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公开(公告)号：US09695197B2
公开(公告)日：2017-07-04
申请号：US14439790
申请日：2013-10-30
Applicant: Alectos Therapeutics Inc. , Merck Sharp & Dohme Corp.
Inventor： Ramesh Kaul , Ernest J. McEachern , David J. Vocadlo , Yuanxi Zhou , Qun Dang , Harold G. Selnick
IPC: C07D498/04 , C07D513/04 , C07H9/06
CPC classification number: C07D513/04 , C07D498/04 , C07H9/06
Abstract: 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.
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公开(公告)号：US20150218147A1
公开(公告)日：2015-08-06
申请号：US14424615
申请日：2013-08-29
Applicant: Alectos Therapeutics Inc. , Merck Sharp & Dohme Corp.
Inventor： Ernest J. McEachern , Jianyu Sun , David J. Vocadlo , Yuanxi Zhou , Harold G. Selnick
IPC: C07D417/06 , C07D401/08 , C07D207/14
CPC classification number: C07D417/06 , C07D207/14 , C07D401/06 , C07D401/08
Abstract: The invention provides compounds for 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.
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公开(公告)号：US20220213058A1
公开(公告)日：2022-07-07
申请号：US17594834
申请日：2020-05-07
Applicant: ALECTOS THERAPEUTICS INC.
Inventor： Ramesh KAUL , Ernest J. MCEACHERN , Jianyu SUN , David J. VOCADLO , Yuanxi ZHOU , Yongbao ZHU
IPC: C07D401/06 , C07D211/46 , C07D405/06 , C07D405/10 , C07D409/06 , C07D401/14 , C07D211/32 , C07D409/14 , C07D417/14 , C07D413/14
Abstract: The invention provides compounds for inhibiting glucosylceramidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds.
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公开(公告)号：US20170107180A1
公开(公告)日：2017-04-20
申请号：US15383705
申请日：2016-12-19
Applicant: Alectos Therapeutics Inc. , Merck Sharp & Dohme Corp.
Inventor： Ernest J. MCEACHERN , David J. VOCADLO , Yuanxi ZHOU , Harold G. SELNICK
IPC: C07D211/60
CPC classification number: C07D211/60
Abstract: The invention provides compounds for 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.
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公开(公告)号：US20170029379A1
公开(公告)日：2017-02-02
申请号：US15107269
申请日：2014-12-22
Applicant: Alectos Therapeutics Inc.
Inventor： Ramesh KAUL , Ernest J. MCEACHERN , Jianyu SUN , David J. VOCADLO , Yuanxi ZHOU , Yongbao ZHU
IPC: C07D221/20
CPC classification number: C07D221/20
Abstract: The invention provides isofogamine analogs of structural formula (I) below that modulate and stabilize glucocerebrosidases and enhance their enzymatic activity in vivo. Such compounds, prodrugs and compositions thereof are useful in treating synucleinopathy, lysosomal storage disease and relevant neurodegenerative disease.
Abstract translation: 本发明提供下述结构式（I）的异佛胺类似物，其调节和稳定葡糖脑苷脂酶并增强其在体内的酶活性。 这些化合物，前药及其组合物可用于治疗突触核蛋白病，溶酶体贮积病和相关的神经变性疾病。
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Patent Agency Ranking
公开(公告)号：US09938299B2
公开(公告)日：2018-04-10
申请号：US14655222
申请日：2013-12-20
Applicant: MERCK SHARP & DOHME CORP. , ALECTOS THERAPEUTICS, INC.
Inventor： Harold G. Selnick , Kun Liu , Ernest J. McEachern , Ramesh Kaul , Zhongyong Wei , Yaode Wang , Jiang Chang
IPC: C07D513/04 , B65D71/14 , B65D71/16 , B65D5/00 , B65D5/20
CPC classification number: C07D513/04 , B65D5/005 , B65D5/2057 , B65D71/14 , B65D71/16 , B65D2571/0016 , B65D2571/0029 , B65D2571/0066 , B65D2571/00716
Abstract: 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.
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公开(公告)号：US20180009761A1
公开(公告)日：2018-01-11
申请号：US15711301
申请日：2017-09-21
Applicant: Alectos Therapeutics Inc.
Inventor： Ramesh KAUL , Ernest J. MCEACHERN , Jianyu SUN , David J. VOCADLO , Yuanxi ZHOU , Yongbao ZHU
IPC: C07D221/20
CPC classification number: C07D221/20
Abstract: The invention provides compounds for modulating glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds.
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公开(公告)号：US09815861B2
公开(公告)日：2017-11-14
申请号：US14966221
申请日：2015-12-11
Applicant: Alectos Therapeutics Inc. , Merck Sharp & Dohme Corp.
Inventor： Ramesh Kaul , Ernest J. McEachern , Changwei Mu , Harold G. Selnick , David J. Vocadlo , Yaode Wang , Zhongyong Wei , Yuanxi Zhou , Yongbao Zhu
IPC: C07H9/06 , C07H9/00 , C07D513/04 , C12Q1/34 , C07H17/00
CPC classification number: C07H9/06 , C07D513/04 , C07H9/00 , C07H17/00 , C12Q1/34 , G01N2333/924 , G01N2500/04 , G01N2500/20
Abstract: 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.
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公开(公告)号：US09522883B2
公开(公告)日：2016-12-20
申请号：US14424602
申请日：2013-08-29
Applicant: Alectos Therapeutics Inc. , Merck Sharp & Dohme Corp.
Inventor： Ernest J. McEachern , David J. Vocadlo , Yuanxi Zhou , Harold G. Selnick
IPC: C07D211/56 , A61K31/445 , A61K31/4523 , C07D401/06 , C07D417/06
CPC classification number: C07D211/56 , A61K31/445 , A61K31/4523 , C07D401/06 , C07D417/06
Abstract: The invention provides compounds of Formula (I) for inhibiting gh cosidases, prodrugs of the compounds, and pharmaceutical compositions comprising the compounds or prodrugs of the compounds. The invention also provides method of treating diseases and disorders related to deficiency or over-expression of O-gh coprotein 2-acetamido-2-deoxy-β-D-glucopyranosidase (O-GlcNAcase), accumulation or deficiency of 2-acetamido-2-deoxy-β-D-glucopyranoside (O-GlcNAc).
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公开(公告)号：US20200207800A1
公开(公告)日：2020-07-02
申请号：US16622870
申请日：2018-06-12
Applicant: ALECTOS THERAPEUTICS INC.
Inventor： David J. VOCADLO , Samy CECIONI
IPC: C07H15/26 , G01N33/58 , G01N21/64 , G01N33/542
Abstract: The invention provides fluorescence-quenched substrates of exo-glycosidase enzymes. The invention also provides methods for imaging exo-glycosidase enzymes activity within cells.
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