公开(公告)号：US09580398B2

公开(公告)日：2017-02-28

申请号：US14390256

申请日：2013-04-02

申请人： The Trustees of Columbia University in the City of New York

发明人： Brent R. Stockwell ,  Scott J. Dixon ,  Rachid Skouta

IPC分类号： C07D213/80 ,  C07C211/50 ,  A61K31/44 ,  A61K31/245 ,  C07D309/14 ,  C07C255/58 ,  C07C271/16 ,  C07C271/24 ,  C07C271/28 ,  C07C205/57 ,  C07C205/58 ,  C07D401/12 ,  C07D239/26 ,  C07C229/60 ,  C07C233/54 ,  C07C237/30 ,  C07D295/088 ,  C07D211/58 ,  C07D295/30 ,  C07D213/36 ,  A61K31/325 ,  A61K31/351 ,  A61K31/4465 ,  A61K31/495 ,  A61K31/5375 ,  A61K45/06 ,  C07C69/78 ,  C07D295/192

CPC分类号： C07D401/12 ,  A61K31/245 ,  A61K31/27 ,  A61K31/325 ,  A61K31/351 ,  A61K31/44 ,  A61K31/444 ,  A61K31/4465 ,  A61K31/4468 ,  A61K31/495 ,  A61K31/505 ,  A61K31/506 ,  A61K31/5375 ,  A61K45/06 ,  C07C69/78 ,  C07C205/57 ,  C07C205/58 ,  C07C211/50 ,  C07C225/22 ,  C07C229/60 ,  C07C233/54 ,  C07C237/30 ,  C07C255/58 ,  C07C271/16 ,  C07C271/24 ,  C07C271/28 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/18 ,  C07C2601/20 ,  C07C2603/74 ,  C07D211/58 ,  C07D213/36 ,  C07D213/74 ,  C07D213/80 ,  C07D239/26 ,  C07D239/42 ,  C07D295/088 ,  C07D295/192 ,  C07D295/30 ,  C07D309/14

摘要： The present invention provides, inter alia, a compound having the structure: (Formula (I). Also provided are compositions containing a pharmaceutically acceptable carrier and a compound according to the present invention. Further provided are methods for treating or ameliorating the effects of an excitotoxic disorder in a subject, methods of modulating ferroptosis in a subject, methods of reducing reactive oxygen species (ROS) in a cell, and methods for treating or ameliorating the effects of a neurodegenerative disease.

摘要翻译： 本发明尤其提供具有以下结构的化合物：（式（I）），还提供含有药学上可接受的载体和本发明化合物的组合物，还提供了治疗或改善 受试者中的兴奋性毒性障碍，受试者中的热of症调节方法，还原细胞中的活性氧（ROS）的方法，以及治疗或改善神经变性疾病的作用的方法。

公开(公告)号：US10947188B2

公开(公告)日：2021-03-16

申请号：US16445104

申请日：2019-06-18

申请人： THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK

发明人： Brent R. Stockwell ,  Kenichi Shimada ,  Rachid Skouta

IPC分类号： C07C311/15 ,  C07D401/12 ,  C07D407/12

摘要： The present invention provides, inter alia, a compound according to formula (I): Also provided are compositions containing a pharmaceutically acceptable carrier and a compound according to the present invention. Further provided are methods for regulating GPX4 in a cell and methods for inducing ferroptosis in a cell.

公开(公告)号：US10597381B2

公开(公告)日：2020-03-24

申请号：US16247354

申请日：2019-01-14

申请人： THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK

发明人： Brent R. Stockwell ,  Scott J. Dixon ,  Rachid Skouta

IPC分类号： C07C225/22 ,  C07C69/78 ,  A61K31/245 ,  C07D401/12 ,  C07C255/58 ,  C07D213/80 ,  C07C271/16 ,  C07C271/24 ,  C07C271/28 ,  C07C205/57 ,  C07C205/58 ,  C07C211/50 ,  C07D239/26 ,  C07C229/60 ,  C07C233/54 ,  C07C237/30 ,  C07D295/088 ,  C07D211/58 ,  C07D295/30 ,  C07D213/36 ,  C07D309/14 ,  A61K31/325 ,  A61K31/351 ,  A61K31/4465 ,  A61K31/495 ,  A61K31/5375 ,  A61K45/06 ,  C07D295/192 ,  A61K31/27 ,  A61K31/44 ,  A61K31/444 ,  A61K31/4468 ,  A61K31/505 ,  A61K31/506 ,  C07D213/74 ,  C07D239/42

摘要： The present invention provides, inter alia, a compound having the structure: Also provided are compositions containing a pharmaceutically acceptable carrier and a compound according to the present invention. Further provided are methods for treating or ameliorating the effects of an excitotoxic disorder in a subject, methods of modulating ferroptosis in a subject, methods of reducing reactive oxygen species (ROS) in a cell, and methods for treating or ameliorating the effects of a neurodegenerative disease.

