8-(2-ethyl-6-methylbenzylamino)-3-hydroxymethyl-2-methylimidazo[1,2-a]pyridine-6-carboxamide

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 咪唑并吡啶类
• 英文名称: 8-(2-ethyl-6-methylbenzylamino)-3-hydroxymethyl-2-methylimidazo[1,2-a]pyridine-6-carboxamide
• 英文别名: AR-HO47116；8-[(2-ethyl-6-methylphenyl)methylamino]-3-(hydroxymethyl)-2-methylimidazo[1,2-a]pyridine-6-carboxamide
• 化学式: C₂₀H₂₄N₄O₂
• 分子量: 352.436
• InChiKey: CKAMGCWTONYLBM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.8
• 重原子数：
  26
• 可旋转键数：
  6
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  92.6
• 氢给体数：
  3
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  8-(2-ethyl-6-methylbenzylamino)-3-hydroxymethyl-2-methylimidazo[1,2-a]pyridine-6-carboxamide 在 sodium hydroxide 作用下， 以 乙醇 、 水 为溶剂， 以0.012 g (60%)的产率得到8-(2-ethyl-6-methylbenzylamino)-3-hydroxymethyl-2-methylimidazo[1,2-a]pyridine-6-carboxylic acid
  参考文献：
  名称：

  Imidazo pyridine derivatives which inhibit gastric acid secretion

  摘要：

  本发明涉及式(I)的咪唑吡啶衍生物，其中苯基部分被取代，咪唑吡啶部分在6位被取代为羧酰胺基团，这些衍生物抑制外源性或内源性刺激引起的胃酸分泌，因此可用于预防和治疗胃肠道炎症性疾病。

  公开号：

  US06313136B1
• 作为产物：
  描述：

  Ethyl 6-(aminocarbonyl)-8-(2-ethyl-6-methylbenzylamino)-2-methylimidazo[1,2-a]pyridine-3-carboxylate 、 锂硼氢 、 四氢呋喃 在 水 、 乙醇乙酸乙酯 、 乙醚 作用下， 以 甲醇 、 水 为溶剂， 反应 8.5h， 以to give the desired product (115 mg, 46%)的产率得到8-(2-ethyl-6-methylbenzylamino)-3-hydroxymethyl-2-methylimidazo[1,2-a]pyridine-6-carboxamide
  参考文献：
  名称：

  Imidazo pyridine derivatives which inhibit gastric acid secretion

  摘要：

  本发明涉及式(I)的咪唑吡啶衍生物，其中苯基取代，咪唑吡啶基团在6位取代为羧酰胺基团，能够抑制内源性或外源性刺激的胃酸分泌，因此可用于预防和治疗胃肠道炎症性疾病。

  公开号：

  US06313137B1

文献信息

• Pharmaceutical preparation comprising an active dispersed on a matrix
  申请人：——

  公开号：US20040058896A1

  公开（公告）日：2004-03-25

  The present invention relates to the field of pharmaceutical technology and describes a novel advantageous preparation for an active ingredient. The novel preparation is suitable for producing a large number of pharmaceutical dosage forms. In the new preparation an active ingredient is present essentially uniformly dispersed in an excipient matrix composed of one or more excipients selected from the group of fatty alcohol, triglyceride, partial glyceride and fatty acid ester.

  本发明涉及制药技术领域，描述了一种新的有利的活性成分制备方法。这种新的制备方法适用于生产大量的药物剂型。在这种新的制备方法中，活性成分基本上均匀地分散在由脂肪醇、甘油三酯、部分甘油酯和脂肪酸酯等多种赋形剂中选择的一种或多种赋形剂组成的赋形剂基质中。
• [EN] IMIDAZO PYRIDINE DERIVATIVES WHICH INHIBIT GASTRIC ACID SECRETION<br/>[FR] DERIVES D'IMIDAZO PYRIDINE QUI INHIBENT LA SECRETION D'ACIDE GASTRIQUE
  申请人：ASTRA AB

  公开号：WO1999055706A1

  公开（公告）日：1999-11-04

  The present invention relates to imidazo pyridine derivatives of formula (I), in which the phenyl moiety is substituted, and in which the imidazo pyridine moiety is substituted with a carboxyamide group in 6-position, which inhibit exogenously or endogenously stimulated gastric acid secretion and thus can be used in the prevention and treatment of gastrointestinal inflammatory diseases.

