：
  0
• 氢受体数：
  4

文献信息

• Heteroaryl-substituted amides comprising a saturated linker group, and their use as pharmaceuticals
  申请人：Sanofi-Aventis Deutschland GmbH

  公开号：EP1741709A1

  公开（公告）日：2007-01-10

  The present invention relates to N-alkylamides of the formula I, in which A, Het, X, R1, R2 and R3 have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of the formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. The invention further relates to processes for the preparation of compounds of the formula I, to pharmaceutical compositions comprising them, and to the use of compounds of the formula I for the manufacture of a medicament for the stimulation of the expression of endothelial NO synthase or for the treatment of various diseases including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency, for example.

  本发明涉及式I的N-烷基酰胺， 其中A、Het、X、R1、R2和R3的含义如权利要求中指出的，这些化合物能够调节内皮型一氧化氮（NO）合酶的转录，并且是有价值的药物活性化合物。具体而言，式I的化合物可以上调内皮型NO合酶的表达，并可用于那些需要增加所述酶的表达、增加NO水平或使降低的NO水平正常化的情况。本发明还涉及制备式I化合物的方法，包含它们的药物组合物，以及使用式I化合物用于制造刺激内皮型NO合酶表达或治疗包括动脉粥样硬化、血栓、冠心病、高血压和心力衰竭等各种疾病的药物。
• Heteroaryl-Substituted Amides Comprising A Saturated Linker Group, And Their Use As Pharmaceuticals
  申请人：STROBEL Harmut

  公开号：US20080171739A1

  公开（公告）日：2008-07-17

  The present invention relates to N-alkylamides of the formula I, in which A, Het, X, R 1 , R 2 and R 3 have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of the formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. The invention further relates to processes for the preparation of compounds of the formula I, to pharmaceutical compositions comprising them, and to the use of compounds of the formula I for the manufacture of a medicament for the stimulation of the expression of endothelial NO synthase or for the treatment of various diseases including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency, for example.

  本发明涉及公式I的N-烷基酰胺，其中A，Het，X，R1，R2和R3具有所述声明中指示的含义，这些化合物调节内皮一氧化氮（NO）合酶的转录，并是有价值的药理活性化合物。具体地，公式I的化合物上调内皮一氧化氮合酶酶的表达，并可应用于需要增加该酶的表达或增加NO水平或规范降低的NO水平的情况。本发明还涉及制备公式I化合物的过程，包括它们的制药组合物，以及公式I化合物用于制造刺激内皮一氧化氮合酶表达或治疗各种疾病的药物的用途，包括心血管疾病，如动脉粥样硬化，血栓形成，冠状动脉疾病，高血压和心脏功能不全等。
• HETEROARYL-SUBSTITUTED AMIDES COMPRISING A SATURATED LINKER GROUP, AND THEIR USE AS PHARMACEUTICALS
  申请人：Sanofi-Aventis

  公开号：EP1899321A1

  公开（公告）日：2008-03-19
• US8518976B2
  申请人：——

  公开号：US8518976B2

  公开（公告）日：2013-08-27
• [EN] HETEROARYL-SUBSTITUTED AMIDES COMPRISING A SATURATED LINKER GROUP, AND THEIR USE AS PHARMACEUTICALS<br/>[FR] AMIDES À SUBSTITUTION HÉTÉROARYLE COMPRENANT UN GROUPE DE LIAISON SATURÉ, ET LEUR UTILISATION EN TANT QUE PRODUITS PHARMACEUTIQUES
  申请人：SANOFI AVENTIS DEUTSCHLAND

  公开号：WO2007000246A1

  公开（公告）日：2007-01-04

  [EN] The present invention relates to N-alkylamides of the formula (I), in which A, Het, X, R¹, R² and R³ have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of the formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. The invention further relates to processes for the preparation of compounds of the formula I, to pharmaceutical compositions comprising them, and to the use of compounds of the formula I for the manufacture of a medicament for the stimulation of the expression of endothelial NO synthase or for the treatment of various diseases including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency, for example.
  [FR] La présente invention concerne des N-alkylamides provenant de la formule (I), dans laquelle A, Het, X, R¹, R² et R³ ont les significations indiquées dans les revendications, qui modulent la transcription de la synthase endothéliale d'oxyde nitrique (NO) et représentent des composés de valeur pharmacologiquement actifs. Plus spécifiquement, les composés de la formule (I) régulent à la hausse l'expression de l'enzyme de la synthase endothéliale d'oxyde nitrique et peuvent être appliqués lorsque l'on souhaite augmenter l'expression dudit enzyme, augmenter le niveau d'oxyde nitrique, ou normaliser le niveau décroissant d'oxyde nitrique. L'invention porte également sur les procédés de préparation de composés de la formule (I), sur les compositions pharmaceutiques les renfermant, et l'utilisation des composés de la formule (I) lors de la fabrication d'un médicament visant à stimuler l'expression de la synthase endothéliale d'oxyde nitrique ou lors du traitement de diverses maladies dont les troubles cardiovasculaires tels que l'athérosclérose, la thrombose, les maladies coronariennes, l'hypertension et l'insuffisance cardiaque, par exemple.