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公开(公告)号:USRE49948E1
公开(公告)日:2024-04-30
申请号:US17592108
申请日:2022-02-03
发明人: Darryl David Dixon , Jonas Grina , John A. Josey , James P. Rizzi , Stephen T. Schlachter , Eli M. Wallace , Bin Wang , Paul Wehn , Rui Xu , Hanbiao Yang
IPC分类号: C07D213/85 , A61K31/09 , A61K31/10 , C07B39/00 , C07C43/205 , C07C43/225 , C07C43/23 , C07C43/263 , C07C43/285 , C07C205/22 , C07C255/54 , C07C255/56 , C07C311/29 , C07C313/06 , C07C317/22 , C07C317/24 , C07C317/32 , C07C317/34 , C07C317/36 , C07C317/40 , C07C317/42 , C07C317/44 , C07C317/46 , C07C317/48 , C07C323/22 , C07C381/10 , C07D213/65 , C07D213/89 , C07D231/56 , A61K41/00 , A61P35/00 , C07C43/275 , C07C43/29
CPC分类号: C07D213/85 , A61K31/09 , A61K31/10 , C07B39/00 , C07C43/205 , C07C43/225 , C07C43/23 , C07C43/263 , C07C43/285 , C07C205/22 , C07C255/54 , C07C255/56 , C07C311/29 , C07C313/06 , C07C317/22 , C07C317/24 , C07C317/32 , C07C317/34 , C07C317/36 , C07C317/40 , C07C317/42 , C07C317/44 , C07C317/46 , C07C317/48 , C07C323/22 , C07C381/10 , C07D213/65 , C07D213/89 , C07D231/56 , A61K41/0038 , A61P35/00 , C07C43/275 , C07C43/29 , C07C2602/04 , C07C2602/08 , C07C2602/10 , C07C2603/94
摘要: The present disclosure relates to HIF-2α inhibitors and methods of making and using them for treating cancer. Certain compounds were potent in HIF-2α scintillation proximity assay, luciferase assay, and VEGF ELISA assay, and led to tumor size reduction and regression in 786-O xenograft bearing mice in vivo.
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公开(公告)号:US20210317150A1
公开(公告)日:2021-10-14
申请号:US17338802
申请日:2021-06-04
发明人: Bin Wang , Hanbiao Yang , Karl Bedke , Paul Wehn , James P. Rizzi
IPC分类号: C07F9/6561
摘要: Compounds that modulate CD73 activity, pharmaceutical compositions containing these compounds, and methods of using these compounds for treating diseases associated with CD73 activity are described herein.
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公开(公告)号:US09884843B2
公开(公告)日:2018-02-06
申请号:US15037047
申请日:2014-12-15
发明人: Darryl David Dixon , Jonas Grina , John A. Josey , James P. Rizzi , Stephen T. Schlachter , Eli M. Wallace , Bin Wang , Paul Wehn , Rui Xu , Hanbiao Yang
IPC分类号: C07D333/64 , C07D333/66 , C07D409/12 , C07D333/78 , C07D335/06 , A61K31/381
CPC分类号: C07D333/64 , A61K31/381 , C07D333/66 , C07D333/78 , C07D335/06 , C07D409/12
摘要: The present disclosure relates to cyclic sulfones and sulfoximines that are HIF-2a inhibitors and methods of making and using them for treating cancers. In another aspect, the present disclosure provides a pharmaceutical composition comprising a compound described herein and a pharmaceutically acceptable carrier or excipient. The compound may exist in an amorphous form, a crystalline form, or as a salt, solvate, or hydrate. In another aspect, the present disclosure provides a method of treating renal cell carcinoma by administrating a therapeutically effective amount of a compound described herein or a pharmaceutical composition thereof to a subject in need of such treatment.
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公开(公告)号:US10786480B2
公开(公告)日:2020-09-29
申请号:US16393793
申请日:2019-04-24
发明人: John A. Josey , Eli M. Wallace , Guangzhou Han
IPC分类号: A61K31/277 , A61K45/06 , A61K31/435 , A61P35/00
摘要: The present invention provides methods and pharmaceutical compositions for treating proliferative disorders.
