公开(公告)号：US09611275B2

公开(公告)日：2017-04-04

申请号：US14399146

申请日：2013-05-03

Applicant: Merck Sharp & Dohme Corp.

Inventor： Harold G. Selnick ,  Wenping Li ,  Eric Hostetler ,  Kun Liu ,  Ernest J. McEachern ,  Yuanxi Zhou ,  Zhongyong Wei ,  Changwei Mu ,  Yaode Wang ,  Jiang Chang

IPC: C07D513/04 ,  C07B59/00 ,  C07H9/06

CPC classification number: C07D513/04 ,  C07B59/005 ,  C07B2200/05 ,  C07H9/06

Abstract: The present invention is directed to compounds and pharmaceutical formulations comprising these compounds which are useful as O-linked N-acetylglucosaminidase (O-GlcNAcase) inhibitors, and thus may be useful for the treatment of certain disorders such as Alzheimer's disease including reducing NFTs and/or hyperphosphorylated tau. The invention is also directed to use of the compounds as O-GlcNAcase imaging agents.

公开(公告)号：US20150152127A1

公开(公告)日：2015-06-04

申请号：US14399146

申请日：2013-05-03

Applicant: Merck Sharp & Dohme Corp.

Inventor： Harold G. Selnick ,  Wenping Li ,  Eric Hostetler ,  Kun Liu ,  Ernest J. McEachern ,  Yuanxi Zhou ,  Zhongyong Wei ,  Changwei Mu ,  Yaode Wang ,  Jiang Chang

IPC: C07H9/06 ,  C07B59/00

CPC classification number: C07D513/04 ,  C07B59/005 ,  C07B2200/05 ,  C07H9/06

Abstract: The present invention is directed to compounds and pharmaceutical formulations comprising these compounds which are useful as O-linked N-acetylglucosaminidase (O-GlcNAcase) inhibitors, and thus may be useful for the treatment of certain disorders such as Alzheimer's disease including reducing NFTs and/or hyperphosphorylated tau. The invention is also directed to use of the compounds as O-GlcNAcase imaging agents.

Abstract translation: 本发明涉及包含这些化合物的化合物和药物制剂，其可用作O-连接的N-乙酰氨基葡糖苷酶（O-GlcNAcase）抑制剂，因此可用于治疗某些疾病，例如阿尔茨海默病，包括减少NFTs和/ 或超磷酸化tau。 本发明还涉及将化合物用作O-GlcNAcase显像剂。