公开(公告)号：US20190135782A1

公开(公告)日：2019-05-09

申请号：US16247354

申请日：2019-01-14

申请人： THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK

发明人： Brent R. Stockwell ,  Scott J. Dixon ,  Rachid Skouta

IPC分类号： C07D401/12 ,  A61K31/245 ,  C07D213/80 ,  C07C271/16 ,  C07C271/24 ,  C07C271/28 ,  C07C205/57 ,  C07C205/58 ,  C07C225/22 ,  A61K31/444 ,  A61K31/4468 ,  A61K31/505 ,  A61K31/506 ,  C07D239/42 ,  C07D213/74 ,  A61K31/27 ,  A61K31/44 ,  C07D309/14 ,  A61K31/325 ,  A61K45/06 ,  C07C69/78 ,  C07C255/58 ,  C07D295/192 ,  A61K31/351 ,  A61K31/4465 ,  A61K31/495 ,  A61K31/5375 ,  C07D213/36 ,  C07D295/30 ,  C07D211/58 ,  C07D295/088 ,  C07C237/30 ,  C07C233/54 ,  C07C229/60 ,  C07D239/26 ,  C07C211/50

CPC分类号： C07D401/12 ,  A61K31/245 ,  A61K31/27 ,  A61K31/325 ,  A61K31/351 ,  A61K31/44 ,  A61K31/444 ,  A61K31/4465 ,  A61K31/4468 ,  A61K31/495 ,  A61K31/505 ,  A61K31/506 ,  A61K31/5375 ,  A61K45/06 ,  C07C69/78 ,  C07C205/57 ,  C07C205/58 ,  C07C211/50 ,  C07C225/22 ,  C07C229/60 ,  C07C233/54 ,  C07C237/30 ,  C07C255/58 ,  C07C271/16 ,  C07C271/24 ,  C07C271/28 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/18 ,  C07C2601/20 ,  C07C2603/74 ,  C07D211/58 ,  C07D213/36 ,  C07D213/74 ,  C07D213/80 ,  C07D239/26 ,  C07D239/42 ,  C07D295/088 ,  C07D295/192 ,  C07D295/30 ,  C07D309/14

摘要： The present invention provides, inter alia, a compound having the structure: Also provided are compositions containing a pharmaceutically acceptable carrier and a compound according to the present invention. Further provided are methods for treating or ameliorating the effects of an excitotoxic disorder in a subject, methods of modulating ferroptosis in a subject, methods of reducing reactive oxygen species (ROS) in a cell, and methods for treating or ameliorating the effects of a neurodegenerative disease.

公开(公告)号：US10259775B2

公开(公告)日：2019-04-16

申请号：US15100967

申请日：2014-12-01

申请人： THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK

发明人： Brent R. Stockwell ,  Rachid Skouta ,  Scott Dixon

IPC分类号： C07C229/56 ,  A61K31/245 ,  A61K45/06 ,  A61K31/196 ,  A61K31/505 ,  C07C255/58 ,  C07C271/24 ,  C07C229/60 ,  C07D401/12 ,  C07D239/26 ,  C07D213/38

摘要： The present invention provides, inter alia, a compound having the structure of Formula (I). Also provided are compositions containing a pharmaceutically acceptable carrier and a compound according to the present invention. Further provided are methods for treating or ameliorating the effects of an excitotoxic disorder in a subject, methods of modulating ferroptosis in a subject, methods of reducing reactive oxygen species (ROS) in a cell, and methods for treating or ameliorating the effects of a neurodegenerative disease.

公开(公告)号：US20150079035A1

公开(公告)日：2015-03-19

申请号：US14390256

申请日：2013-04-02

申请人： The Trustees of Columbia University in the City of New York

发明人： Brent R. Stockwell ,  Scott J. Dixon ,  Rachid Skouta

IPC分类号： C07D309/14 ,  A61K31/245 ,  A61K45/06 ,  A61K31/351 ,  A61K31/5375 ,  A61K31/4465 ,  C07D295/30 ,  C07C271/28 ,  A61K31/325 ,  A61K31/495 ,  C07C69/78 ,  C07D295/192

CPC分类号： C07D401/12 ,  A61K31/245 ,  A61K31/27 ,  A61K31/325 ,  A61K31/351 ,  A61K31/44 ,  A61K31/444 ,  A61K31/4465 ,  A61K31/4468 ,  A61K31/495 ,  A61K31/505 ,  A61K31/506 ,  A61K31/5375 ,  A61K45/06 ,  C07C69/78 ,  C07C205/57 ,  C07C205/58 ,  C07C211/50 ,  C07C225/22 ,  C07C229/60 ,  C07C233/54 ,  C07C237/30 ,  C07C255/58 ,  C07C271/16 ,  C07C271/24 ,  C07C271/28 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/18 ,  C07C2601/20 ,  C07C2603/74 ,  C07D211/58 ,  C07D213/36 ,  C07D213/74 ,  C07D213/80 ,  C07D239/26 ,  C07D239/42 ,  C07D295/088 ,  C07D295/192 ,  C07D295/30 ,  C07D309/14

摘要： The present invention provides, inter alia, a compound having the structure: (Formula (I). Also provided are compositions containing a pharmaceutically acceptable carrier and a compound according to the present invention. Further provided are methods for treating or ameliorating the effects of an excitotoxic disorder in a subject, methods of modulating ferroptosis in a subject, methods of reducing reactive oxygen species (ROS) in a cell, and methods for treating or ameliorating the effects of a neurodegenerative disease.

