3-cyclohexyl-2-methyl-3H-imidazo[4,5-b]pyridin-5-ol | 1217349-53-5

• 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-cyclohexyl-2-methyl-3H-imidazo[4,5-b]pyridin-5-ol
• 英文别名: 3-cyclohexyl-2-methyl-4H-imidazo[4,5-b]pyridin-5-one
• CAS: 1217349-53-5
• 化学式: C₁₃H₁₇N₃O
• 分子量: 231.297
• InChiKey: WJKZYWAHBPIEOJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.9
• 重原子数：
  17
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.54
• 拓扑面积：
  46.9
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  原乙酸三甲酯 、 5-氨基-6-(环己基氨基)吡啶-2-醇 在 三氟乙酸 acetonitrile-water 作用下， 反应 16.0h， 以to give the title compound (0.006 g)的产率得到3-cyclohexyl-2-methyl-3H-imidazo[4,5-b]pyridin-5-ol
  参考文献：
  名称：

  3H-IMIDAZO[4,5-B]PYRIDIN-5-OL DERIVATIVES USEFUL IN THE TREATMENT OF GPR81 RECEPTOR DISORDERS

  摘要：

  本发明涉及公式(Ia)的某些3H-咪唑[4,5-b]吡啶-5-醇衍生物及其药学上可接受的盐，这些化合物具有有用的药理学特性，例如作为GPR81受体的激动剂。本发明还提供了含有该发明化合物的制药组合物，以及使用该发明化合物和组合物治疗GPR81相关疾病的方法，例如血脂异常、动脉硬化、动脉粥样硬化、高血压、冠心病、中风、胰岛素抵抗、糖耐量受损、2型糖尿病、X综合征、肥胖症、牛皮癣、类风湿性关节炎、克罗恩病、移植排斥反应、多发性硬化症、全身性红斑狼疮、溃疡性结肠炎、1型糖尿病和痤疮。

  公开号：

  US20110172209A1

文献信息

• [EN] 3H-IMIDAZO[4,5-b]PYRIDIN-5-OL DERIVATIVES USEFUL IN THE TREATMENT OF GPR81 RECEPTOR DISORDERS<br/>[FR] DÉRIVÉS 3H-IMIDAZO[4,5-B]PYRIDIN-5-OL UTILES DANS LE TRAITEMENT DE TROUBLES DU RÉCEPTEUR GPR81
  申请人：ARENA PHARM INC

  公开号：WO2010030360A1

  公开（公告）日：2010-03-18

  The present invention is directed to certain 3H-imidazo[4,5-b]pyridin-5-ol derivatives of Formula (Ia) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the GPR81 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of GPR81 associated disorders, for example, dyslipidemia, atherosclerosis, atheromatous disease, hypertension, coronary heart disease, stroke, insulin resistance, impaired glucose tolerance, type 2 diabetes, syndrome X, obesity, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type 1 diabetes and acne.

  本发明涉及某些Formula（Ia）的3H-咪唑[4,5-b]吡啶-5-醇衍生物及其药学上可接受的盐，这些衍生物具有有用的药理特性，例如作为GPR81受体的激动剂。本发明还提供了含有本发明化合物的药物组合物，以及使用本发明化合物和组合物治疗GPR81相关疾病的方法，例如脂质代谢异常、动脉粥样硬化、动脉粥样病、高血压、冠心病、中风、胰岛素抵抗、糖耐量受损、2型糖尿病、X综合征、肥胖、牛皮癣、类风湿性关节炎、克罗恩病、移植排斥反应、多发性硬化症、全身性红斑狼疮、溃疡性结肠炎、1型糖尿病和痤疮。
• 3H-IMIDAZO[4,5-B]PYRIDIN-5-OL DERIVATIVES USEFUL IN THE TREATMENT OF GPR81 RECEPTOR DISORDERS
  申请人：Boatman P. Douglas

  公开号：US20110172209A1

  公开（公告）日：2011-07-14

  The present invention is directed to certain 3H-imidazo[4,5-b]pyridin-5-ol derivatives of Formula (Ia) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the GPR81 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of GPR81 associated disorders, for example, dyslipidemia, atherosclerosis, atheromatous disease, hypertension, coronary heart disease, stroke, insulin resistance, impaired glucose tolerance, type 2 diabetes, syndrome X, obesity, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type 1 diabetes and acne.

  本发明涉及公式(Ia)的某些3H-咪唑[4,5-b]吡啶-5-醇衍生物及其药学上可接受的盐，这些化合物具有有用的药理学特性，例如作为GPR81受体的激动剂。本发明还提供了含有该发明化合物的制药组合物，以及使用该发明化合物和组合物治疗GPR81相关疾病的方法，例如血脂异常、动脉硬化、动脉粥样硬化、高血压、冠心病、中风、胰岛素抵抗、糖耐量受损、2型糖尿病、X综合征、肥胖症、牛皮癣、类风湿性关节炎、克罗恩病、移植排斥反应、多发性硬化症、全身性红斑狼疮、溃疡性结肠炎、1型糖尿病和痤疮。
• US8507473B2
  申请人：——

  公开号：US8507473B2

  公开（公告）日：2013-08-13
• 3H-imidazo[4,5-b]pyridin-5-ol derivatives useful in the treatment of GPR81 receptor disorders
  申请人：Boatman P. Douglas

  公开号：US08507473B2

  公开（公告）日：2013-08-13

  The present invention is directed to certain 3H-imidazo[4,5-b]pyridin-5-ol derivatives of Formula (Ia) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the GPR81 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of GPR81 associated disorders, for example, dyslipidemia, atherosclerosis, atheromatous disease, hypertension, coronary heart disease, stroke, insulin resistance, impaired glucose tolerance, type 2 diabetes, syndrome X, obesity, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type 1 diabetes and acne.

  本发明涉及某些3H-咪唑[4,5-b]吡啶-5-醇衍生物（Ia式）及其药学上可接受的盐，这些衍生物具有有用的药理特性，例如作为GPR81受体的激动剂。本发明还提供了包含本发明化合物的药物组合物，并且提供了使用本发明化合物和组合物治疗GPR81相关疾病的方法，例如脂质代谢异常、动脉粥样硬化、动脉粥样病、高血压、冠心病、中风、胰岛素抵抗、糖耐量受损、2型糖尿病、X综合征、肥胖症、牛皮癣、类风湿性关节炎、克隆病、移植排斥反应、多发性硬化症、系统性红斑狼疮、溃疡性结肠炎、1型糖尿病和痤疮。