N-(6,7-Dihydro-5H-[1]pyrindin-6-yl)-6-methoxymethylnicotinamide | 654675-63-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: N-(6,7-Dihydro-5H-[1]pyrindin-6-yl)-6-methoxymethylnicotinamide
• 英文别名: N-(6,7-dihydro-5H-cyclopenta[b]pyridin-6-yl)-6-(methoxymethyl)pyridine-3-carboxamide
• CAS: 654675-63-5
• 化学式: C₁₆H₁₇N₃O₂
• 分子量: 283.33
• InChiKey: NBQAJSTVWCIHKF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.8
• 重原子数：
  21
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.31
• 拓扑面积：
  64.1
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  6-methoxymethylnicotinic acid 、 6,7-二氢-5H-环戊二烯并[b]吡啶-6-胺 在 O-<[cyano(ethoxycarbonyl)methylene]amino>-1,1,3,3-tetramethyluronium tetrafluoroborate 、 N,N-二异丙基乙胺 作用下， 以 四氢呋喃 、 DMF (N,N-dimethyl-formamide) 为溶剂， 反应 12.5h， 生成 N-(6,7-Dihydro-5H-[1]pyrindin-6-yl)-6-methoxymethylnicotinamide
  参考文献：
  名称：

  Acylated, heteroaryl-condensed cycloalkenylamines and their use as pharmaceuticals

  摘要：

  本发明涉及公式I的酰化的异杂环缩合环烯基胺，其中A，R1，R2，R3，R4，R5和n具有声明中指定的含义。公式I的化合物是有价值的药理活性化合物，可用于治疗各种疾病状态，包括心血管疾病，如动脉粥样硬化，血栓形成，冠状动脉疾病，高血压和心脏衰竭。它们升调内皮一氧化氮（NO）合酶的表达，并可应用于需要增加该酶的表达或增加NO水平或恢复降低的NO水平的情况。本发明还涉及公式I化合物的制备方法，它们的使用，特别是作为药物中的活性成分，以及包含它们的制药制剂。

  公开号：

  EP1388342A1

文献信息

• ACYLATED, HETEROARYL-CONDENSED CYCLOALKENYLAMINES AND THEIR USE AS PHARMACEUTICALS
  申请人：Aventis Pharma Deutschland GmbH

  公开号：EP1534277A1

  公开（公告）日：2005-06-01
• [EN] ACYLATED, HETEROARYL-CONDENSED CYCLOALKENYLAMINES AND THEIR USE AS PHARMACEUTICALS<br/>[FR] CYCLOALCENYLAMINES ACYLEES ET HETEROARYLE-CONDENSEES ET UTILISATION DE CELLES-CI COMME PRODUITS PHARMACEUTIQUES
  申请人：AVENTIS PHARMA GMBH

  公开号：WO2004014372A1

  公开（公告）日：2004-02-19

  The present invention relates to acylated, heteroaryl-condensed cycloalkenylamines of the formula I, (I) in which A, R1, R2, R3, R4, R5 and n have the meanings indicated in the claims. The compounds of formula I are valuable pharmacologically active compounds which are useful in the treatment of various disease states including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency. They upregulate the expression of the enzyme endothelial nitric oxide (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 furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.
• Acylated, heteroaryl-condensed cycloalkenylamines and their use as pharmaceuticals
  申请人：Aventis Pharma Deutschland GmbH

  公开号：EP1388342A1

  公开（公告）日：2004-02-11

  The present invention relates to acylated, heteroaryl-condensed cycloalkenylamines of the formula I, in which A, R1, R2, R3, R4, R5 and n have the meanings indicated in the claims. The compounds of formula I are valuable pharmacologically active compounds which are useful in the treatment of various disease states including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency. They upregulate the expression of the enzyme endothelial nitric oxide (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 furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.

  本发明涉及公式I的酰化的异杂环缩合环烯基胺，其中A，R1，R2，R3，R4，R5和n具有声明中指定的含义。公式I的化合物是有价值的药理活性化合物，可用于治疗各种疾病状态，包括心血管疾病，如动脉粥样硬化，血栓形成，冠状动脉疾病，高血压和心脏衰竭。它们升调内皮一氧化氮（NO）合酶的表达，并可应用于需要增加该酶的表达或增加NO水平或恢复降低的NO水平的情况。本发明还涉及公式I化合物的制备方法，它们的使用，特别是作为药物中的活性成分，以及包含它们的制药制剂。