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公开(公告)号：US20210214323A1
公开(公告)日：2021-07-15
申请号：US17187061
申请日：2021-02-26
发明人： Kenneth W. Bair , David R. Lancia, JR. , Hongbin LI , James Loch , Wei Lu , Matthew W. Martin , David S. Millan , Shawn E.R. Schiller , Mark J. Tebbe
IPC分类号： C07D295/192 , A61K45/06 , C07D215/14 , C07D231/56 , C07D405/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D257/04 , C07D487/04 , C07D263/57 , C07D491/048 , C07D271/12 , C07D495/04 , C07D209/18 , C07D277/62 , C07D277/66 , C07D513/04 , C07D213/56 , C07D305/08 , A61K31/4965 , A61P35/00 , A61K31/495 , A61K31/496 , A61K31/497 , A61K31/4985 , A61K31/5025 , A61K31/506 , C07D209/08 , C07D213/65 , C07D213/69 , C07D217/16 , C07D231/12 , C07D235/08 , C07D401/04 , C07D403/04 , C07D417/04
摘要： The present invention relates to compounds and composition for inhibition of FASN, their synthesis, applications, and antidotes. An illustrative compound of the invention is shown below:
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公开(公告)号：US20200347025A1
公开(公告)日：2020-11-05
申请号：US15929751
申请日：2020-05-20
发明人： Kenneth W. Bair , David R. Lancia, JR. , Hongbin Li , James Loch , Wei Lu , Matthew W. Martin , David S. Millan , Shawn E.R. Schiller , Mark J. Tebbe
IPC分类号： C07D295/192 , A61K45/06 , C07D215/14 , C07D231/56 , C07D405/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D257/04 , C07D487/04 , C07D263/57 , C07D491/048 , C07D271/12 , C07D495/04 , C07D209/18 , C07D277/62 , C07D277/66 , C07D513/04 , C07D213/56 , C07D305/08 , A61K31/4965 , A61P35/00 , A61K31/495 , A61K31/496 , A61K31/497 , A61K31/4985 , A61K31/5025 , A61K31/506 , C07D209/08 , C07D213/65 , C07D213/69 , C07D217/16 , C07D231/12 , C07D235/08 , C07D401/04 , C07D403/04 , C07D417/04
摘要： The present invention relates to compounds and composition for inhibition of FASN, their synthesis, applications, and antidotes. An illustrative compound of the invention is shown below:
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公开(公告)号：US20200017458A1
公开(公告)日：2020-01-16
申请号：US16566119
申请日：2019-09-10
发明人： Kenneth W. Bair , David R. Lancia, JR. , Hongbin LI , James Loch , Wei Lu , Matthew W. Martin , David S. Millan , Shawn E.R. Schiller , Mark J. Tebbe
IPC分类号： C07D295/192 , C07D417/04 , C07D403/04 , C07D401/04 , C07D235/08 , C07D231/12 , C07D217/16 , C07D213/69 , C07D213/65 , C07D209/08 , A61K31/506 , A61K31/5025 , A61K31/4985 , A61K31/497 , A61K31/496 , A61K31/495 , A61K31/4965 , C07D305/08 , C07D213/56 , C07D513/04 , C07D277/66 , C07D277/62 , C07D209/18 , C07D495/04 , C07D271/12 , C07D491/048 , C07D263/57 , C07D487/04 , C07D257/04 , C07D471/04 , C07D417/12 , C07D413/12 , C07D405/12 , C07D231/56 , C07D215/14 , A61K45/06
摘要： The present invention relates to compounds and composition for inhibition of FASN, their synthesis, applications, and antidotes. An illustrative compound of the invention is shown below:
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公开(公告)号：US20190330233A1
公开(公告)日：2019-10-31
申请号：US16444032
申请日：2019-06-18
