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公开(公告)号：US20170210759A1
公开(公告)日：2017-07-27
申请号：US15480220
申请日：2017-04-05
IPC分类号： C07D513/04 , C07D239/94 , C07D239/86 , C07D401/12 , C07D491/048 , C07D405/12 , C07D495/04 , C07D239/88 , C07D217/22 , C07D471/04 , C07D403/12 , C07D239/93
CPC分类号： C07D513/04 , A61K31/517 , A61P25/28 , C07D217/22 , C07D239/86 , C07D239/88 , C07D239/93 , C07D239/94 , C07D401/12 , C07D403/12 , C07D405/12 , C07D471/04 , C07D491/04 , C07D491/048 , C07D495/04
摘要： The present application discloses compounds which are activators of autophagic flux and pharmaceutical compositions comprising said activators. It further discloses use of said compounds and pharmaceutical compositions in the treatment of neurodegenerative diseases, particularly proteinopathies and tauopathies such as Alzheimer's disease. It further discloses methods of enhancing autophagic flux.
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公开(公告)号：US20200216469A1
公开(公告)日：2020-07-09
申请号：US16818388
申请日：2020-03-13
IPC分类号： C07D513/04 , A61P25/28 , C07D491/048 , C07D401/12 , C07D239/88 , C07D217/22 , A61K31/517 , C07D495/04 , C07D491/04 , C07D471/04 , C07D239/94 , C07D239/93 , C07D239/86 , C07D405/12 , C07D403/12
摘要： The present application discloses compounds which are activators of autophagic flux and pharmaceutical compositions comprising said activators. It further discloses use of said compounds and pharmaceutical compositions in the treatment of neurodegenerative diseases, particularly proteinopathies and tauopathies such as Alzheimer's disease. It further discloses methods of enhancing autophagic flux.
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公开(公告)号：US20190112317A1
公开(公告)日：2019-04-18
申请号：US15765801
申请日：2016-10-05
IPC分类号： C07D513/04 , A61K31/517 , C07D217/22 , C07D239/88 , C07D239/93 , C07D239/94 , C07D401/12 , C07D403/12 , C07D405/12 , C07D491/048 , A61P25/28
摘要： The present application discloses compounds which are activators of autophagic flux and pharmaceutical compositions comprising said activators. It further discloses use of said compounds and pharmaceutical compositions in the treatment of neurodegenerative diseases, particularly proteinopathies and tauopathies such as Alzheimer's disease. It further discloses methods of enhancing autophagic flux.
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公开(公告)号：US20180312526A1
公开(公告)日：2018-11-01
申请号：US16027930
申请日：2018-07-05
IPC分类号： C07D513/04 , C07D491/048 , C07D401/12 , C07D217/22 , C07D239/88 , C07D495/04 , C07D405/12 , C07D471/04 , C07D239/94 , C07D239/93 , A61K31/517 , C07D403/12 , C07D239/86 , C07D491/04
CPC分类号： C07D513/04 , A61K31/517 , C07D217/22 , C07D239/86 , C07D239/88 , C07D239/93 , C07D239/94 , C07D401/12 , C07D403/12 , C07D405/12 , C07D471/04 , C07D491/04 , C07D491/048 , C07D495/04
摘要： The present application discloses compounds which are activators of autophagic flux and pharmaceutical compositions comprising said activators. It further discloses use of said compounds and pharmaceutical compositions in the treatment of neurodegenerative diseases, particularly proteinopathies and tauopathies such as Alzheimer's disease. It further discloses methods of enhancing autophagic flux.
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公开(公告)号：US11261199B2
公开(公告)日：2022-03-01
申请号：US16818388
申请日：2020-03-13
IPC分类号： C07D513/04 , C07D403/12 , C07D405/12 , C07D239/86 , C07D239/93 , C07D239/94 , C07D471/04 , C07D491/04 , C07D495/04 , A61K31/517 , C07D217/22 , C07D239/88 , C07D401/12 , C07D491/048 , A61P25/28
摘要： The present application discloses compounds which are activators of autophagic flux and pharmaceutical compositions comprising said activators. It further discloses use of said compounds and pharmaceutical compositions in the treatment of neurodegenerative diseases, particularly proteinopathies and tauopathies such as Alzheimer's disease. It further discloses methods of enhancing autophagic flux.
