5-amino-6-chloro-2-methyl-N-{[1-(2-methoxy-2-methylpropyl)piperidin-4-yl]methyl}imidazo[1,2-a]pyridine-8-carboxamide | 519148-53-9

• 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: 5-amino-6-chloro-2-methyl-N-{[1-(2-methoxy-2-methylpropyl)piperidin-4-yl]methyl}imidazo[1,2-a]pyridine-8-carboxamide
• 英文别名: 5-amino-6-chloro-N-[[1-(2-methoxy-2-methylpropyl)piperidin-4-yl]methyl]-2-methylimidazo[1,2-a]pyridine-8-carboxamide
• CAS: 519148-53-9
• 化学式: C₂₀H₃₀ClN₅O₂
• 分子量: 407.944
• InChiKey: VHGFCHKOURGVER-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  28
• 可旋转键数：
  6
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.6
• 拓扑面积：
  84.9
• 氢给体数：
  2
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  5-氨基-6-氯-N-[(1-异丁基-4-哌啶基)甲基]-2-甲基咪唑并[1,2-a]吡啶-8-甲酰胺 、 5-AMINO-6-CHLORO-2-ETHYL-N-{[1-(2-METHOXY-2-METHYLPROPYL)PIPERIDIN-4-YL]METHYL}IMIDAZO[1,2-a]PYRIDINE-8-CARBOXAMIDE 生成 5-amino-6-chloro-2-methyl-N-{[1-(2-methoxy-2-methylpropyl)piperidin-4-yl]methyl}imidazo[1,2-a]pyridine-8-carboxamide
  参考文献：
  名称：

  Imidazopyridine compounds as 5-HT4 receptor agonists

  摘要：

  该发明提供了一个式（I）的化合物或其药学上可接受的盐，其中R1代表氢原子或卤素原子；R2代表甲基基团或乙基基团；R3代表分支烷基基团，其具有3至6个碳原子，或具有从1到6个碳原子的烷氧基取代的3至6个碳原子的烷基基团；但当所述R3的烷基基团的末端碳原子被所述烷氧基取代时，该烷基基团是分支烷基基团。这些化合物具有5-HT4受体结合活性，因此对哺乳动物，特别是人类的治疗胃食管反流病、非溃疡性消化不良、功能性消化不良、肠易激综合征或类似疾病具有用处。该发明还提供了包含上述化合物的制药组合物。

  公开号：

  US20040122043A1

文献信息

• Imidazopyridine compounds as 5-HT4 receptor modulators
  申请人：——

  公开号：US20030092699A1

  公开（公告）日：2003-05-15

  This invention provides a compound of the formula (I): 1 or the pharmaceutically acceptable salts thereof wherein R 1 is hydrogen, halo or alkyl; R 2 and R 3 are independently hydrogen, alkyl, alkenyl, alkynyl, aminoalkyl or hydroxyalkyl; or R 2 and R 3 taken together with the nitrogen atom to which they are attached may form hetrocyclic; R 4 is hydrogen, halo, acyl, amino, amido, aryl, arylalkyl, or heteroaryl; R 5 is hydrogen, halo, alkyl, alkenyl, alkynyl, acyl, amino, amido, aryl, arylalkyl, or heteroaryl; R 6 is hydrogen, alkyl or alkoxyalkyl; X is NR 9 wherein R 9 is hydrogen or alkyl; and Y is (CR 7 R 8 ) n wherein n is an integer from 0 to 5. These compounds have 5-HT 4 receptor binding activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, Functional dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans. This invention also provides a pharmaceutical composition comprising the above compound.

