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公开(公告)号：US20150353552A1
公开(公告)日：2015-12-10
申请号：US14443294
申请日：2013-11-15
申请人： Abdelghani Abe ACHAB , Michael D. ALTMAN , Yongqi DENG , Timothy GUZI , Solomon KATTAR , Jason D. KATZ , Joey L. METHOT , Hua ZHOU , Meredeth MCGOWAN , Matthew P. CHRISTOPHER , Yudith GARCIA , Neville John THONY , Francesc Xavier FRADERA LLINAS , Changwei MU , Sixing ZHANG , Rong ZHANG , Kin Chiu FONG , Xiansheng LENG , MERCK SHARP & DOHME CORP.
发明人： Abdelghani Abe Achab , Michael D. Altman , Yongqi Deng , Timothy Guzi , Solomon Kattar , Jason D. Katz , Joey L. Methot , Hua Zhou , Meredeth McGowan , Matthew P. Christopher , Yudith Garcia , Neville John Anthony , Francesc Xavier Fradera Llinas , Kin Chiu Fong , Xiansheng Leng , Changwei Mu , Sixing Zhang , Rong Zhang
IPC分类号： C07D473/30 , A61K31/5377 , A61K31/52
CPC分类号： A61K31/52 , A61K31/5377 , A61K45/06 , C07D473/00 , C07D473/06 , C07D473/30 , C07D473/38 , C07D519/00 , A61K2300/00
摘要： The instant invention provides compounds of formula I which are PI3K-delta inhibitors, and as such are useful for the treatment of PI3K-delta-mediated diseases such as inflammation, asthma, COPD and cancer.
摘要翻译： 本发明提供了作为PI3K-δ抑制剂的式I化合物，因此可用于治疗PI3K-δ介导的疾病如炎症，哮喘，COPD和癌症。
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公开(公告)号：US20170114078A1
公开(公告)日：2017-04-27
申请号：US15318483
申请日：2015-06-09
申请人： Meredeth Ann MCGOWAN , Kin Chiu FONG , Neville John ANTHONY , Hua ZHOU , Jason D. KATZ , Lihu YANG , Chaomin LI , Yuan TIAN , Changwei MU , Baijun YE , Feng SHI , Xiaoli ZHAO , Jianmin FU , Yabin LI , Merck Sharp & Dohme Corp.
发明人： Meredeth Ann McGowan , Kin Chiu Fong , Neville John Anthony , Hua Zhou , Jason D. Katz , Lihu Yang , Chaomin Li , Yuan Tian , Changwei Mu , Baijun Ye , Feng Shi , Xiaoli Zhao , Jianmin Fu , Yabin Li
IPC分类号： C07D519/00 , C07D473/30 , C07D473/34 , A61K31/52
CPC分类号： C07D519/00 , A61K31/52 , C07D473/30 , C07D473/34
摘要： The instant invention provides compounds of formula (I) which are PI3K-delta inhibitors, and as such are useful for the treatment of PI3K-delta-mediated diseases such as inflammation, asthma, COPD and cancer.
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公开(公告)号：US10100064B2
公开(公告)日：2018-10-16
申请号：US15318483
申请日：2015-06-09
发明人： Meredeth Ann McGowan , Kin Chiu Fong , Neville John Anthony , Hua Zhou , Jason D. Katz , Lihu Yang , Chaomin Li , Yuan Tian , Changwei Mu , Baijun Ye , Feng Shi , Xiaoli Zhao , Jianmin Fu , Yabin Li
IPC分类号： C07D473/30 , C07D473/34 , C07D519/00 , A61K31/52
摘要： The instant invention provides compounds of formula (I) which are PI3K-delta inhibitors, and as such are useful for the treatment of PI3K-delta-mediated diseases such as inflammation, asthma, COPD and cancer.
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公开(公告)号：US20150152127A1
公开(公告)日：2015-06-04
申请号：US14399146
申请日：2013-05-03
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
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。
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公开(公告)号：US09938281B2
公开(公告)日：2018-04-10
申请号：US14443314
申请日：2013-11-15
发明人： Abdelghani Abe Achab , Michael D. Altman , Yongqi Deng , Solomon Kattar , Jason D. Katz , Joey L. Methot , Hua Zhou , Meredeth McGowan , Matthew P. Christopher , Yudith Garcia , Neville John Anthony , Francesc Xavier Fradera Llinas , Liping Yang , Changwei Mu , Xiaona Wang , Feng Shi , Baijun Ye , Sixing Zhang , Xiaoli Zhao , Rong Zhang , Kin Chiu Fong , Xiansheng Leng
IPC分类号： A61K31/52 , A61K31/535 , C07D473/00 , C07D403/00 , C07D487/04 , C07D473/34 , A61K45/06 , A61K31/5377 , A61K31/55 , C07D519/00
CPC分类号： C07D487/04 , A61K31/52 , A61K31/5377 , A61K31/55 , A61K45/06 , C07D473/34 , C07D519/00 , A61K2300/00
摘要： The instant invention provides compounds of formula I which are PI3K-delta inhibitors, and as such are useful for the treatment of PI3K-delta-mediated diseases such as inflammation, asthma, COPD and cancer.
