LY377770 | 160126-61-4

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: LY377770
• 英文别名: 3S,4AR,6S,8AR-6-((((1H-tetrazole-5-yl)methyl)oxy)methyl)-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline-3-carboxylic acid；6-((((1H-Tetrazol-5-yl)methyl)oxy)methyl)-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline-3-carboxylic acid；(3S,4aR,6S,8aR)-6-(2H-tetrazol-5-ylmethoxymethyl)-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline-3-carboxylic acid
• CAS: 160126-61-4
• 化学式: C₁₃H₂₁N₅O₃
• 分子量: 295.341
• InChiKey: BLZIYDWBKOOBIK-MMWGEVLESA-N

物化性质

• 沸点：
  534.9±58.0 °C(Predicted)
• 密度：
  1.287±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  -2.2
• 重原子数：
  21
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.85
• 拓扑面积：
  113
• 氢给体数：
  3
• 氢受体数：
  7

制备方法与用途

LY294486是一种具有生物活性的化学物质。

反应信息

• 作为产物：
  描述：

  三正丁基叠氮化锡 、 Ethyl 3S,4aR,6S,8aR 6-(((Cyanomethyl)oxy)methyl)-2-methoxycarbonyl-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline-3-carboxylate 生成 LY377770
  参考文献：
  名称：

  摘要：

  DOI：

文献信息

• Sulfide and disulfide compounds and compositions for cholesterol management and related uses
  申请人：Dasseux Henri Jean-Louis

  公开号：US20050020694A1

  公开（公告）日：2005-01-27

  The invention encompasses novel sulfide and disulfide compounds, compositions comprising sulfide and disulfide compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising an ether compound. The compounds, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's Disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatitis, hypertension, renal disease, cancer, inflammation, and impotence. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.

  本发明涵盖了新型硫化物和二硫化物化合物，包含硫化物和二硫化物化合物的组合物，以及使用含有醚化合物的组合物进行治疗和预防心血管疾病、脂质代谢异常、蛋白质异常和葡萄糖代谢紊乱的方法。本发明的化合物、组合物和方法还可用于治疗和预防阿尔茨海默病、X综合征、过氧化物酶体增殖物激活受体相关疾病、败血症、血栓性疾病、肥胖症、胰腺炎、高血压、肾脏疾病、癌症、炎症和阳痿。在某些实施例中，本发明的化合物、组合物和方法与其他治疗剂如降胆固醇和降血糖药物联合治疗非常有效。
• Methods of treating neurological disorders with group I mGluR antagonists
  申请人：——

  公开号：US20030100539A1

  公开（公告）日：2003-05-29

  Compositions and uses of mGluR5 antagonists for the treatment and prevention of neurological disorders, such as Fragile X, autism, mental retardation, schizophrenia and Down's Syndrome, are disclosed.

  本研究公开了用于治疗和预防神经系统疾病（如脆性 X、自闭症、智力迟钝、精神分裂症和唐氏综合症）的 mGluR5 拮抗剂的组成和用途。
• Selective iGluR5 receptor antagonists
  申请人：——

  公开号：US20040192722A1

  公开（公告）日：2004-09-30

  The present invention provides a method of treating or preventing migraine comprising administering to a patient in need thereof an effective amount of a selective iGluR 5 receptor antagonist. The present invention further provides novel compounds functional as selective iGluR 5 receptor antagonists as well as compositions and formulations comprising said selective iGluR 5 receptor antagonists.

  本发明提供了一种治疗或预防偏头痛的方法，包括向有需要的患者施用有效量的选择性 iGluR 5 受体拮抗剂。本发明进一步提供了具有选择性 iGluR 5 受体拮抗剂的新型化合物以及包含所述选择性 iGluR 5 受体拮抗剂的组合物和制剂。
• Methods of treating disorders with group I mGluR antagonists
  申请人：Bear F. Mark

  公开号：US20050171067A1

  公开（公告）日：2005-08-04

  mGluR5 antagonists are used for the treatment and prevention of disorders, including Fragile X, autism, mental retardation, schizophrenia and Down's Syndrome. The methods of the invention can be used to treat epilepsy and anxiety in a human having Fragile X syndrome, autism, mental retardation, schizophrenia and Down's Syndrome.

  mGluR5 拮抗剂可用于治疗和预防各种疾病，包括脆性 X、自闭症、智力迟钝、精神分裂症和唐氏综合症。本发明的方法可用于治疗脆性 X 综合征、自闭症、智力迟钝、精神分裂症和唐氏综合征患者的癫痫和焦虑。
• SELECTIVE iGluR 5? RECEPTOR ANTAGONISTS FOR THE TREATMENT OF MIGRAINE
  申请人：ELI LILLY AND COMPANY

  公开号：EP1200073B1

  公开（公告）日：2007-01-10