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公开(公告)号：US10040767B2
公开(公告)日：2018-08-07
申请号：US15310429
申请日：2015-05-14
发明人： Darryl David Dixon , Jonas Grina , John A. Josey , James P. Rizzi , Stephen T. Schlachter , Eli M. Wallace , Bin Wang , Paul Wehn , Hanbiao Yang
IPC分类号： C07D487/04 , C07D235/12 , C07D401/06 , C07D403/12 , A61K31/4184 , A61K31/4188 , A61P35/00
摘要： Benzimidazole derivatives of Formula I, that modulate the activity of ACSS2 are disclosed for therapeutic use. The fused imidazole ring of the compounds disclosed has a diarylmethyl or diarylmethanol moiety attached at the 2-position and the as compounds have at least one other substituent at the 5 or 6 position of the benzimidazole. Also disclosed are methods of using the benzimidazole compounds for the treatment of diseases or disorders, such as cancer.
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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：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：US20170217891A1
公开(公告)日：2017-08-03
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： C07D213/85 , C07D213/65 , C07C317/22
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：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：US20180155279A1
公开(公告)日：2018-06-07
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： C07C311/29 , C07D231/56 , C07D213/89 , A61K31/09 , A61K31/10 , C07C43/205 , C07D213/85 , C07D213/65 , C07C381/10 , C07C323/22 , C07C317/48 , C07C317/46 , C07C317/44 , C07C317/42 , C07C317/40 , C07C317/36 , C07C317/34 , C07C317/32 , C07C317/24 , C07C317/22 , C07C313/06 , C07C255/56 , C07C255/54 , C07C205/22 , C07C43/285 , C07C43/263 , C07C43/23 , C07C43/225
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：US20190119214A1
公开(公告)日：2019-04-25
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： C07D213/85 , A61K31/10 , C07C255/56 , A61K31/09 , C07C205/22 , C07C311/29 , C07C313/06 , C07D213/89 , C07D231/56 , C07D213/65 , C07C255/54 , C07C43/225 , C07C43/23 , C07C43/263 , C07C43/205 , C07C43/285 , C07C381/10 , C07C323/22 , C07C317/48 , C07C317/46 , C07C317/44 , C07C317/42 , C07C317/40 , C07C317/36 , C07C317/34 , C07C317/32 , C07C317/24 , C07C317/22
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：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：US20170217892A1
公开(公告)日：2017-08-03
申请号：US15439494
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： C07D213/85 , C07C317/22 , C07C317/36 , C07C381/10
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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