摘要翻译： 本发明尤其提供具有以下结构的化合物：（式（I）），还提供含有药学上可接受的载体和本发明化合物的组合物，还提供了治疗或改善 受试者中的兴奋性毒性障碍，受试者中的热of症调节方法，还原细胞中的活性氧（ROS）的方法，以及治疗或改善神经变性疾病的作用的方法。

公开(公告)号：US11192849B2

公开(公告)日：2021-12-07

申请号：US16297190

申请日：2019-03-08

申请人： THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK

发明人： Brent R. Stockwell ,  Rachid Skouta ,  Scott Dixon

IPC分类号： C07C229/56 ,  A61K31/245 ,  A61K45/06 ,  A61K31/196 ,  A61K31/505 ,  C07C255/58 ,  C07C271/24 ,  C07C229/60 ,  C07D401/12 ,  C07D239/26 ,  C07D213/38

摘要： The present invention provides, inter alia, a compound having the structure of Formula (I). Also provided are compositions containing a pharmaceutically acceptable carrier and a compound according to the present invention. Further provided are methods for treating or ameliorating the effects of an excitotoxic disorder in a subject, methods of modulating ferroptosis in a subject, methods of reducing reactive oxygen species (ROS) in a cell, and methods for treating or ameliorating the effects of a neurodegenerative disease.

公开(公告)号：US20190315681A1

公开(公告)日：2019-10-17

申请号：US16445104

申请日：2019-06-18

申请人： THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK

发明人： Brent R. Stockwell ,  Kenichi Shimada ,  Rachid Skouta

IPC分类号： C07C311/15 ,  C07D407/12 ,  C07D401/12

摘要： The present invention provides, inter alia, a compound according to formula (I): Also provided are compositions containing a pharmaceutically acceptable carrier and a compound according to the present invention. Further provided are methods for regulating GPX4 in a cell and methods for inducing ferroptosis in a cell.

公开(公告)号：US20190292135A1

公开(公告)日：2019-09-26

申请号：US16297190

申请日：2019-03-08

申请人： THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK

发明人： Brent R. Stockwell ,  Rachid Skouta ,  Scott Dixon

IPC分类号： C07C229/56 ,  C07C229/60 ,  C07D401/12 ,  C07D239/26 ,  C07D213/38 ,  A61K45/06 ,  A61K31/196 ,  A61K31/505 ,  C07C255/58 ,  A61K31/245 ,  C07C271/24

摘要： The present invention provides, inter alia, a compound having the structure of Formula (I). Also provided are compositions containing a pharmaceutically acceptable carrier and a compound according to the present invention. Further provided are methods for treating or ameliorating the effects of an excitotoxic disorder in a subject, methods of modulating ferroptosis in a subject, methods of reducing reactive oxygen species (ROS) in a cell, and methods for treating or ameliorating the effects of a neurodegenerative disease.

公开(公告)号：US10233171B2

公开(公告)日：2019-03-19

申请号：US15442475

申请日：2017-02-24

申请人： THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK

发明人： Brent R. Stockwell ,  Scott J. Dixon ,  Rachid Skouta

IPC分类号： C07D213/74 ,  A61K31/47 ,  C07D401/12 ,  C07D309/14 ,  C07C255/58 ,  C07D213/80 ,  C07C271/16 ,  C07C271/24 ,  C07C271/28 ,  C07C205/57 ,  C07C205/58 ,  C07C211/50 ,  C07D239/26 ,  C07C229/60 ,  C07C233/54 ,  C07C237/30 ,  C07D295/088 ,  C07D211/58 ,  C07D295/30 ,  C07D213/36 ,  A61K31/245 ,  A61K31/325 ,  A61K31/351 ,  A61K31/4465 ,  A61K31/495 ,  A61K31/5375 ,  A61K45/06 ,  C07C69/78 ,  C07D295/192 ,  A61K31/27 ,  A61K31/44 ,  A61K31/444 ,  A61K31/4468 ,  A61K31/505 ,  A61K31/506 ,  C07C225/22 ,  C07D239/42

摘要： The present invention provides, inter alia, a compound having the structure: Also provided are compositions containing a pharmaceutically acceptable carrier and a compound according to the present invention. Further provided are methods for treating or ameliorating the effects of an excitotoxic disorder in a subject, methods of modulating ferroptosis in a subject, methods of reducing reactive oxygen species (ROS) in a cell, and methods for treating or ameliorating the effects of a neurodegenerative disease.