发明人： Kenneth W. Bair , Torsten Herbertz , Goss S. Kauffman , Katherine J. Kayser-Bricker , George P. Luke , Matthew W. Martin , David S. Millan , Shawn E.R. Schiller , Adam C. Talbot , Mark J. Tebbe
IPC分类号： C07D498/04 , A61K31/553 , C07D401/14 , A61K31/506 , A61K31/517 , A61K31/551 , A61K31/541 , A61K31/5377 , A61K31/519 , A61K31/5025 , C07D495/04 , C07D491/048 , C07D487/08 , C07D487/04 , C07D471/04 , C07D451/04 , C07D241/50 , C07D417/06 , C07D417/04 , C07D413/12 , C07D413/06 , C07D409/12 , C07D409/06 , C07D405/12 , C07D405/10 , C07D405/04 , C07D403/06 , C07D401/12 , C07D401/10 , C07D401/06 , A61K31/53 , C07D403/12 , A61K31/498 , A61K45/06 , C07D417/14 , C07D417/10 , C07D241/42 , C07D413/04 , C07D409/14 , C07D405/06 , C07D403/14 , C07D403/10 , C07D403/04 , C07D401/04 , A61K31/4985 , C07D413/14 , C07D405/14 , A61K31/55
摘要： The present invention relates to inhibitors of bromo and extra terminal (BET) bromodomains that are useful for the treatment of cancer, inflammatory diseases, diabetes, and obesity, having Formula (I): wherein X, Y, Z, R1, R2, R4 and R7 are defined herein.
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![3-alkyl-4-amido-bicyclic [4,5,0] hydroxamic acids as HDAC inhibitors](/abs-image/US/2019/10/29/US10457652B2/abs.jpg.150x150.jpg)
公开(公告)号：US10457652B2
公开(公告)日：2019-10-29
申请号：US16219648
申请日：2018-12-13
发明人： Xiaozhang Zheng , Pui Yee Ng , Bingsong Han , Jennifer R. Thomason , Mary-Margaret Zablocki , Cuixian Liu , Heather Davis , Aleksandra Rudnitskaya , David R. Lancia, Jr. , Kenneth W. Bair , David S. Millan , Matthew W. Martin
IPC分类号： A61K31/5513 , C07D243/14 , C07D401/06 , C07D401/10 , C07D403/06 , C07D403/10 , C07D413/06 , C07D417/06 , C07D267/14 , C07D413/12 , C07D413/04 , C07D291/08 , C07D405/06 , C07D413/14 , C07D417/04 , C07D471/04 , C07D498/04 , C07D498/08 , C07D493/08 , C07D413/08 , C07D491/107 , C07D495/10 , C07D267/12
摘要： The present disclosure relates to inhibitors of zinc-dependent histone deacetylases (HDACs) useful in the treatment of diseases or disorders associated with an HDAC, e.g., HDAC6, having a Formula I: where R, L, X1, X2, X3, X4, Y1, Y2, Y3, and Y4 are described herein.
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![3-ALKYL-4-AMIDO-BICYCLIC [4,5,0] HYDROXAMIC ACIDS AS HDAC INHIBITORS](/abs-image/US/2019/04/25/US20190119228A1/abs.jpg.150x150.jpg)
公开(公告)号：US20190119228A1
公开(公告)日：2019-04-25
申请号：US16219592
申请日：2018-12-13
发明人： Xiaozhang Zheng , Pui Yee Ng , Bingsong Han , Jennifer R. Thomason , Mary-Margaret Zablocki , Cuixian Liu , Heather Davis , Aleksandra Rudnitskaya , David R. Lancia, Jr. , Kenneth W. Bair , David S. Millan , Matthew W. Martin
IPC分类号： C07D267/14 , C07D413/04 , C07D267/12 , C07D413/06 , C07D401/06 , C07D417/04 , C07D471/04 , C07D498/04 , C07D243/14 , C07D291/08 , C07D498/08 , C07D401/10 , C07D403/06 , C07D403/10 , C07D405/06 , C07D413/14 , C07D495/10 , C07D491/107 , C07D413/08 , C07D493/08 , C07D413/12
摘要： The present disclosure relates to inhibitors of zinc-dependent histone deacetylases (HDACs) useful in the treatment of diseases or disorders associated with an HDAC, e.g., HDAC6, having a Formula I: where R, L, X1, X2, X3, X4, Y1, Y2, Y3, and Y4 are described herein.