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公开(公告)号：US09730940B2
公开(公告)日：2017-08-15
申请号：US14443294
申请日：2013-11-15
发明人： Abdelghani Abe Achab , Michael D. Altman , Yongqi Deng , Timothy Guzi , Solomon Kattar , Jason D. Katz , Joey L. Methot , Hua Zhou , Meredeth McGowan , Matthew P. Christopher , Yudith Garcia , Neville John Anthony , Francesc Xavier Fradera Llinas , Kin Chiu Fong , Xiansheng Leng , Changwei Mu , Sixing Zhang , Rong Zhang
IPC分类号： A61K31/52 , C07D473/00 , C07D473/06 , C07D473/30 , C07D473/38 , C07D519/00 , A61K31/5377 , A61K45/06
CPC分类号： A61K31/52 , A61K31/5377 , A61K45/06 , C07D473/00 , C07D473/06 , C07D473/30 , C07D473/38 , C07D519/00 , A61K2300/00
摘要： The instant invention provides compounds of formula I which are PI3K-delta inhibitors, and as such are useful for the treatment of PI3K-delta-mediated diseases such as inflammation, asthma, COPD and cancer.
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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
发明人： Ramesh Kaul , Ernest J. McEachern , Changwei Mu , Harold G. Selnick , David J. Vocadlo , Yaode Wang , Zhongyong Wei , Yuanxi Zhou , Yongbao Zhu
IPC分类号： C07H9/06 , C07H9/00 , C07D513/04 , C12Q1/34 , C07H17/00
CPC分类号： C07H9/06 , C07D513/04 , C07H9/00 , C07H17/00 , C12Q1/34 , G01N2333/924 , G01N2500/04 , G01N2500/20
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.
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公开(公告)号：US09611275B2
公开(公告)日：2017-04-04
申请号：US14399146
申请日：2013-05-03
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.
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公开(公告)号：US20160207926A1
公开(公告)日：2016-07-21
申请号：US14443314
申请日：2013-11-15
发明人： Abdelghani Abe Achab , Michael D. Altman , Yongqi Deng , Solomon Kattar , Jason D. Katz , Joey L. Methot , Hua Zhou , Meredeth McGowan , Matthew P. Christopher , Yudith Garcia , Neville John Anthony , Francesc Xavier Fradera Llinas , Liping Yang , Changwei Mu , Xiaona Wang , Feng Shi , Baijun Ye , Sixing Zhang , Xiaoli Zhao , Rong Zhang , Kin Chiu Fong , Xiansheng Leng
IPC分类号： C07D487/04 , A61K31/55 , A61K31/5377 , A61K31/52 , C07D519/00
CPC分类号： C07D487/04 , A61K31/52 , A61K31/5377 , A61K31/55 , A61K45/06 , C07D473/34 , C07D519/00 , A61K2300/00
摘要： The instant invention provides compounds of formula I which are PI3K-delta inhibitors, and as such are useful for the treatment of PI3K-delta-mediated diseases such as inflamation, asthma, COPD and cancer.
摘要翻译： 本发明提供了作为PI3K-δ抑制剂的式I化合物，因此可用于治疗PI3K-δ介导的疾病如炎症，哮喘，COPD和癌症。
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公开(公告)号：US20140005191A1
公开(公告)日：2014-01-02
申请号：US13884061
申请日：2011-11-09
申请人： Craig A. Coburn , Kun Liu , Ernest J. McEacher , Changwei Mu , Harold G. Selnick , David J. Vocadlo , Yaode Wang , Zhongyong Wei , Yuanxi Zhou
发明人： Craig A. Coburn , Kun Liu , Ernest J. McEacher , Changwei Mu , Harold G. Selnick , David J. Vocadlo , Yaode Wang , Zhongyong Wei , Yuanxi Zhou
IPC分类号： C07D513/14
CPC分类号： C07D513/14 , C07D513/04 , C07H9/06 , C07H13/04 , C07H13/12 , C07H15/18 , C12Q1/48 , G01N2500/02
摘要： 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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