  本发明涉及公式(I)的咪唑吡啶衍生物，其中苯基基团被取代，咪唑吡啶基团在6位被羧酰胺基团取代，能够抑制外源性或内源性刺激胃酸分泌，因此可用于预防和治疗胃肠道炎症性疾病。
• Imidazo[1,2-a]pyridine derivatives for use in the treatment of sleep disturbance due to silent gastro-esophageal reflux
  申请人：AstraZeneca AB

  公开号：EP1974730A1

  公开（公告）日：2008-10-01

  The present invention relates to a new method of treatment of sleep disturbance due to silent gastro-esophageal reflux. In particular, the present invention relates to the use of certain imidazo[1,2-a]pyridines derivatives in said treatment.

  本发明涉及一种治疗无声胃食管反流引起的睡眠障碍的新方法。本发明尤其涉及某些咪唑并[1,2-a]吡啶衍生物在上述治疗中的应用。
• Novel modified release formulation
  申请人：——

  公开号：US20040067252A1

  公开（公告）日：2004-04-08

  The present invention is directed to a multiparticulate, modified release solid dispersion formulation, comprising a drug substance having a pH-dependent solubility, said drug substance being a compound of the formula I, or a pharmaceutically acceptable salt thereof; a hydrophobic matrix former which is a water-insoluble, non-swelling amphiphilic lipid; and a hydrophilic matrix former which is a meltable, water-soluble excipient; wherein the weight ratio hydrophobic matrix former/hydrophilic matrix former is ≧1; and the particle size is less than 300 &mgr;m. Also a unit dosage of the same, as well as a process for the preparation thereof and the use of the formulation and unit dosage is claimed.

  本发明涉及一种多颗粒、改进释放型固体分散制剂，包括一种溶解度取决于 pH 值的药物，所述药物为式 I 的化合物或其药学上可接受的盐； 疏水基质前体，它是一种不溶于水、无溶胀性的两性脂质；以及亲水基质前体，它是一种可熔化的水溶性赋形剂；其中疏水基质前体/亲水基质前体的重量比为≧1;，粒度小于300&mgr;m。 此外，还要求得到一种相同的单位剂量及其制备工艺，以及该制剂和单位剂量的使用方法。
• Compositions useful for treating gastrointestinal motility disorders
  申请人：Landau B. Steven

  公开号：US20050059704A1

  公开（公告）日：2005-03-17

  The present invention relates to method of treating a gastrointestinal motility disorder in a subject in need of treatment comprising coadministering to said subject a first amount of a compound having 5-HT 3 receptor agonist activity or a pharmaceutically acceptable salt, hydrate or solvate thereof; and a second amount of at least one gastric acid suppressing agent (e.g., a proton pump inhibitor, an H 2 receptor antagonist or a pharmaceutically acceptable salt, hydrate or solvate thereof; or an acid pump antagonist or pharmaceutically acceptable salt, hydrate or solvate thereof) wherein the first and second amounts together comprise a therapeutically effective amount. In particular, the method is for treating GERD, including nocturnal GERD. The invention further relates to a method of treating nocturnal GERD comprising administering to a subject in need thereof a therapeutically effective amount of a compound having 5-HT 3 receptor agonist activity or a pharmaceutically acceptable salt, hydrate or solvate thereof. The invention further relates to a method of increasing esophageal motility in a subject in need thereof. The method of increasing esophageal motility can be achieved by administration of a compound having 5-HT 3 receptor agonist activity or a pharmaceutically acceptable salt, hydrate or solvate thereof. The coadministration can also be used to increase esophageal motility.

  本发明涉及治疗需要治疗的受试者胃肠道运动紊乱的方法，包括向所述受试者联合施用第一种量的具有 5-HT 3 受体激动剂活性的化合物或其药学上可接受的盐、水合物或溶液；以及第二种量的至少一种胃酸抑制剂（如质子泵抑制剂、H 2 受体拮抗剂或其药学上可接受的盐、水合物或溶液；或酸泵拮抗剂或其药学上可接受的盐、水合物或溶液），其中第一和第二量共同构成治疗有效量。特别是，该方法用于治疗胃食管反流病，包括夜间胃食管反流病。本发明进一步涉及一种治疗夜间胃食管反流病的方法，该方法包括向有需要的受试者施用治疗有效量的具有 5-HT 3 受体激动剂活性的化合物或其药学上可接受的盐、水合物或溶液。本发明进一步涉及一种增加需要者食管蠕动的方法。增加食管蠕动的方法可通过给予具有 5-HT 3 受体激动剂活性的化合物或其药学上可接受的盐、水合物或溶液。联合给药也可用于增加食管运动。