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公开(公告)号：US11230558B2
公开(公告)日：2022-01-25
申请号：US16027951
申请日：2018-07-05
IPC分类号： C07D513/04 , C07D403/12 , C07D405/12 , C07D239/86 , C07D239/93 , C07D239/94 , C07D471/04 , C07D491/04 , C07D495/04 , A61K31/517 , C07D217/22 , C07D239/88 , C07D401/12 , C07D491/048 , A61P25/28
摘要： The present application discloses compounds which are activators of autophagic flux and pharmaceutical compositions comprising said activators. It further discloses use of said compounds and pharmaceutical compositions in the treatment of neurodegenerative diseases, particularly proteinopathies and tauopathies such as Alzheimer's disease. It further discloses methods of enhancing autophagic flux.
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公开(公告)号：US11008341B2
公开(公告)日：2021-05-18
申请号：US16027930
申请日：2018-07-05
IPC分类号： C07D513/04 , A61P25/28 , A61K31/517 , C07D217/22 , C07D239/86 , C07D239/88 , C07D239/93 , C07D239/94 , C07D401/12 , C07D403/12 , C07D405/12 , C07D471/04 , C07D491/04 , C07D491/048 , C07D495/04
摘要： The present application discloses compounds which are activators of autophagic flux and pharmaceutical compositions comprising said activators. It further discloses use of said compounds and pharmaceutical compositions in the treatment of neurodegenerative diseases, particularly proteinopathies and tauopathies such as Alzheimer's disease. It further discloses methods of enhancing autophagic flux.
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公开(公告)号：US20180312527A1
公开(公告)日：2018-11-01
申请号：US16027990
申请日：2018-07-05
IPC分类号： C07D513/04 , C07D491/048 , C07D401/12 , C07D217/22 , C07D239/88 , C07D495/04 , C07D405/12 , C07D471/04 , C07D239/94 , C07D239/93 , A61K31/517 , C07D403/12 , C07D239/86 , C07D491/04
CPC分类号： C07D513/04 , A61K31/517 , C07D217/22 , C07D239/86 , C07D239/88 , C07D239/93 , C07D239/94 , C07D401/12 , C07D403/12 , C07D405/12 , C07D471/04 , C07D491/04 , C07D491/048 , C07D495/04
摘要： The present application discloses compounds which are activators of autophagic flux and pharmaceutical compositions comprising said activators. It further discloses use of said compounds and pharmaceutical compositions in the treatment of neurodegenerative diseases, particularly proteinopathies and tauopathies such as Alzheimer's disease. It further discloses methods of enhancing autophagic flux.
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9.发明申请公开(公告)号：US20220251143A1
公开(公告)日：2022-08-11
申请号：US17476656
申请日：2021-09-16
摘要： The present disclosure provides conjugate compositions comprising non-hydrolyzable, non-cleavable, stable linkers, a targeting moiety, and a therapeutic or chemotherapeutic agent. More specifically the present disclosure provides for compositions comprising non-hydrolyzable, non-cleavable, stable linkers, a somatostatin receptor (SSTR) targeting moiety, such as lanreotide, and a chemotherapeutic agent targeting microtubules, such as mertansine. Methods of using the compositions to treat cancer and other diseases are also provided.
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公开(公告)号：US20190070183A1
公开(公告)日：2019-03-07
申请号：US15773430
申请日：2016-11-04
发明人： Changchun Deng , Shi-Xian Deng , Donald W. Landry , Mark Lipstein , Michael Mangone , Owen O'Connor , Xavier O. Jirau Serrano , Luigi Scotto , Xiaoming Xu
IPC分类号： A61K31/52 , A61K31/551 , A61P9/10 , A61P35/02 , A61K31/336 , A61K31/5375
摘要： The invention relates to the co-administration of select proteasome and PI3K inhibitors is useful for treating c-Myc-overexpressing cancers, particularly hematological cancers such as aggressive B- and T-cell lymphomas. In exemplified embodiments, coadministration of a dual PI3K/CK-1 inhibitor with a proteasome inhibitor synergistically increases cell death of aggressive B- and T-cell lymphomas as well as multiple myeloma over the individual or additive effect of either or both agents. This synergistic effect is associated with the previously unknown inhibition of the kinase casein kinase 1 epsilon (CK-1ε) by a PI3K inhibitor, such as TGR-1202. Accordingly, use of PI3K inhibitors that possess CK-1ε inhibition in combination with proteasome inhibitors provides a new therapy regime for treating c-Myc-overexpressing cancers, and particularly hematological cancers.
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