3-Bromo-5-methyl-imidazo[1,2-a]pyridine-2-carboxylic acid ethyl ester | 1123167-64-5

• 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: 3-Bromo-5-methyl-imidazo[1,2-a]pyridine-2-carboxylic acid ethyl ester
• 英文别名: ethyl 3-bromo-5-methylimidazo[1,2-a]pyridine-2-carboxylate
• CAS: 1123167-64-5
• 化学式: C₁₁H₁₁BrN₂O₂
• 分子量: 283.125
• InChiKey: YOGUYQICWYJXPE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.7
• 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

反应信息

• 作为反应物：
  描述：

  3-Bromo-5-methyl-imidazo[1,2-a]pyridine-2-carboxylic acid ethyl ester 在 sodium hydroxide 、 盐酸 作用下， 以 四氢呋喃 、 乙醇 、 水 为溶剂， 反应 2.0h， 生成 3-bromo-5-methylimidazo[1,2-a]pyridine-2-carboxylic acid hydrochloride
  参考文献：
  名称：

  [EN] SUBSTITUTED HETEROARYL FUSED DERIVATIVES AS PI3K INHIBITORS
  [FR] DÉRIVÉS CONDENSÉS D'HÉTÉROARYLES SUBSTITUÉS À TITRE D'INHIBITEURS DE PI3K

  摘要：

  本发明提供了公式（I）的融合衍生物，可调节磷脂酰肌醇3-激酶（PI3Ks）的活性，并在治疗与PBKs活性相关的疾病方面具有用处，例如炎症性疾病、免疫性疾病、癌症和其他疾病。

  公开号：

  WO2011075643A1
• 作为产物：
  描述：

  5-甲基咪唑[1,2-Alpha]吡啶-2-羧酸乙酯 在 N-溴代丁二酰亚胺(NBS) 作用下， 以 乙腈 为溶剂， 反应 0.5h， 以58%的产率得到3-Bromo-5-methyl-imidazo[1,2-a]pyridine-2-carboxylic acid ethyl ester
  参考文献：
  名称：

  [EN] SUBSTITUTED HETEROARYL FUSED DERIVATIVES AS PI3K INHIBITORS
  [FR] DÉRIVÉS CONDENSÉS D'HÉTÉROARYLES SUBSTITUÉS À TITRE D'INHIBITEURS DE PI3K

  摘要：

  本发明提供了公式（I）的融合衍生物，可调节磷脂酰肌醇3-激酶（PI3Ks）的活性，并在治疗与PBKs活性相关的疾病方面具有用处，例如炎症性疾病、免疫性疾病、癌症和其他疾病。

  公开号：

  WO2011075643A1

文献信息

• HETEROCYCLES AS POTASSIUM CHANNEL MODULATORS
  申请人：Christos Thomas Eugene

  公开号：US20090062290A1

  公开（公告）日：2009-03-05

  Compounds, compositions and methods are provided which are useful in the treatment of diseases through the modulation of potassium ion flux through voltage-dependent potassium channels. More particularly, the invention provides heterocycles, compositions and methods that are useful in the treatment of central or peripheral nervous system disorders (e.g., migraine, ataxia, Parkinson's disease, bipolar disorders, trigeminal neuralgia, spasticity, mood disorders, brain tumors, psychotic disorders, myokymia, seizures, epilepsy, seizure, retinal degeneration, hearing and vision loss, Alzheimer's disease, age-related memory loss, learning deficiencies, anxiety, neuronal degeneration and motor neuron diseases, maintaining bladder control or treating urinary incontinence) and as neuroprotective agents (e.g., to prevent stroke and the like) by modulating potassium channels associated with the onset or recurrence of the indicated conditions.

  提供了在通过调节电压依赖性钾通道的钾离子通量来治疗疾病方面有用的化合物、组合物和方法。更具体地，本发明提供了对中枢或外周神经系统疾病（例如偏头痛、共济失调、帕金森病、双相障碍、三叉神经痛、痉挛、情绪障碍、脑肿瘤、精神障碍、肌肉震颤、癫痫、癫痫、视网膜退行性疾病、听力和视力丧失、阿尔茨海默病、与年龄相关的记忆丧失、学习缺陷、焦虑、神经元退化和运动神经元疾病、维持膀胱控制或治疗尿失禁）有用的杂环、组合物和方法，以及作为神经保护剂（例如通过调节与所述疾况的发作或复发相关的钾通道）（例如预防中风等）的方法。
• [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。
• Heterocycles as potassium channel modulators
  申请人：Icagen, Inc.