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公开(公告)号：US10266487B2
公开(公告)日：2019-04-23
申请号：US15925559
申请日：2018-03-19
发明人： Kenneth W. Bair , Nicholas Barczak , Bingsong Han , David R. Lancia, Jr. , Cuixian Liu , Matthew W. Martin , Pui Yee Ng , Aleksandra Rudnitskaya , Jennifer R. Thomason , Mary-Margaret Zablocki , Xiaozhang Zheng
IPC分类号： C07C259/06 , C07D209/46 , C07D213/75 , C07D213/81 , C07D215/12 , C07D317/68 , C07D231/14 , C07D231/18 , C07D233/36 , C07D233/38 , C07D333/70 , C07D401/04 , C07D401/12 , C07D235/30 , C07D239/20 , C07D239/22 , C07D405/12 , C07D409/04 , C07D409/12 , C07D241/12 , C07D417/12 , C07D249/18 , C07D257/04 , C07D261/18 , C07D401/14 , C07D487/04 , C07D487/08 , C07D307/68 , C07D213/65 , C07D295/192 , C07D211/58 , C07D211/16 , C07D513/10 , C07D491/10 , C07D209/42 , C07D277/56 , C07D209/08 , C07D498/04 , C07D207/267 , C07D493/08 , C07D207/10 , A61K31/407 , A61K31/5377 , C07D495/10 , A61K31/185 , A61K31/438 , A61K31/277 , C07D209/44 , A61K31/4035 , C07D295/155 , A61K31/451 , C07D471/10 , A61K31/435 , C07D487/10 , C07D221/20 , A61K31/397 , C07D235/14 , A61K31/4184 , C07D233/68 , A61K31/417 , C07D213/56 , A61K31/44 , C07D241/08 , A61K31/495 , C07D417/04 , A61K31/4439 , C07D471/04
摘要： The present invention relates to inhibitors of histone deacetylases, in particular HDAC8, that are useful for the treatment of cancer and other diseases and disorders, as well as the synthesis and applications of said inhibitors.
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![3-ALKYL BICYCLIC [4,5,0] HYDROXAMIC ACIDS AS HDAC INHIBITORS](/abs-image/US/2019/04/18/US20190112283A1/abs.jpg.150x150.jpg)
公开(公告)号：US20190112283A1
公开(公告)日：2019-04-18
申请号：US16218132
申请日：2018-12-12
发明人： Xiaozhang Zheng , Pui Yee Ng , Bingsong Han , Jennifer R. Thomason , Mary-Margaret Zablocki , Cuixian Liu , Aleksandra Rudnitskaya , David R. Lancia, JR. , David S. Millan , Matthew W. Martin , Kenneth W. Bair
IPC分类号： C07D267/14 , C07D413/04 , C07D267/12 , C07D413/06 , C07D401/06 , C07D417/04 , C07D471/04 , C07D498/04 , C07D243/14 , C07D291/08 , C07D498/08 , C07D401/10 , C07D403/06 , C07D403/10 , C07D405/06 , C07D413/14 , C07D495/10 , C07D491/107 , C07D413/08 , C07D493/08 , C07D413/12
摘要： The present disclosure relates to inhibitors of zinc-dependent histone deacetylases (HDACs) useful in the treatment of diseases or disorders associated with an HDAC, e.g., HDAC6, having a Formula I: where R, L, X1, X2, X3, X4, Y1, Y2, Y3, and Y4 are described herein.
