N-[3-(pyridin-3-yl)propionyl]-4-(4-diphenylmethyl-1-piperazinyl)butylamine | 107755-78-2

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: N-[3-(pyridin-3-yl)propionyl]-4-(4-diphenylmethyl-1-piperazinyl)butylamine
• 英文别名: N-[4-(4-diphenylmethyl-piperazin-1-yl)-butyl]-3-pyridin-3-yl-propionamide；N-[3-(3-pyridyl)propionyl]-4-(4-diphenylmethyl-1-piperazinyl)butylamine；N-[4-(4-benzhydrylpiperazin-1-yl)butyl]-3-pyridin-3-ylpropanamide
• CAS: 107755-78-2
• 化学式: C₂₉H₃₆N₄O
• 分子量: 456.631
• InChiKey: JFHVQGJIXVSWFD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.1
• 重原子数：
  34
• 可旋转键数：
  11
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  48.5
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  反-3(3-吡啶基)烯丙酸 在 palladium on activated charcoal 氢气 、 盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺 作用下， 以 甲醇 、 二氯甲烷 、 N,N-二甲基甲酰胺 为溶剂， 25.0 ℃ 、101.33 kPa 条件下， 生成 N-[3-(pyridin-3-yl)propionyl]-4-(4-diphenylmethyl-1-piperazinyl)butylamine
  参考文献：
  名称：

  Acrylamide derivatives as antiallergic agents. 2. Synthesis and structure activity relationships of N-[4-[4-(diphenylmethyl)-1-piperazinyl]butyl]-3-(3-pyridyl)acrylamides

  摘要：

  A new series of 3-(3-pyridyl)acrylamides 16, 17, 19, and 26, and 5-(3-pyridyl)-2,4-pentadienamides 20-25 were prepared and evaluated for their antiallergic activity. Several of these compounds exhibited more potent inhibitory activities than the parent compound 1a [(E)-N-[4-[4-(diphenylmethyl)-1-piperazinyl]butyl]-3- (3-pyridyl)acrylamide] against the rat passive cutaneous anaphylaxis (PCA) reaction and the enzyme 5-lipoxygenase. Particularly, (E)-N-[4-[4-(diphenylmethyl)-1-piperazinyl]butyl]-3- (6-methyl-3-pyridyl)acrylamide (17p) showed an ED50 value of 3.3 mg/kg po in the rat PCA test, which was one-fifth of ketotifen and oxatomide. As compared with ketotifen and oxatomide, compound 17p (AL-3264) possessed a better balance of antiallergic properties due to inhibition of chemical mediator release, inhibition of 5-lipoxygenase, and antagonism of histamine.

  DOI：

  10.1021/jm00123a012

文献信息

• Use of pyridyl amides as inhibitors of angiogenesis
  申请人：Fujisawa Deutschland GmbH

  公开号：EP1348434A1

  公开（公告）日：2003-10-01

  The invention relates to the use of derivatives of Formula I in the manufacture of a pharmaceutical composition for the treatment of a mammal, in which inappropriate, excessive or undesirable angiogenesis has occurred, and to the prevention thereof.

  本发明涉及使用公式I的衍生物制备药物组合物，用于治疗哺乳动物中发生了不合适、过度或不良的血管生成，并防止其发生。
• Pyridine compounds, process for the preparation thereof and pharmaceutical composition containing the same
  申请人：Dainippon Pharmaceutical Co., Ltd.

  公开号：EP0210782A2

  公开（公告）日：1987-02-04

  Compounds of the formula: wherein X is alkylene or-(CR6-CR7)r- wherein R6 is H, alkyl or phenyl, R7 is H, alkyl, cyano or phenyl, and r is 1 or 2; A is alkylene or alkylene interrupted by at least one double bond; R1 is H, halogen, alkyl, alkoxy, alkylthio, cycloalkyloxy, cycloa-Ikylthio, alkoxycarbonyl, carboxy, phenyl, phenoxy, phenylthio, 3-pyridyloxy or 3-pyridylthio; R2 is H, hydroxy, alkanoyloxy or alkoxycarbonyloxy, or adjacent R, and R2 may combine to form tetramethylene or-CH2OCR8R9O-(R8 and Rg are alkyl); R3 is H, alkyl or hydroxyalkyl; R4 is H or alkyl; R5 is phenyl, heteroaryl or-(CH2)m-CHR10R11 (R10 is H or phenyl, R11 is phenyl or pyridyl and m is 0 to 2); p is 0 or 1; and q is 2 or 3; the phenyl group or moiety being optionally substituted, and salts thereof show excellent antiallergic activity mainly through 5-lipoxygenase inhibiting activity, antihistamine activity and/or inhibitory activity against chemical mediator release and are useful for treatment of allergic diseases. Processes for their preparation and pharmaceutical compositions containing them are also described.

  式中的化合物： 其中 X 是亚烷基或-(CR6-CR7)r- 其中 R6 是 H、烷基或苯基，R7 是 H、烷基、氰基或苯基，r 是 1 或 2；A 是亚烷基或至少被一个双键打断的亚烷基； R1 是 H、卤素、烷基、烷氧基、烷硫基、环烷氧基、环烷硫基、烷氧羰基、羧基、苯基、苯氧基、苯硫基、3-吡啶氧基或 3-吡啶硫基；R2 是 H、羟基、烷酰氧基或烷氧基羰基氧基，或相邻 R 和 R2 可结合形成四亚甲基或-CH2OCR8R9O-（R8 和 Rg 是烷基）；R3 是 H、烷基或羟烷基；R4 是 H 或烷基；R5 是苯基、杂芳基或-(CH2)m-CHR10R11（R10 是 H 或苯基，R11 是苯基或吡啶基，m 是 0 至 2）；p 是 0 或 1；q 是 2 或 3；苯基或分子被任选取代，其盐类主要通过 5-脂氧合酶抑制活性、抗组胺活性和/或对化学介质释放的抑制活性显示出优异的抗过敏活性，可用于治疗过敏性疾病。此外，还介绍了它们的制备工艺和含有它们的药物组合物。
• Use of pyridly amides as inhibitors of angiogenesis
  申请人：Biedermann Elfi

  公开号：US20060052419A1

  公开（公告）日：2006-03-09

  The invention relates to the use of derivatives of Formula I in the manufacture of a pharmaceutical composition for the treatment of a mammal, in which inappropriate, excessive or undesirable angiogenesis has occurred, and to the prevention thereof. (I)

  本发明涉及式 I 衍生物在制造药物组合物中的用途，该药物组合物用于治疗发生了不适当、过度或不良血管生成的哺乳动物，以及预防其发生。(I)
• USE OF PYRIDYL AMIDES AS INHIBITORS OF ANGIOGENESIS
  申请人：Fujisawa Deutschland GmbH

  公开号：EP1487444A1

  公开（公告）日：2004-12-22
• JP2005528361A
  申请人：——

  公开号：JP2005528361A

  公开（公告）日：2005-09-22