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公开(公告)号：US11827639B2
公开(公告)日：2023-11-28
申请号：US16626191
申请日：2018-06-28
发明人： Zhonghua Pei , Brendan Parr , Wendy Liu , Richard Pastor , Lewis Gazzard , Firoz Jaipuri , Sanjeev Kumar , Hima Potturi , Guoshen Wu , Xingyu Lin , Yanyan Chu , Powai Yuen
IPC分类号： C07D487/04 , A61K31/4188 , A61K31/438 , A61K31/439 , A61K31/4439 , A61K31/454 , A61K31/437 , A61K31/4725 , A61K31/5377 , A61K45/06
CPC分类号： C07D487/04
摘要： Presently provided are inhibitors of TD02 and IDO1 and pharmaceutical compositions thereof, useful for modulating an activity of tryptophan 2,3 dioxygenase and indoleamine 2,3-dioxygenase 1; treating immunosuppression; treating a medical conditions that benefit from the inhibition of tryptophan degradation; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; and treating tumor-specific immunosuppression associated with cancer.
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公开(公告)号：US10800780B2
公开(公告)日：2020-10-13
申请号：US16065397
申请日：2016-12-23
发明人： Xingyu Lin , Po-wai Yuen , Rohan Mendonca , Brendan Parr , Richard Pastor , Zhonghua Pei , Lewis Gazzard , Firoz Jaipuri , Sanjeev Kumar , Xiaokai Li , Roheeth Pavana , Hima Potturi , Venkata Velvadapu , Jesse Waldo , Zuhui Zhang , Guosheng Wu , Benjamin Douglas Sellers
IPC分类号： A61K31/4188 , A61K31/407 , A61K31/4035 , C07D487/04 , C07D519/00 , A61P35/00 , A61K45/06 , A61K38/16
摘要： Presently provided are inhibitors of cellularly expressed TDO2 and pharmaceutical compositions thereof, useful for modulating an activity of tryptophan 2, 3 dioxygenase; treating immunosuppression; treating a medical conditions that benefit from the inhibition of tryptophan degradation; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; and treating tumor-specific immunosuppression associated with cancer.
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公开(公告)号：US20220306635A1
公开(公告)日：2022-09-29
申请号：US17068574
申请日：2020-10-12
发明人： Xingyu Lin , Po-wai Yuen , Rohan Mendonca , Brendan Parr , Richard Pastor , Zhonghua Pei , Lewis Gazzard , Firoz Jaipuri , Sanjeev Kumar , Xiaokai Li , Roheeth Pavana , Hima Potturi , Venkata Velvadapu , Jesse Waldo , Zuhui Zhang , Guosheng Wu , Benjamin Douglas Sellers
IPC分类号： C07D487/04 , A61P35/00 , A61K38/16 , A61K45/06 , C07D519/00
摘要： Presently provided are inhibitors of cellularly expressed TD02 and pharmaceutical compositions thereof, useful for modulating an activity of tryptophan 2, 3 dioxygenase; treating immunosuppression; treating a medical conditions that benefit from the inhibition of tryptophan degradation; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; and treating tumor-specific immunosuppression associated with cancer.
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公开(公告)号：US20190016726A1
公开(公告)日：2019-01-17
申请号：US16065397
申请日：2016-12-23
发明人： Xingyu Lin , Po-wai Yuen , Rohan Mendonca , Brendan Parr , Richard Pastor , Zhonghua Pei , Lewis Gazzard , Firoz Jaipuri , Sanjeev Kumar , Xiaokai Li , Roheeth Pavana , Hima Potturi , Venkata Velvadapu , Jesse Waldo , Zuhui Zhang , Guosheng Wu
IPC分类号： C07D487/04 , A61P35/00 , C07D519/00 , A61K38/16
摘要： Presently provided are inhibitors of cellularly expressed TDO2 and pharmaceutical compositions thereof, useful for modulating an activity of tryptophan 2, 3 dioxygenase; treating immunosuppression; treating a medical conditions that benefit from the inhibition of tryptophan degradation; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; and treating tumor-specific immunosuppression associated with cancer.
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公开(公告)号：US20240132507A1
公开(公告)日：2024-04-25
申请号：US18496146
申请日：2023-10-27
发明人： Zhonghua Pei , Brendan Parr , Wendy Liu , Richard Pastor , Lewis Gazzard , Firoz Jaipuri , Sanjeev Kumar , Hima Potturi , Guoshen Wu , Xingyu Lin , Yanyan Chu , Po-wai Yuen
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： Presently provided are inhibitors of TD02 and IDO1 and pharmaceutical compositions thereof, useful for modulating an activity of tryptophan 2,3 dioxygenase and indoleamine 2,3-dioxygenase 1; treating immunosuppression; treating a medical conditions that benefit from the inhibition of tryptophan degradation; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; and treating tumor-specific immunosuppression associated with cancer.
