2-(2-chloro-phenyl)-1-{4-[4-(3,4-dihydro-2H-quinoline-1-carbonyl)-thiazol-2-yl]-piperidin-1-yl}-ethanone | 870476-99-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 英文名称: 2-(2-chloro-phenyl)-1-{4-[4-(3,4-dihydro-2H-quinoline-1-carbonyl)-thiazol-2-yl]-piperidin-1-yl}-ethanone
• 英文别名: 2-(2-chlorophenyl)-1-[4-[4-(3,4-dihydro-2H-quinoline-1-carbonyl)-1,3-thiazol-2-yl]piperidin-1-yl]ethanone
• CAS: 870476-99-6
• 化学式: C₂₆H₂₆ClN₃O₂S
• 分子量: 480.03
• InChiKey: ZLJDFWOXKCVPNS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5
• 重原子数：
  33
• 可旋转键数：
  4
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.35
• 拓扑面积：
  81.8
• 氢给体数：
  0
• 氢受体数：
  4

文献信息

• Human G protein-coupled receptor and modulators thereof for the treatment of hyperglycemia and related disorders
  申请人：Qiu Jun

  公开号：US20070231263A1

  公开（公告）日：2007-10-04

  The present invention relates to methods of identifying whether one or more candidate compounds is a modulator of a G protein-coupled receptor (GPCR) or a modulator of blood glucose concentration. In certain embodiments, the GPCR is human. The present invention also relates to methods of using a modulator of the GPCR. A preferred modulator is agonist. Agonists of the invention are useful as therapeutic agents for lowering blood glucose concentration, for preventing or treating certain metabolic disorders, such as insulin resistance, impaired glucose tolerance, and diabetes, and for preventing or treating a complication of an elevated blood glucose concentration, such as atherosclerosis, heart disease, stroke, hypertension and peripheral vascular disease.

  本发明涉及一种识别一个或多个候选化合物是否为G蛋白偶联受体（GPCR）的调节剂或血糖浓度的调节剂的方法。在某些实施例中，该GPCR为人类。本发明还涉及使用GPCR的调节剂的方法。首选的调节剂是激动剂。本发明的激动剂可用作治疗剂，用于降低血糖浓度，预防或治疗某些代谢性疾病，如胰岛素抵抗、糖耐量受损和糖尿病，以及预防或治疗血糖浓度升高的并发症，如动脉粥样硬化、心脏病、中风、高血压和外周血管疾病。
• Human G Protein-Coupled Receptor and Modulators Thereof for the Treatment of Hyperglycemia and Related Disorders
  申请人：Qiu Jun

  公开号：US20080306114A1

  公开（公告）日：2008-12-11

  The present invention relates to methods of identifying whether one or more candidate compounds is a modulator of a G protein-coupled receptor (GPCR) or a modulator of blood glucose concentration. In certain embodiments, the GPCR is human. The present invention also relates to methods of using a modulator of the GPCR. A preferred modulator is agonist. Agonists of the invention are useful as therapeutic agents for lowering blood glucose concentration, for preventing or treating certain metabolic disorders, such as insulin resistance, impaired glucose tolerance, and diabetes, and for preventing or treating a complication of an elevated blood glucose concentration, such as atherosclerosis, heart disease, stroke, hypertension and peripheral vascular disease.

  本发明涉及一种识别一个或多个候选化合物是否为G蛋白偶联受体（GPCR）调节剂或血糖浓度调节剂的方法。在某些实施例中，GPCR是人类的。本发明还涉及使用GPCR调节剂的方法。首选的调节剂是激动剂。本发明的激动剂可用作降低血糖浓度的治疗剂，用于预防或治疗某些代谢性疾病，如胰岛素抵抗、糖耐量受损和糖尿病，以及预防或治疗血糖浓度升高的并发症，如动脉粥样硬化、心脏病、中风、高血压和周围血管疾病。