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Development of 2-Aminooxazoline 3-Azaxanthenes as Orally Active-Secretase Inhibitors for the Treatment of Alzheimer’s Disease

Jian Jeffrey ChenQingyian LiuChester YuanVijay GorePatricia LopezVu MaAlbert AmegadzieWenyuan QianTed JuddAna Elena MinattiJim BrownYuan ChengMay XueWenge ZhongThomas A.DineenOleg EpsteinJason HumanChuck KreimanIsaac MarxMatt WeissTimothy S.PowersStephen A.HitchcockRobert C.WahlPaul A.WenDouglas A.WhittingtonAlan C.ChengMike BartbergerDean HickmanBob DunnStephen WoodRobert T.Fremeau JrRyan WhiteVinod F.Patel

Amgen Inc.

摘要:The site amyloid precursor protein cleaving enzyme 1(BACE1) is a 501 amino acid aspartic protease first discovered in 1999.It is the rate-limiting enzyme for the formation of A peptides.Studies over the last decade have suggested that one of the main causes of Alzheimer’s disease(AD) is the accumulation,oliomerization,and aggregation of amyloid peptides(A) of 38-43 amino acids.BACE1 has therefore been extensively investigated as a therapeutic target for the development of disease modifying agents for AD.There are significant challenges in identifying potent,orally active and brain penetrating BACE1 inhibitors.In this talk we will discuss the lead identification and optimization of 2-aminooxazine 3-azaxanthenes as potent BACE1 inhibitors.The lead compound significantly reduced CSF and brain A levels in both rat and non-human primate pharmacodynamic model.
会议名称:

2014第十二届国际新药发明年会——2014第四届药物递放系统研讨会,2014第五届国际药物化学大会

会议时间:

2014-11-18

会议地点:

中国江苏苏州

  • 专辑:

    医药卫生科技

  • 专题:

    药学

  • 分类号:

    R914

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