公开(公告)号：US09938299B2

公开(公告)日：2018-04-10

申请号：US14655222

申请日：2013-12-20

申请人： MERCK SHARP & DOHME CORP. ,  ALECTOS THERAPEUTICS, INC.

发明人： Harold G. Selnick ,  Kun Liu ,  Ernest J. McEachern ,  Ramesh Kaul ,  Zhongyong Wei ,  Yaode Wang ,  Jiang Chang

IPC分类号： C07D513/04 ,  B65D71/14 ,  B65D71/16 ,  B65D5/00 ,  B65D5/20

CPC分类号： C07D513/04 ,  B65D5/005 ,  B65D5/2057 ,  B65D71/14 ,  B65D71/16 ,  B65D2571/0016 ,  B65D2571/0029 ,  B65D2571/0066 ,  B65D2571/00716

摘要： The invention provides compounds with enhanced permeability for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.

公开(公告)号：US09611275B2

公开(公告)日：2017-04-04

申请号：US14399146

申请日：2013-05-03

申请人： Merck Sharp & Dohme Corp.

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

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

CPC分类号： C07D513/04 ,  C07B59/005 ,  C07B2200/05 ,  C07H9/06

摘要： 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

申请人： Merck Sharp & Dohme Corp.

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

IPC分类号： C07H9/06 ,  C07B59/00

CPC分类号： C07D513/04 ,  C07B59/005 ,  C07B2200/05 ,  C07H9/06

摘要： 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.

摘要翻译： 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。