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.

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。

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.

公开(公告)号：US20160096858A1

公开(公告)日：2016-04-07

申请号：US14966221

申请日：2015-12-11

Applicant: Merck Sharp & Dohme Corp. ,  Alectos Therapeutics Inc.

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 ,  C12Q1/34 ,  C07D513/04

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.

Abstract translation: 本发明提供了具有增强的选择性抑制糖苷酶的通透性的化合物，化合物的前药以及包含化合物的化合物或前药的药物组合物。 本发明还提供了治疗与O-GlcNAcase的缺乏或过度表达相关的疾病和障碍的方法，O-GlcNAc的积累或缺乏。