  公开号：US08058274B2

  公开（公告）日：2011-11-15

  Compounds, compositions and methods are provided which are useful in the treatment of diseases through the modulation of potassium ion flux through voltage-dependent potassium channels. More particularly, the invention provides heterocycles, compositions and methods that are useful in the treatment of central or peripheral nervous system disorders (e.g., migraine, ataxia, Parkinson's disease, bipolar disorders, trigeminal neuralgia, spasticity, mood disorders, brain tumors, psychotic disorders, myokymia, seizures, epilepsy, seizure, retinal degeneration, hearing and vision loss, Alzheimer's disease, age-related memory loss, learning deficiencies, anxiety, neuronal degeneration and motor neuron diseases, maintaining bladder control or treating urinary incontinence) and as neuroprotective agents (e.g., to prevent stroke and the like) by modulating potassium channels associated with the onset or recurrence of the indicated conditions.

  本发明提供了用于治疗疾病的化合物、组合物和方法，通过调节电压依赖性钾通道中的钾离子通量。特别地，本发明提供了杂环、组合物和方法，用于治疗中枢或外周神经系统疾病（例如偏头痛、共济失调、帕金森病、双相情感障碍、三叉神经痛、痉挛、情绪障碍、脑肿瘤、精神障碍、肌纤维颤搐、癫痫、癫痫、视网膜退化、听力和视力损失、阿尔茨海默病、年龄相关的记忆丧失、学习缺陷、焦虑、神经退行性和运动神经元疾病、维持膀胱控制或治疗尿失禁），并作为神经保护剂（例如预防中风等），通过调节与所述条件的发生或复发有关的钾通道。
• SUBSTITUTED HETEROARYL FUSED DERIVATIVES AS PI3K INHIBITORS
  申请人：Combs Andrew P.

  公开号：US20110190319A1

  公开（公告）日：2011-08-04

  The present invention provides fused derivatives of Formula I: that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.

  本发明提供了公式I的融合衍生物，其调节磷脂酰肌醇3-激酶（PI3Ks）的活性，并且在治疗与PI3Ks活性相关的疾病方面具有用途，例如，炎症性疾病、免疫相关疾病、癌症和其他疾病。
• Heterocycles As Potassium Channel Modulators
  申请人：Icagen Inc.

  公开号：US20130143889A1

  公开（公告）日：2013-06-06

  Compounds, compositions and methods are provided which are useful in the treatment of diseases through the modulation of potassium ion flux through voltage-dependent potassium channels. More particularly, the invention provides heterocycles, compositions and methods that are useful in the treatment of central or peripheral nervous system disorders (e.g., migraine, ataxia, Parkinson's disease, bipolar disorders, trigeminal neuralgia, spasticity, mood disorders, brain tumors, psychotic disorders, myokymia, seizures, epilepsy, seizure, retinal degeneration, hearing and vision loss, Alzheimer's disease, age-10 related memory loss, learning deficiencies, anxiety, neuronal degeneration and motor neuron diseases, maintaining bladder control or treating urinary incontinence) and as neuroprotective agents (e.g., to prevent stroke and the like) by modulating potassium channels associated with the onset or recurrence of the indicated conditions.

  本发明提供了一些化合物、组合物和方法，通过调节电压依赖性钾通道中的钾离子通量，对治疗疾病有用。更具体地，本发明提供了杂环化合物、组合物和方法，对治疗中枢或外周神经系统疾病（例如偏头痛、共济失调、帕金森病、双相障碍、三叉神经痛、痉挛、情绪障碍、脑肿瘤、精神疾病、肌颤、癫痫、抽搐、视网膜退化、听力和视力丧失、阿尔茨海默病、与年龄相关的记忆丧失、学习障碍、焦虑、神经退行性和运动神经疾病、维持膀胱控制或治疗尿失禁）以及作为神经保护剂（例如预防中风等）具有用处，通过调节与所述疾病的发生或复发有关的钾通道。