-
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.
-
公开(公告)号:US10155726B2
公开(公告)日:2018-12-18
申请号:US15553570
申请日:2016-03-04
发明人: Paul Wehn , Rui Xu , Hanbiao Yang
IPC分类号: C07D221/18 , A61K45/06 , A61K31/438 , C07D401/12 , C07D237/26 , A61P43/00 , A61P35/00
摘要: Substituted pyridines that modulate HIF-2a activity, pharmaceutical compositions containing the substituted pyridines, and methods of using these chemical entities for treating proliferative diseases and conditions associated with HIF-2a activity are described herein.
-
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.
-
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.
-
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.
-
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.
-
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.
-
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.
-
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.
-
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.
-
-
-
-
-
-
-
-
-