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公开(公告)号:US09969689B2
公开(公告)日:2018-05-15
申请号:US15439308
申请日:2017-02-22
发明人: Darryl David Dixon , Jonas Grina , John A. Josey , James P. Rizzi , Stephen T. Schlachter , Eli M. Wallace , Bin Wang , Paul Wehn , Rui Xu , Hanbiao Yang
IPC分类号: C07C43/29 , C07C43/275 , A61K31/09 , C07D213/85 , C07C317/22 , C07D213/65
CPC分类号: C07D213/85 , A61K31/09 , A61K31/10 , A61K41/0038 , A61P35/00 , C07C43/205 , C07C43/225 , C07C43/23 , C07C43/263 , C07C43/275 , C07C43/285 , C07C43/29 , C07C205/22 , C07C255/54 , C07C255/56 , C07C311/29 , C07C313/06 , C07C317/22 , C07C317/24 , C07C317/32 , C07C317/34 , C07C317/36 , C07C317/40 , C07C317/42 , C07C317/44 , C07C317/46 , C07C317/48 , C07C323/22 , C07C381/10 , C07C2602/04 , C07C2602/08 , C07C2602/10 , C07C2603/94 , C07D213/65 , C07D213/89 , C07D231/56
摘要: The present disclosure relates to HIF-2α inhibitors and methods of making and using them for treating cancer. Certain compounds were potent in HIF-2α scintillation proximity assay, luciferase assay, and VEGF ELISA assay, and led to tumor size reduction and regression in 786-O xenograft bearing mice in vivo.
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公开(公告)号:US20220162193A1
公开(公告)日:2022-05-26
申请号:US17598389
申请日:2020-04-06
发明人: Michelle Ann Estrada , Jonas Grina , Paul Wehn , Rui Xu
IPC分类号: C07D403/12 , C07D405/14 , A61P35/00
摘要: Compounds of formula I, that induce RBM39 protein degradation, pharmaceutical compositions containing these compounds, and methods of using these compounds for treating diseases associated with RBM39 protein activity are described herein.
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公开(公告)号:US10597366B2
公开(公告)日:2020-03-24
申请号:US16164653
申请日:2018-10-18
发明人: Darryl David Dixon , Jonas Grina , John A. Josey , James P. Rizzi , Stephen T. Schlachter , Eli M. Wallace , Bin Wang , Paul Wehn , Rui Xu , Hanbiao Yang
IPC分类号: C07B39/00 , C07C43/295 , A61K31/09 , C07D213/85 , C07C43/285 , C07C43/205 , C07C43/263 , C07C43/23 , C07C43/225 , A61K31/10 , C07C255/54 , C07C255/56 , C07C205/22 , C07C313/06 , C07C317/22 , C07C317/24 , C07C317/32 , C07C317/34 , C07C317/36 , C07C317/40 , C07C317/42 , C07C317/44 , C07C317/46 , C07C317/48 , C07C323/22 , C07C381/10 , C07D213/89 , C07D231/56 , C07D213/65 , C07C311/29 , A61K41/00 , A61P35/00 , C07C43/275 , C07C43/29
摘要: The present disclosure relates to HIF-2α inhibitors and methods of making and using them for treating cancer. Certain compounds were potent in HIF-2α scintillation proximity assay, luciferase assay, and VEGF ELISA assay, and led to tumor size reduction and regression in 786-O xenograft bearing mice in vivo.
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公开(公告)号:US10144711B2
公开(公告)日:2018-12-04
申请号:US15805390
申请日:2017-11-07
发明人: Darryl David Dixon , Jonas Grina , John A. Josey , James P. Rizzi , Stephen T. Schlachter , Eli M. Wallace , Bin Wang , Paul Wehn , Rui Xu , Hanbiao Yang
IPC分类号: A61P35/00 , A61K41/00 , A61K31/09 , C07C43/29 , C07C43/275 , C07D213/85 , C07C43/285 , C07C43/205 , C07C43/263 , C07C43/23 , C07C43/225 , A61K31/10 , C07C255/54 , C07C255/56 , C07C205/22 , C07C311/29 , C07C313/06 , C07C317/22 , C07C317/24 , C07C317/32 , C07C317/34 , C07C317/36 , C07C317/40 , C07C317/42 , C07C317/44 , C07C317/46 , C07C317/48 , C07C323/22 , C07C381/10 , C07D213/89 , C07D231/56 , C07D213/65
摘要: The present disclosure relates to HIF-2α inhibitors and methods of making and using them for treating cancer. Certain compounds were potent in HIF-2α scintillation proximity assay, luciferase assay, and VEGF ELISA assay, and led to tumor size reduction and regression in 786-O xenograft bearing mice in vivo.
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公开(公告)号:US20240294548A1
公开(公告)日:2024-09-05
申请号:US18681173
申请日:2022-09-14
发明人: James P. Rizzi , Paul Wehn
IPC分类号: C07D513/04 , A61K31/542 , A61K31/549
CPC分类号: C07D513/04 , A61K31/542 , A61K31/549
摘要: Compounds of formula I, that modulate DCAF15 and induce RBM39 protein degradation, pharmaceutical compositions containing these compounds, and methods of using these compounds for treating diseases associated with RBM39 protein activity and DCAF15 modulation are described herein.
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公开(公告)号:US20210387946A1
公开(公告)日:2021-12-16
申请号:US17286581
申请日:2019-10-23
IPC分类号: C07C317/22 , A61K9/20
摘要: Provided herein are solid dispersions comprising a HIF-2α inhibitor, pharmaceutical compositions comprising the solid dispersions, and methods for treating HIF-2α-mediated diseases and conditions.
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