8-溴-5-甲基咪唑并[1,2-A]砒啶-2-羧酸乙酯 | 135995-45-8

• 物质功能分类: 医药中间体 - 杂环化合物 - 吡啶类化合物
• 分子结构分类: 有机化合物 - 有机杂环化合物 - 咪唑并吡啶类
• 中文名称: 8-溴-5-甲基咪唑并[1,2-A]砒啶-2-羧酸乙酯
• 中文别名: 8-溴-5-甲基咪唑并[1,2-A]吡啶-2-羧酸乙酯
• 英文名称: Ethyl 8-bromo-5-methylimidazo[1,2-a]pyridine-2-carboxylate
• CAS: 135995-45-8
• 化学式: C₁₁H₁₁BrN₂O₂
• 分子量: 283.12
• InChiKey: MCVBSXMGJRXQSJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.4
• 重原子数：
  16
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.27
• 拓扑面积：
  43.6
• 氢给体数：
  0
• 氢受体数：
  3

安全信息

• 危险性防范说明：
  P233,P260,P261,P264,P270,P271,P280,P301+P312,P302+P352,P304,P304+P340,P305+P351+P338,P312,P321,P330,P332+P313,P337+P313,P340,P362,P403,P403+P233,P405,P501
• 危险性描述：
  H302,H315,H319,H335

文献信息

• [EN] SUBSTITUTED IMIDAZO[1,2-A]PYRIDINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE AS ß-SECRETASE INHIBITORS<br/>[FR] DÉRIVÉS IMIDAZO[1,2-A]PYRIDINE SUBSTITUÉS, COMPOSITIONS PHARMACEUTIQUES, ET PROCÉDÉS D'UTILISATION COMME INHIBITEURS DE LA ?-SÉCRÉTASE
  申请人：HIGH POINT PHARMACEUTICALS LLC

  公开号：WO2010126745A1

  公开（公告）日：2010-11-04

  The present invention is directed to substituted imidazo[1,2-a]pyridine derivatives, pharmaceutically acceptable salts thereof, and tautomers of such compounds or salts, that inhibit β-site amyloid precursor protein-cleaving enzyme (BACE) and that may be useful in the treatment of diseases in which BACE is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which BACE is involved.

  本发明涉及替代咪唑[1,2-a]吡啶衍生物，其药学上可接受的盐，以及这些化合物或盐的互变异构体，其抑制β-淀粉样前体蛋白裂解酶（BACE）并且可能在治疗涉及BACE的疾病，如阿尔茨海默病中有用。该发明还涉及包含这些化合物的药物组合物以及在治疗涉及BACE的这类疾病中使用这些化合物和组合物。
• Imidazo[1,2-a]pyridinylalkyl compounds for treatment of neurotoxic injury
  申请人：G.D. Searle & Co.

  公开号：EP0436831A2

  公开（公告）日：1991-07-17

  A class of imidazo[1,2-a]pyridinylalkyl compounds is described for treatment to reduce neurotoxic injury associated with anoxia or ischemia which typically follows stroke, cardiac arrest or perinatal asphyxia. The treatment includes administration of a compound of this class alone or in a composition in an amount effective as an antagonist to inhibit excitotoxic actions at major neuronal excitatory amino acid receptor sites. Compounds of most interest are those of the formula: wherein each of R22, R23 and R24 is independently selected from hydrido, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl and cycloheptyl; wherein each of Ym and Yn is a spacer group independently selected methylene and ethylene radicals which may be unsubstituted and from methylene radicals which may be substituted with a group selected from halo, hydroxy and oxo; wherein each of m and n is a number independently selected from zero to two, inclusive; wherein each X and T is one or more groups independently selected from hydrido, alkyl, cycloalkyl, halo, haloalkyl, hydroxy, hydroxyalkyl, alkoxy, alkoxyalkyl and alkanoyl; or a pharmaceutically-acceptable salt thereof.

  描述了一类咪唑并[1,2-a]吡啶烷基化合物，用于治疗减少与缺氧或缺血相关的神经毒性损伤，这种损伤通常发生在中风、心脏骤停或围产期窒息之后。治疗方法包括单独施用或在组合物中施用该类化合物，施用量为有效的拮抗剂，以抑制主要神经元兴奋性氨基酸受体部位的兴奋毒性作用。最令人感兴趣的化合物是式中的化合物： 其中 R22、R23 和 R24 各自独立地选自肼、甲基、乙基、正丙基、异丙基、正丁基、异丁基、仲丁基、叔丁基、环丙基、环丁基、环戊基、环己基和环庚基；其中 Ym 和 Yn 各自是一个间隔基团，该间隔基团独立地选自可能未被取代的亚甲基和亚乙基，以及可能被选自卤代、羟基和氧代的基团取代的亚甲基；其中每个 m 和 n 是独立选自 0 至 2（包括 2）的数字；其中每个 X 和 T 是一个或多个独立选自氢基、烷基、环烷基、卤基、卤代烷基、羟基、羟基烷基、烷氧基、烷氧基烷基和烷酰基的基团；或其药学上可接受的盐。
• SUBSTITUTED IMIDAZO[1,2-A]PYRIDINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE AS -SECRETASE INHIBITORS
  申请人：High Point Pharmaceuticals, LLC

  公开号：EP2424866A1

  公开（公告）日：2012-03-07
• US5716964A
  申请人：——

  公开号：US5716964A

  公开（公告）日：1998-02-10