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公开(公告)号：US10695337B2
公开(公告)日：2020-06-30
申请号：US15995323
申请日：2018-06-01
发明人： Taisheng Huang , Chu-Biao Xue
IPC分类号： A61K31/519 , A61P17/04 , A61K31/4545 , C07D487/04 , A61P1/00 , A61P11/00 , A61P35/00 , A61P11/06 , A61P27/02 , C07D401/14 , C07D405/14 , A61K9/00 , C07D519/00 , C07D471/04
摘要： The present invention provides piperidin-4-yl azetidine derivatives, as well as their compositions and methods of use, that modulate the activity of Janus kinase 1 (JAK1) and are useful in the treatment of diseases related to the activity of JAK1 including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.
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公开(公告)号：US20230043959A1
公开(公告)日：2023-02-09
申请号：US17674237
申请日：2022-02-17
发明人： Taisheng Huang , Chu-Biao Xue , Hui-Yin Li , Qun Li , Anlai Wang , Lingquan Kong , Hai Fen Ye , Wenqing Yao , James D. Rodgers , Stacey Shepard , Haisheng Wang , Lixin Shao
IPC分类号： A61K31/4545 , C07D487/04 , A61P1/00 , A61P11/00 , A61P35/00 , A61P11/06 , A61P27/02 , A61P17/04 , A61P37/06 , C07D401/14 , C07D405/14 , A61K9/00 , A61K31/519
摘要： The present invention provides piperidin-4-y1 azetidine derivatives, as well as their compositions and methods of use, that modulate the activity of Janus kinase 1 (JAK1) and are useful in the treatment of diseases related to the activity of JAK1 including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.
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公开(公告)号：US11285140B2
公开(公告)日：2022-03-29
申请号：US16878281
申请日：2020-05-19
发明人： Taisheng Huang , Chu-Biao Xue
IPC分类号： A61K31/519 , A61P37/06 , C07D487/04 , A61K31/4545 , A61P1/00 , A61P11/00 , A61P35/00 , A61P11/06 , A61P27/02 , A61P17/04 , C07D401/14 , C07D405/14 , A61K9/00 , C07D519/00 , C07D471/04
摘要： The present invention provides piperidin-4-yl azetidine derivatives, as well as their compositions and methods of use, that modulate the activity of Janus kinase 1 (JAK1) and are useful in the treatment of diseases related to the activity of JAK1 including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.
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公开(公告)号：US09464088B2
公开(公告)日：2016-10-11
申请号：US14289121
申请日：2014-05-28
发明人： Taisheng Huang , Chu-Biao Xue , Hui-Yin Li , Qun Li
IPC分类号： C07D487/04 , A61K31/519 , C07D401/14 , C07D405/14 , C07D471/04 , A61K31/437 , A61P35/02 , A61P35/04 , A61P19/02 , A61P29/00 , A61P37/06 , A61P3/10 , A61P17/06 , A61P17/00 , C07D519/00
CPC分类号： A61K31/4545 , A61K9/0014 , A61K9/0019 , A61K9/0024 , A61K9/0048 , A61K31/519 , A61P1/00 , A61P11/00 , A61P11/06 , A61P27/02 , A61P35/00 , C07B2200/13 , C07D401/14 , C07D405/14 , C07D471/04 , C07D487/04 , C07D519/00
摘要： The present invention provides piperidin-4-yl azetidine derivatives, as well as their compositions and methods of use, that modulate the activity of Janus kinase 1 (JAK1) and are useful in the treatment of diseases related to the activity of JAK1 including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.
摘要翻译： 本发明提供哌啶-4-基氮杂环丁烷衍生物及其组合物和使用方法，其调节Janus激酶1（JAK1）的活性，并且可用于治疗与JAK1的活性相关的疾病，包括对于 例如炎症性疾病，自身免疫性疾病，癌症和其它疾病。
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公开(公告)号：US20180353499A1
公开(公告)日：2018-12-13
申请号：US15995323
申请日：2018-06-01
发明人： Taisheng Huang , Chu-Biao Xue , Hui-Yin Li , Qun Li , Anlai Wang , Lingquan Kong , Hai Fen Ye , Wenqing Yao , James D. Rodgers , Stacey Shepard , Haisheng Wang , Lixin Shao
IPC分类号： A61K31/4545 , C07D487/04 , A61P11/06 , A61P1/00 , A61P27/02 , C07D405/14 , C07D401/14 , A61K31/519 , A61K9/00 , A61P35/00 , A61P11/00 , C07D471/04 , C07D519/00
摘要： The present invention provides piperidin-4-yl azetidine derivatives, as well as their compositions and methods of use, that modulate the activity of Janus kinase 1 (JAK1) and are useful in the treatment of diseases related to the activity of JAK1 including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.
