公开(公告)号：EP3233834A1

公开(公告)日：2017-10-25

申请号：EP15820456.0

申请日：2015-12-16

申请人： Janssen Pharmaceutica, N.V.

发明人： TRABANCO-SUÁREZ, Andrés, Avelino ,  DELGADO-GONZÁLEZ, Óscar ,  GIJSEN, Henricus, Jacobus, Maria ,  VAN GOOL, Michiel, Luc, Maria ,  VAN BRANDT, Sven, Franciscus, Anna ,  DE CLEYN, Michel, Anna, Jozef ,  FUSTERO LARDIÉS, Santos ,  MATEU SANCHÍS, Natalia

IPC分类号： C07D403/12 ,  C07D401/10 ,  C07D401/12 ,  C07D403/10 ,  C07D413/12 ,  A61K31/506 ,  A61P25/28

摘要： wherein the radicals are as defined in the specification. 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 associated with beta-amyloid, age-related macular degeneration, type 2 diabetes or metabolic disorders.

摘要翻译： 本发明涉及具有式（I）所示结构的β-分泌酶的2,3,4,5-四氢吡啶-6-胺和3,4-二氢-2H-吡咯-5-胺化合物抑制剂，其中 基团如说明书中所定义。 本发明还涉及包含此类化合物的药物组合物，涉及用于制备此类化合物和组合物的方法，并且涉及此类化合物和组合物用于预防和治疗涉及β-分泌酶的疾病如阿尔茨海默病（ AD），轻度认知障碍，衰老，痴呆，路易体痴呆，唐氏综合症，与中风相关的痴呆，与帕金森病相关的痴呆，与β-淀粉样蛋白相关的痴呆，年龄相关性黄斑变性，2型糖尿病或代谢紊乱。