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公开(公告)号：US20200216456A1
公开(公告)日：2020-07-09
申请号：US16626191
申请日：2018-06-28
发明人： Zhonghua Pei , Brendan Parr , Wendy Liu , Richard Pastor , Lewis Gazzard , Firoz Jaipuri , Sanjeev Kumar , Hima Potturi , Guoshen Wu , Xingyu Lin , Yanyan Chu , Powai Yuen
IPC分类号： C07D487/04
摘要： Presently provided are inhibitors of TD02 and IDOl and pharmaceutical compositions thereof, useful for modulating an activity of tryptophan 2,3 dioxygenase and indoleamine 2,3-dioxygenase 1; treating immunosuppression; treating a medical conditions that benefit from the inhibition of tryptophan degradation; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; and treating tumor-specific immunosuppression associated with cancer.
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公开(公告)号：US20160185797A1
公开(公告)日：2016-06-30
申请号：US15060325
申请日：2016-03-03
申请人： Genentech, Inc.
发明人： Nicole Blaquiere , Georgette Castanedo , Jianwen A. Feng , Baihua Hu , Steven Staben , Po-wai Yuen , Guosheng Wu , Xingyu Lin , Jason Burch
IPC分类号： C07D495/04 , C07D403/10 , C07D403/14 , C07D491/107 , C07D409/14 , C07D417/14 , C07D487/04 , C07D401/14 , C07D471/04 , C07D413/10 , C07D405/10 , C07D401/10 , C07D405/14
CPC分类号： C07D401/10 , A61K31/395 , C07D401/14 , C07D403/10 , C07D403/14 , C07D405/10 , C07D405/14 , C07D409/14 , C07D413/10 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D491/048 , C07D491/107 , C07D495/04 , C07D495/06
摘要： The invention relates to compounds of Formula (0): wherein A1-A8, R4 and R5 each has the meaning as described herein. Compounds of Formula (0) and pharmaceutical compositions thereof are useful in the treatment of diseases and disorders in which undesired or over-activation of NF-kB signaling is observed.
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公开(公告)号：US20150057260A1
公开(公告)日：2015-02-26
申请号：US14466176
申请日：2014-08-22
申请人： Genentech, Inc.
发明人： Nicole Blaquiere , Georgette Castanedo , Jianwen A. Feng , Baihua Hu , Steven Staben , Po-wai Yuen , Guosheng Wu , Xingyu Lin , Jason Burch
IPC分类号： C07D495/04 , C07D403/10 , C07D405/14 , C07D409/14 , C07D491/107 , C07D403/14 , C07D401/10
CPC分类号： C07D401/10 , A61K31/395 , C07D401/14 , C07D403/10 , C07D403/14 , C07D405/10 , C07D405/14 , C07D409/14 , C07D413/10 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D491/048 , C07D491/107 , C07D495/04 , C07D495/06
摘要： The invention relates to compounds of Formula (0): wherein A1-A8, R4 and R5 each has the meaning as described herein. Compounds of Formula (0) and pharmaceutical compositions thereof are useful in the treatment of diseases and disorders in which undesired or over-activation of NF-kB signaling is observed.
摘要翻译： 本发明涉及式（O）的化合物：其中A1-A8，R4和R5各自具有如本文所述的含义。 式（0）的化合物及其药物组合物可用于治疗其中观察到NF-kB信号传导的不期望或过度活化的疾病和病症。
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公开(公告)号：US20170210724A1
公开(公告)日：2017-07-27
申请号：US15481852
申请日：2017-04-07
申请人： Genentech, Inc.
发明人： Nicole Blaquiere , Georgette Castanedo , Jianwen A. Feng , Baihua Hu , Steven Staben , Po-wai Yuen , Guosheng Wu , Xingyu Lin , Jason Burch
IPC分类号： C07D401/10 , C07D401/14 , C07D491/107 , C07D409/14 , C07D405/14 , C07D495/04 , C07D495/06 , C07D471/04 , C07D487/04 , C07D413/10 , C07D403/10 , C07D405/10 , C07D417/14 , C07D491/048 , C07D413/14
CPC分类号： C07D401/10 , A61K31/395 , C07D401/14 , C07D403/10 , C07D403/14 , C07D405/10 , C07D405/14 , C07D409/14 , C07D413/10 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D491/048 , C07D491/107 , C07D495/04 , C07D495/06
摘要： The invention relates to compounds of Formula (0): wherein A1-A8, R4 and R5 each has the meaning as described herein. Compounds of Formula (0) and pharmaceutical compositions thereof are useful in the treatment of diseases and disorders in which undesired or over-activation of NF-kB signaling is observed.
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公开(公告)号：US11236046B2
公开(公告)日：2022-02-01
申请号：US16657102
申请日：2019-10-18
申请人： Genentech, Inc.
发明人： Huifen Chen , Yanyan Chu , Steven Do , Anthony Estrada , Baihua Hu , Aleksandr Kolesnikov , Xingyu Lin , Joseph P. Lyssikatos , Daniel Shore , Vishal Verma , Lan Wang , Guosheng Wu , Po-wai Yuen
IPC分类号： C07D207/48 , C07D403/12 , C07D401/14 , C07D401/12 , C07D403/14 , C07D417/12 , C07D451/02 , C07D491/048 , C07D405/14
摘要： The invention is concerned with the compounds of formula I or II: and salts thereof. In addition, the present invention relates to methods of manufacturing and methods of using the compounds of formula I or II as well as pharmaceutical compositions containing such compounds. The compounds may be useful in treating diseases and conditions mediated by TRPA1, such as pain.
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