rac-[1-(5-bromo-2,4-difluoro-phenyl)-1-methyl-2-methylamino-ethyl]-carbamic acid tert-butyl ester | 1353759-81-5

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯酚醚
• 英文名称: rac-[1-(5-bromo-2,4-difluoro-phenyl)-1-methyl-2-methylamino-ethyl]-carbamic acid tert-butyl ester
• 英文别名: tert-butyl N-[2-(5-bromo-2,4-difluorophenyl)-1-(methylamino)propan-2-yl]carbamate
• CAS: 1353759-81-5
• 化学式: C₁₅H₂₁BrF₂N₂O₂
• 分子量: 379.245
• InChiKey: DNFQEQPSGXROJG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  22
• 可旋转键数：
  6
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.53
• 拓扑面积：
  50.4
• 氢给体数：
  2
• 氢受体数：
  5

文献信息

• [EN] 3-AMINO-5,6-DIHYDRO-1H-PYRAZIN-2-ONE DERIVATIVES USEFUL FOR THE TREATEMENT OF ALZHEIMER'S DISEASE AND OTHER FORMS OF DEMENTIA<br/>[FR] DÉRIVÉS DE 3-AMINO-5,6-DIHYDRO-1H-PYRAZIN-2-ONE UTILES POUR LE TRAITEMENT DE LA MALADIE D'ALZHEIMER ET D'AUTRES FORMES DE DÉMENCE
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：WO2012000933A1

  公开（公告）日：2012-01-05

  The present invention relates to novel 3-amino-5,6-dihydro-1H-pyrazin-2-one derivatives as inhibitors of beta-secretase, also known as beta-site amyloid cleaving enzyme, BACE, BACE1, Asp2, or memapsin2. 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 or dementia associated with beta- amyloid.

  本发明涉及作为β-分泌酶抑制剂的新型3-氨基-5,6-二氢-1H-吡嗪-2-酮衍生物，β-分泌酶也称为β-位点淀粉样蛋白裂解酶、BACE、BACE1、Asp2或memapsin2。该发明还涉及包含这些化合物的药物组合物，用于制备这些化合物和组合物的方法，以及用于预防和治疗涉及β-分泌酶的疾病的这些化合物和组合物的用途，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或与β-淀粉样蛋白相关的痴呆。
• 3-AMINO-5,6-DIHYDRO-1H-PYRAZIN-2-ONE DERIVATIVES USEFUL FOR THE TREATMENT OF ALZHEIMER'S DISEASE AND OTHER FORMS OF DEMENTIA
  申请人：Delgado-Jiménez Francisca

  公开号：US20130102618A1

  公开（公告）日：2013-04-25

  The present invention relates to novel 3-amino-5,6-dihydro-1H-pyrazin-2-one derivatives as inhibitors of beta-secretase, also known as beta-site amyloid cleaving enzyme, BACE, BACE1, Asp2, or memapsin2. 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 or dementia associated with beta-amyloid.

  本发明涉及新型3-氨基-5,6-二氢-1H-吡嗪-2-酮衍生物，作为β-分泌酶抑制剂，也被称为β-位点淀粉样蛋白裂解酶、BACE、BACE1、Asp2或memapsin2。该发明还涉及包含这种化合物的药物组合物，用于制备这种化合物和组合物的方法，以及用于预防和治疗涉及β-分泌酶的疾病的这种化合物和组合物的用途，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或与β-淀粉样蛋白相关的痴呆。
• 3-AMINO-5,6-DIHYDRO-1H-PYRAZIN-2-ONE DERIVATIVES USEFUL FOR THE TREATEMENT OF ALZHEIMER'S DISEASE AND OTHER FORMS OF DEMENTIA
  申请人：Janssen Pharmaceutica, N.V.

  公开号：EP2585440A1

  公开（公告）日：2013-05-01