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![PYRROLO[2,3-C]PYRIDINES AS IMAGING AGENTS FOR NEUROFIBRILLARY](/abs-image/US/2017/05/04/US20170119912A1/abs.jpg.150x150.jpg)
公开(公告)号：US20170119912A1
公开(公告)日：2017-05-04
申请号：US15317333
申请日：2015-06-09
Applicant: Abbas W. Walji , Eric Hostetler , Thomas J. Greshock , Jing Li , Keith P. Moore , Idriss Bennacef , James Mulhearn , Harold Selnick , Yaode Wang , Kun Yang , Jianmin Fu , MERCK SHARP & DOHME CORP.
Inventor： Abbas W. Walji , Eric Hostetler , Thomas J. Greshock , Jing Li , Keith P. Moore , Idriss Bennacef , James Mulhearn , Harold Selnick , Yaode Wang , Kun Yang , Jianmin Fu
IPC: A61K51/04 , C07D519/00 , C07D471/04
CPC classification number: A61K51/0455 , A61K51/0459 , C07B2200/05 , C07D471/04 , C07D519/00
Abstract: The present invention is directed to pyrrolopyridine compounds of formula (I) or their pharmaceutically acceptable salts, which may be suitable for imaging tau aggregates, b-sheet aggregates, beta-amyloid aggregates or alpha-synuclein aggregates, and hence are useful in binding and imaging tau aggregates in Alzheimer's patients. More specifically, this invention relates to a method of using the compounds of this invention as tracers in positron emission tomography (PET) imaging to study tau deposits in brain in vivo to allow diagnosis of Alzheimer's disease and other neurodegenerative diseases characterized by tau pathology. The invention further relates to a method of measuring clinical efficacy of therapeutic agents for Alzheimer's disease and other neurodegenerative diseases characterized by tau pathology.
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公开(公告)号：US20140213584A9
公开(公告)日：2014-07-31
申请号：US13884061
申请日：2011-11-08
Applicant: Craig A. Coburn , Kun Liu , Ernest J. McEachern , Changwei Mu , Harold G. Selnick , David J. Vocadlo , Yaode Wang , Zhongyong Wei , Yuanxi Zhou
Inventor： Craig A. Coburn , Kun Liu , Ernest J. McEachern , Changwei Mu , Harold G. Selnick , David J. Vocadlo , Yaode Wang , Zhongyong Wei , Yuanxi Zhou
IPC: C07D513/14
CPC classification number: C07D513/14 , C07D513/04 , C07H9/06 , C07H13/04 , C07H13/12 , C07H15/18 , C12Q1/48 , G01N2500/02
Abstract: The invention provides compounds 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：US20140018309A1
公开(公告)日：2014-01-16
申请号：US13997484
申请日：2011-12-21
Applicant: Ramesh Kaul , Ernest J. Mceachern , Changwei Mu , Harold G. Selnick , David J. Vocadlo , Yaode Wang , Zhongyong Wei , Yuanxi Zhou , Yongbao Zhu
Inventor： Ramesh Kaul , Ernest J. Mceachern , Changwei Mu , Harold G. Selnick , David J. Vocadlo , Yaode Wang , Zhongyong Wei , Yuanxi Zhou , Yongbao Zhu
IPC: 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.
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。
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公开(公告)号：US09718854B2
公开(公告)日：2017-08-01
申请号：US14008388
申请日：2012-03-20
Applicant: Ramesh Kaul , Ernest J. McEachern , David J. Vocadlo , Yuanxi Zhou , Kun Liu , Harold G. Selnick , Zhongyong Wei , Changwei Mu , Yaode Wang , Xiaona Wang
Inventor： Ramesh Kaul , Ernest J. McEachern , David J. Vocadlo , Yuanxi Zhou , Kun Liu , Harold G. Selnick , Zhongyong Wei , Changwei Mu , Yaode Wang , Xiaona Wang
IPC: C07H19/24 , C07D513/04 , A61K31/429 , C12N9/99 , C12Q1/34 , C07H9/06 , C07H11/00 , C07H13/12 , C07H15/04 , C07H15/12 , C07H15/18 , C07H15/203 , C07H15/207 , C07H17/02 , C07H17/04 , A61K31/7056
CPC classification number: C07H19/24 , A61K31/7056 , C07D513/04 , C07H9/06 , C07H11/00 , C07H13/12 , C07H15/04 , C07H15/12 , C07H15/18 , C07H15/203 , C07H15/207 , C07H17/02 , C07H17/04 , C12N9/99 , C12Q1/34 , C12Y302/01169
Abstract: The invention provides compounds of formula (I) with substituents as specified in claim 1 for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceuticals compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to over-expression of O-GlcNAcase or accumulation of O-GlcNac.
