(9ci)-4-乙基-1H-咪唑-4,5-二羧酸-5-甲酯 | 312758-84-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 中文名称: (9ci)-4-乙基-1H-咪唑-4,5-二羧酸-5-甲酯
• 英文名称: 4-O-ethyl 5-O-methyl 1H-imidazole-4,5-dicarboxylate
• CAS: 312758-84-2
• 化学式: C₈H₁₀N₂O₄
• 分子量: 198.18
• InChiKey: CIOAKZIBAGYGSB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.8
• 重原子数：
  14
• 可旋转键数：
  5
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  81.3
• 氢给体数：
  1
• 氢受体数：
  5

文献信息

• [EN] 4-AMINO-6-PHENYL-5,6-DIHYDROIMIDAZO[1,5-A]PYRAZIN-3(2H)-ONE DERIVATIVES AS INHIBITORS OF BETA-SECRETASE (BACE)<br/>[FR] DÉRIVÉS DE 4-AMINO-6-PHÉNYL-5,6-DIHYDRO-IMIDAZO[1,5-A]PYRAZIN-3(2H)-ONE UTILISÉS COMME INHIBITEURS DE LA BÊTA-SÉCRÉTASE (BACE)
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：WO2014198851A1

  公开（公告）日：2014-12-18

  The present invention relates to novel 5,6-dihydroimidazo[1,5-a]pyrazin-3(2H)-one derivatives as inhibitors of beta-secretase, also known as beta-site amyloid cleaving enzyme, BACE, in particular BACE1 and/or BACE2 (wherein BACE1, is also known as Asp2, or memapsin2 and BACE2 is also known as Asp1, Memapsin 1 or DRAP). The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which beta-secretase is involved, such as Alzheimer's disease (AD), mild cognitive impairment, senility, dementia, dementia with Lewy bodies, Down's syndrome, dementia associated with stroke, dementia associated with Parkinson's disease, dementia of the Alzheimer's type, dementia associated with beta-amyloid, age-related macular degeneration, type 2 diabetes and other metabolic disorders.

  本发明涉及一种新型的5,6-二氢咪唑并[1,5-a]吡嗪-3(2H)-酮衍生物，作为β-分泌酶抑制剂，也称为β-位点淀粉样蛋白裂解酶，BACE，特别是BACE1和/或BACE2（其中BACE1也称为Asp2，或memapsin2，BACE2也称为Asp1，Memapsin 1或DRAP）。该发明还涉及包含这些化合物的药物组合物，制备这些化合物和组合物的方法，以及利用这些化合物和组合物预防和治疗涉及β-分泌酶的疾病，如阿尔茨海默病（AD），轻度认知障碍，老年痴呆，带有Lewy小体的痴呆，唐氏综合征，与中风相关的痴呆，与帕金森病相关的痴呆，阿尔茨海默型痴呆，与β-淀粉样蛋白相关的痴呆，年龄相关性黄斑变性，2型糖尿病和其他代谢性疾病的治疗。
• 4-AMINO-6-PHENYL-5,6-DIHYDROIMIDAZO[1,5-A]PYRAZIN-3(2H)-ONE DERIVATIVES AS INHIBITORS OF BETA-SECRETASE (BACE)
  申请人：Janssen Pharmaceutica N.V.

  公开号：EP3008067A1

  公开（公告）日：2016-04-20