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公开(公告)号：US20180297939A1
公开(公告)日：2018-10-18
申请号：US15925559
申请日：2018-03-19
发明人： Kenneth W. Bair , Nicholas Barczak , Bingsong Han , David R. Lancia, JR. , Cuixian Liu , Matthew W. Martin , Pui Yee Ng , Aleksandra Rudnitskaya , Jennifer R. Thomason , Mary-Margaret Zablocki , Xiaozhang Zheng
IPC分类号： C07C259/06 , C07D471/04 , C07D417/04 , C07D241/08 , C07D213/56 , C07D233/68 , C07D235/14 , C07D487/10 , C07D471/10 , C07D295/155 , C07D209/44 , A61K31/5377 , A61K31/4439 , A61K31/495 , A61K31/44 , A61K31/417 , A61K31/4184 , A61K31/397 , C07D495/10 , A61K31/407 , A61K31/435 , A61K31/451 , A61K31/4035 , A61K31/277 , A61K31/438 , C07D221/20 , A61K31/185 , C07D307/68 , C07D213/65 , C07D295/192 , C07D211/58 , C07D211/16 , C07D513/10 , C07D209/46 , C07D209/42 , C07D277/56 , C07D209/08 , C07D498/04 , C07D207/267 , C07D493/08 , C07D207/10 , C07D491/10 , C07D487/08 , C07D487/04 , C07D261/18 , C07D257/04 , C07D249/18 , C07D417/12 , C07D241/12 , C07D409/12 , C07D409/04 , C07D405/12 , C07D239/22 , C07D239/20 , C07D235/30 , C07D401/12 , C07D401/04 , C07D333/70 , C07D233/38 , C07D233/36 , C07D231/18 , C07D231/14 , C07D317/68 , C07D215/12 , C07D213/81 , C07D213/75 , C07D401/14
CPC分类号： C07C259/06 , A61K31/185 , A61K31/277 , A61K31/397 , A61K31/4035 , A61K31/407 , A61K31/417 , A61K31/4184 , A61K31/435 , A61K31/438 , A61K31/44 , A61K31/4439 , A61K31/451 , A61K31/495 , A61K31/5377 , C07D207/10 , C07D207/267 , C07D209/08 , C07D209/42 , C07D209/44 , C07D209/46 , C07D211/16 , C07D211/58 , C07D213/56 , C07D213/65 , C07D213/75 , C07D213/81 , C07D215/12 , C07D221/20 , C07D231/14 , C07D231/18 , C07D233/36 , C07D233/38 , C07D233/68 , C07D235/14 , C07D235/30 , C07D239/20 , C07D239/22 , C07D241/08 , C07D241/12 , C07D249/18 , C07D257/04 , C07D261/18 , C07D277/56 , C07D295/155 , C07D295/192 , C07D307/68 , C07D317/68 , C07D333/70 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/04 , C07D409/12 , C07D417/04 , C07D417/12 , C07D471/04 , C07D471/10 , C07D487/04 , C07D487/08 , C07D487/10 , C07D491/10 , C07D493/08 , C07D495/10 , C07D498/04 , C07D513/10 , Y02A50/393 , Y02A50/411 , Y02A50/481
摘要： The present invention relates to inhibitors of histone deacetylases, in particular HDAC8, that are useful for the treatment of cancer and other diseases and disorders, as well as the synthesis and applications of said inhibitors.
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公开(公告)号：US09630922B2
公开(公告)日：2017-04-25
申请号：US15130613
申请日：2016-04-15
发明人： Pui Yee Ng , Heather Davis , Kenneth W. Bair , David S. Millan , Aleksandra Rudnitskaya , Xiaozhang Zheng , Bingsong Han , Nicholas Barczak , David R. Lancia, Jr.
IPC分类号： C07D221/20 , C07D403/04 , C07D209/96 , C07D401/04 , C07D417/06 , C07D519/00 , C07D401/06 , C07D413/06 , C07D405/04 , C07D471/04 , C07D497/10 , C07D491/107 , C07D405/06 , C07D403/06 , C07D405/10
CPC分类号： C07D209/96 , C07D221/20 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/06 , C07D405/04 , C07D405/06 , C07D405/10 , C07D413/06 , C07D417/06 , C07D471/04 , C07D491/107 , C07D497/10 , C07D519/00
摘要： The present invention is directed to inhibitors of histone deacetylases (HDACs) such as HDAC6, and their use in the treatment of diseases such as cell proliferative diseases (e.g., cancer), neurological (e.g., neurodegenerative disease or neurodevelopmental disease), inflammatory or autoimmune disease, infection, metabolic disease, hematologic disease, or cardiovascular disease.
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