首页> 外国专利> Hexahidro - difluoro - difluoro - and ciclopentaoxacinilos hexahidro - benzooxacinilos as BACE1 inhibitors

Hexahidro - difluoro - difluoro - and ciclopentaoxacinilos hexahidro - benzooxacinilos as BACE1 inhibitors

机译:作为BACE1抑制剂的六面体-二氟-二氟-和环丙沙星六环-苯并沙星

摘要

Refers to ciclopentaoxacinilos difluoro - and difluoroenzooxacinilos Derivatives of formula (i) wherein R1, R2, R3, R4, R5, and N are as described in the present.Preferred compounds are: [3 - ((4S, 4aR, 7aR) - 2 - amino - 5.5 - difluoro - 4 - methyl - - - 4,4a 5,6,7,7a, hexahidro cyclopenta [e] [1,3] oxazin - 4-yl) phenyl] - 4 - fluoro - amide acid - 2 - 5 - but iniloxi - pyrazine carboxylic Acid - 2 - [3 - ((4S, 4aR, 7aR) - 2 - amino - 5.5 - difluoro - 4 - methyl - - - 4,4a 5,6,7,7a, hexahidro cyclopenta [e] [1,3] oxazin IL - 4 - 4 - fluoro) - phenyl] - 5 - (fluoromethyl acid amide pyrazine - 2 - carboxylic acid; among others.It also relates to pharmaceutical compositions. These compounds are BACE1 Inhibitory activity to be useful in the treatment of Alzheimer's disease
机译:指式(i)的环五氧杂环丁酸二氟-和二氟环氧杂环丁酸衍生物,其中R1,R2,R3,R4,R5和N如本发明中所述。优选的化合物为:[3-(((4S,4aR,7aR)-2 -氨基-5.5-二氟-4-甲基---4,4a 5,6,7,7a,六羟基环戊[e] [1,3]恶嗪-4-基)苯基]-4-氟-酰胺酸- 2-5-但iniloxi-吡嗪羧酸-2-[3-((4S,4aR,7aR)-2-氨基-5.5-二氟-4-甲基---4,4a 5,6,7,7a,六羟基环戊[e] [1,3]恶嗪IL-4-4-氟)-苯基]-5-(氟甲基酰胺吡嗪-2-羧酸);其中一些还涉及药物组合物。这些化合物是BACE1抑制活性可用于治疗阿尔茨海默氏病

著录项

  • 公开/公告号PE24502014A1

    专利类型

  • 公开/公告日2015-01-28

    原文格式PDF

  • 申请/专利权人 F. HOFFMANN-LA ROCHE AG.;

    申请/专利号PE20140002406

  • 发明设计人 HILPERT HANS;

    申请日2013-06-24

  • 分类号A61K31/536;A61P25/00;C07D265/12;C07D413/12;

  • 国家 PE

  • 入库时间 2022-08-21 15:13:33

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