  这项发明提供了式(I)的化合物： 1 或其药学上可接受的盐，其中R 1 为氢、卤素或烷基；R 2 和R 3 独立地为氢、烷基、烯基、炔基、氨基烷基或羟基烷基；或R 2 和R 3 与它们连接的氮原子一起可能形成杂环；R 4 为氢、卤素、酰基、氨基、酰胺基、芳基、芳基烷基或杂芳基；R 5 为氢、卤素、烷基、烯基、炔基、酰基、氨基、酰胺基、芳基、芳基烷基或杂芳基；R 6 为氢、烷基或烷氧基烷基；X为NR 9 ，其中R 9 为氢或烷基；Y为(CR 7 R 8 ) n ，其中n为0至5的整数。 这些化合物具有5-HT 4 受体结合活性，因此对于哺乳动物，特别是人类的胃食管反流病、非溃疡性消化不良、功能性消化不良、肠易激综合征或类似疾病的治疗是有用的。该发明还提供了包含上述化合物的药物组合物。
• [EN] IMIDAZOPYRIDINE COMPUNDS AS 5-HT4 RECEPTOR AGONISTS<br/>[FR] COMPOSES D'IMIDAZOPYRIDINE COMME AGONISTES DU RECEPTEUR 5-HT4
  申请人：PFIZER PHARMA

  公开号：WO2004026869A1

  公开（公告）日：2004-04-01

  This invention provides a compound of the formula (I): (I) 5 wherein Rl represents a hydrogen atom or a halogen atom; R2 represents a methyl group or an ethyl group; R3 represents a branched alkyl group having from 3 to 6 carbon atoms or an alkyl group having from 3 to 6 carbon atoms substituted by an alkoxy group having from 1 to 6 carbon atoms; with the proviso that when the terminal carbon atom of said alkyl group is substituted by said alkoxy goroup, said alkyl group is a branched alkyl group; and pharmaceutically acceptable salts thereof. These compounds have 5-HT4 receptor binding activity, and thus are usefulfor the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans. This invention also provides a pharmaceutical composition comprising the above compound.

  本发明提供了式(I)的化合物，其中R1代表氢原子或卤素原子；R2代表甲基基团或乙基基团；R3代表分支烷基基团，其具有3到6个碳原子，或者是具有3到6个碳原子的烷基基团，其被1到6个碳原子的烷氧基取代；但是当所述烷基基团的末端碳原子被所述烷氧基取代时，所述烷基基团是一种分支烷基基团；以及其药学上可接受的盐。这些化合物具有5-HT4受体结合活性，因此对哺乳动物，特别是人类的胃食管反流病、非溃疡性消化不良、功能性消化不良、肠易激综合征等疾病的治疗是有用的。本发明还提供了包括上述化合物的制药组合物。
• Imidazopyridine compounds as 5-HT4 receptor agonists
  申请人：Pfizer Inc.

  公开号：US07012080B2

  公开（公告）日：2006-03-14

  This invention provides a compound of the formula (I): or a pharmaceutically acceptable salt thereof, wherein R1 represents a hydrogen atom or a halogen atom; R2 represents a methyl group or an ethyl group; R3 represents a branched alkyl group having from 3 to 6 carbon atoms or an alkyl group having from 3 to 6 carbon atoms substituted by an alkoxy group having from 1 to 6 carbon atoms; with the proviso that when the terminal carbon atom of said alkyl group of R3 is substituted by said alkoxy group, said alkyl group is a branched alkyl group. These compounds have 5-HT4 receptor binding activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans. This invention also provides a pharmaceutical composition comprising the above compound.

  本发明提供了式(I)的化合物或其药学上可接受的盐，其中R1代表氢原子或卤素原子；R2代表甲基基团或乙基基团；R3代表分支烷基基团，其具有3至6个碳原子，或者是具有3至6个碳原子的烷基基团，其被1至6个碳原子的烷氧基取代；但是当R3的烷基基团的末端碳原子被所述的烷氧基取代时，该烷基基团是分支烷基基团。这些化合物具有5-HT4受体结合活性，因此对于哺乳动物，特别是人类的治疗胃食管反流病、非溃疡性消化不良、功能性消化不良、肠易激综合征或类似疾病非常有用。本发明还提供了包含上述化合物的药物组合物。
• IMIDAZOPYRIDINE COMPOUNDS AS 5-HT 4? RECEPTOR MODULATORS
  申请人：PFIZER INC.

  公开号：EP1440071B1

  公开（公告）日：2005-10-26
• US6624162B2
  申请人：——

  公开号：US6624162B2

  公开（公告）日：2003-09-23