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Patent Agency Ranking
公开(公告)号：US20140005191A1
公开(公告)日：2014-01-02
申请号：US13884061
申请日：2011-11-09
Applicant: Craig A. Coburn , Kun Liu , Ernest J. McEacher , Changwei Mu , Harold G. Selnick , David J. Vocadlo , Yaode Wang , Zhongyong Wei , Yuanxi Zhou
Inventor： Craig A. Coburn , Kun Liu , Ernest J. McEacher , Changwei Mu , Harold G. Selnick , David J. Vocadlo , Yaode Wang , Zhongyong Wei , Yuanxi Zhou
IPC: C07D513/14
CPC classification number: C07D513/14 , C07D513/04 , C07H9/06 , C07H13/04 , C07H13/12 , C07H15/18 , C12Q1/48 , G01N2500/02
Abstract: The invention provides compounds 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：US20130296301A1
公开(公告)日：2013-11-07
申请号：US13883811
申请日：2011-11-08
Applicant: Jiang Chang , Kun Liu , Ernest J. McEachern , Changwei Mu , Harold G. Selnick , Feng Shi , David J. Vocadlo , Yaode Wang , Zhongyong Wei , Yuanxi Zhou , Yongbao Zhu
Inventor： Jiang Chang , Kun Liu , Ernest J. McEachern , Changwei Mu , Harold G. Selnick , Feng Shi , David J. Vocadlo , Yaode Wang , Zhongyong Wei , Yuanxi Zhou , Yongbao Zhu
IPC: C07D513/04
CPC classification number: C07D513/04
Abstract: The invention is directed to compounds for selectively inhibiting glycosidases, uses of the compounds and pharmaceutical compositions including the compounds, and methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, and/or accumulation or deficiency of O-GlcNAc.
Abstract translation: 本发明涉及用于选择性抑制糖苷酶的化合物，化合物的用途和包含该化合物的药物组合物，以及治疗与O-GlcNAC的缺乏或过度表达有关的疾病和障碍和/或O-GlcNAc的积累或缺陷的方法。
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公开(公告)号：US08933040B2
公开(公告)日：2015-01-13
申请号：US13884061
申请日：2011-11-08
Applicant: Craig A. Coburn , Kun Liu , Ernest J. McEacher , Changwei Mu , Harold G. Selnick , David J. Vocadlo , Yaode Wang , Zhongyong Wei , Yuanxi Zhou
Inventor： Craig A. Coburn , Kun Liu , Ernest J. McEacher , Changwei Mu , Harold G. Selnick , David J. Vocadlo , Yaode Wang , Zhongyong Wei , Yuanxi Zhou
IPC: C08B37/00 , C07D487/02 , A61K31/70 , A61K31/425 , C07D513/14 , C07D513/04 , C07H9/06 , C07H13/04 , C07H13/12 , C07H15/18 , C12Q1/48
CPC classification number: C07D513/14 , C07D513/04 , C07H9/06 , C07H13/04 , C07H13/12 , C07H15/18 , C12Q1/48 , G01N2500/02
Abstract: The invention provides compounds 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: 本发明提供了用于选择性抑制糖苷酶，化合物前药和包含化合物的化合物或前药的药物组合物的化合物。 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。
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公开(公告)号：US08901087B2
公开(公告)日：2014-12-02
申请号：US13883811
申请日：2011-11-08
Applicant: Jiang Chang , Kun Liu , Ernest J. McEachern , Changwei Mu , Harold G. Selnick , Feng Shi , David J. Vocadlo , Yaode Wang , Zhongyong Wei , Yuanxi Zhou , Yongbao Zhu
Inventor： Jiang Chang , Kun Liu , Ernest J. McEachern , Changwei Mu , Harold G. Selnick , Feng Shi , David J. Vocadlo , Yaode Wang , Zhongyong Wei , Yuanxi Zhou , Yongbao Zhu
IPC: C08B37/00 , C07D487/02 , A61K31/70 , A61K31/425 , C07D513/04
CPC classification number: C07D513/04
Abstract: The invention is directed to compounds for selectively inhibiting glycosidases, uses of the compounds and pharmaceutical compositions including the compounds, and methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, and/or accumulation or deficiency of O-GlcNAc.
Abstract translation: 本发明涉及用于选择性抑制糖苷酶的化合物，化合物的用途和包含该化合物的药物组合物，以及治疗与O-GlcNAC的缺乏或过度表达有关的疾病和障碍和/或O-GlcNAc的积累或缺陷的方法。
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公开(公告)号：US20140088028A1
公开(公告)日：2014-03-27
申请号：US14008388
申请日：2012-03-20
Applicant: Ramesh Kaul , Ernest J. McEachern , David J. Vocadlo , Yuanxi Zhou , Kun Liu , Harold G. Selnick , Zhongyong Wei , Changwei Mu , Yaode Wang , Xiaona Wang
Inventor： Ramesh Kaul , Ernest J. McEachern , David J. Vocadlo , Yuanxi Zhou , Kun Liu , Harold G. Selnick , Zhongyong Wei , Changwei Mu , Yaode Wang , Xiaona Wang
IPC: C07H19/24
CPC classification number: C07H19/24 , A61K31/7056 , C07D513/04 , C07H9/06 , C07H11/00 , C07H13/12 , C07H15/04 , C07H15/12 , C07H15/18 , C07H15/203 , C07H15/207 , C07H17/02 , C07H17/04 , C12N9/99 , C12Q1/34 , C12Y302/01169
Abstract: The invention provides compounds of formula (I) with substituents as specified in Claim 1 for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceuticals compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to over-expression of O-GlcNAcase or accumulation of O-GlcNac.
Abstract translation: 本发明提供具有权利要求1所述取代基的式（I）化合物，用于选择性抑制糖苷酶，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的过度表达或O-GlcNac的积累有关的疾病和病症的方法。
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