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公开(公告)号：US09999619B2
公开(公告)日：2018-06-19
申请号：US15288641
申请日：2016-10-07
发明人： Taisheng Huang , Chu-Biao Xue
IPC分类号： A61K31/519 , A61P37/06 , A61K31/4545 , A61K9/00 , C07D487/04
CPC分类号： A61K31/4545 , A61K9/0014 , A61K9/0019 , A61K9/0024 , A61K9/0048 , A61K31/519 , A61P1/00 , A61P11/00 , A61P11/06 , A61P27/02 , A61P35/00 , C07B2200/13 , C07D401/14 , C07D405/14 , C07D471/04 , C07D487/04 , C07D519/00
摘要： The present invention provides piperidin-4-yl azetidine derivatives, as well as their compositions and methods of use, that modulate the activity of Janus kinase 1 (JAK1) and are useful in the treatment of diseases related to the activity of JAK1 including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.
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公开(公告)号：US20170246157A1
公开(公告)日：2017-08-31
申请号：US15288641
申请日：2016-10-07
发明人： Taisheng Huang , Chu-Biao Xue , Hui-Yin Li , Qun Li , Anlai Wang , Lingquan Kong , Hai Fen Ye , Wenqing Yao , James D Rodgers , Stacey Shepard , Haisheng Wang , Lixin Shao
IPC分类号： A61K31/4545 , A61K9/00
CPC分类号： A61K31/4545 , A61K9/0014 , A61K9/0019 , A61K9/0024 , A61K9/0048 , A61K31/519 , A61P1/00 , A61P11/00 , A61P11/06 , A61P27/02 , A61P35/00 , C07B2200/13 , C07D401/14 , C07D405/14 , C07D471/04 , C07D487/04 , C07D519/00
摘要： The present invention provides piperidin-4-yl azetidine derivatives, as well as their compositions and methods of use, that modulate the activity of Janus kinase 1 (JAK1) and are useful in the treatment of diseases related to the activity of JAK1 including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.
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公开(公告)号：US12060433B2
公开(公告)日：2024-08-13
申请号：US17138306
申请日：2020-12-30
申请人： Incyte Corporation
发明人： Horacio G. Nastri , Shaun M. Stewart , Juan Carlos Almagro , Jing Zhou , Rebecca A. Buonpane , Hui Wang , Yingnan Chen , Xiaozhao Wang , Peter Niels Carlsen , Yong Li , Chao Qi , Liangxing Wu , Wenqing Yao , Wenyu Zhu , Taisheng Huang
IPC分类号： C07K16/28 , A61K31/135 , A61K31/4985 , A61P35/00 , A61K39/00
CPC分类号： C07K16/2896 , A61K31/135 , A61K31/4985 , A61P35/00 , A61K2039/505
摘要： Disclosed are combination therapies comprising administration of a CD73 inhibitor and an adenosine A2A or A2B receptor inhibitor. The disclosed combination therapies are useful in the treatment of diseases related to the activity of adenosine receptors and/or CD73 including, for example, cancer, inflammatory diseases, cardiovascular diseases, and neurodegenerative diseases. Anti-CD73 antibodies and A2A/A2B inhibitors are also disclosed.
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公开(公告)号：US11767320B2
公开(公告)日：2023-09-26
申请号：US17449696
申请日：2021-10-01
申请人： INCYTE CORPORATION
发明人： Taisheng Huang , Xiaozhao Wang , Wenqing Yao
IPC分类号： C07D471/04 , A61P35/00
CPC分类号： C07D471/04 , A61P35/00 , C07B2200/05
摘要： Disclosed are compounds of Formula I, methods of using the compounds for inhibiting KRAS activity and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders associated with KRAS activity such as cancer.
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公开(公告)号：US11673894B2
公开(公告)日：2023-06-13
申请号：US17077713
申请日：2020-10-22
申请人： Incyte Corporation
发明人： Xiaozhao Wang , Pei Gan , Taisheng Huang , Chao Qi , Ding-Quan Qian , Liangxing Wu , Wenqing Yao , Zhiyong Yu , Fenglei Zhang , Le Zhao , Chunhong He
IPC分类号： C07D497/04 , C07D487/04 , C07D491/056 , C07D519/00 , A61P35/00 , A61P25/00 , A61P9/00 , A61P29/00
CPC分类号： C07D487/04 , A61P9/00 , A61P25/00 , A61P29/00 , A61P35/00 , C07D491/056 , C07D519/00
摘要： This application relates to compounds of Formula (I):
or pharmaceutically acceptable salts or stereoisomers thereof, which modulate the activity of adenosine receptors, such as subtypes A2A and A2B receptors, and are useful in the treatment of diseases related to the activity of adenosine receptors including, for example, cancer, inflammatory diseases, cardiovascular diseases, and neurodegenerative diseases.
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