公开(公告)号：US09283230B2

公开(公告)日：2016-03-15

申请号：US13984841

申请日：2011-08-15

申请人： Scott Clunas ,  John Mervyn David Storey ,  James Peter Sinclair ,  Thomas Craven Baddeley ,  Ahtsham Ishaq ,  Michael Simpson ,  Craig Williamson ,  Barry Alan Wood ,  Claude Michel Wischik ,  Charles Robert Harrington ,  Janet Elizabeth Rickard ,  David Horsley ,  Yin Sze Loh ,  Colin Marshall ,  Karrar Ahmad Khan

发明人： Scott Clunas ,  John Mervyn David Storey ,  James Peter Sinclair ,  Thomas Craven Baddeley ,  Ahtsham Ishaq ,  Michael Simpson ,  Craig Williamson ,  Barry Alan Wood ,  Claude Michel Wischik ,  Charles Robert Harrington ,  Janet Elizabeth Rickard ,  David Horsley ,  Yin Sze Loh ,  Colin Marshall ,  Karrar Ahmad Khan

IPC分类号： A61K31/5415 ,  C07D279/20 ,  C07D309/04 ,  C07C309/05 ,  A61K9/20 ,  C07C309/04 ,  A61K9/28 ,  C07C309/30 ,  C07C309/35

CPC分类号： A61K31/5415 ,  A61K9/0053 ,  A61K9/2095 ,  A61K9/2893 ,  A61L2/0052 ,  C07C303/32 ,  C07C309/04 ,  C07C309/05 ,  C07C309/30 ,  C07C309/35 ,  C07D279/20 ,  Y02A50/393 ,  Y02A50/411

摘要： The invention relates to compounds of general formula (I): wherein: each of R1 and R9 is independently selected from: —H, C1-4alkyl, C2-4alkenyl, and halogenated C1-4alkyl; each of R3NA and R3NB is independently selected from: —H, C1-4alkyl, C2-4alkenyl, and halogenated C1-4alkyl; each of R7NA and R7NB is independently selected from: —H, C1-4alkyl, C2-4alkenyl, and halogenated C1-4alkyl; and wherein: each of RA and RB is independently selected from: C1-4alkyl, halogenated C1-4alkyl, and C6-10aryl; or RA and RB are linked to form a group selected from: C1-6 alkylene and C6-10 arylene; and pharmaceutically acceptable salts thereof, which are useful in the treatment of, for example, Alzheimer's disease. In other aspects the invention also relates to novel formulations of 3,7-diamino-10H-phenothiazinium salts.

摘要翻译： 本发明涉及通式（I）的化合物：其中：R 1和R 9各自独立地选自：-H，C 1-4烷基，C 2-4链烯基和卤代C 1-4烷基; R 3NA和R 3NB中的每一个独立地选自：-H，C 1-4烷基，C 2-4链烯基和卤代C 1-4烷基; R7NA和R7NB中的每一个独立地选自：-H，C 1-4烷基，C 2-4链烯基和卤代C 1-4烷基; 并且其中：RA和RB各自独立地选自：C 1-4烷基，卤代C 1-4烷基和C 6-10芳基; 或RA和RB连接形成选自以下的基团：C 1-6亚烷基和C 6-10亚芳基; 和其药学上可接受的盐，其可用于治疗例如阿尔茨海默氏病。 在其它方面，本发明还涉及3,7-二氨基-10H-吩噻嗪鎓盐的新配方。

公开(公告)号：US20130315992A1

公开(公告)日：2013-11-28

申请号：US13984841

申请日：2011-08-15

申请人： Scott Clunas ,  John Mervyn David Storey ,  James Peter Sinclair ,  Thomas Craven Baddeley ,  Ahtsham Ishaq ,  Michael Simpson ,  Craig Williamson ,  Barry Alan Wood ,  Claude Michel Wischik ,  Charles Robert Harrington ,  Janet Elizabeth Rickard ,  David Horsley ,  Yin Sze Loh ,  Colin Marshall ,  Karrar Ahmad Khan

发明人： Scott Clunas ,  John Mervyn David Storey ,  James Peter Sinclair ,  Thomas Craven Baddeley ,  Ahtsham Ishaq ,  Michael Simpson ,  Craig Williamson ,  Barry Alan Wood ,  Claude Michel Wischik ,  Charles Robert Harrington ,  Janet Elizabeth Rickard ,  David Horsley ,  Yin Sze Loh ,  Colin Marshall ,  Karrar Ahmad Khan

IPC分类号： C07D279/20 ,  C07C309/30 ,  A61K9/28 ,  C07C309/35 ,  A61K9/20 ,  C07C309/04 ,  C07C309/05

CPC分类号： A61K31/5415 ,  A61K9/0053 ,  A61K9/2095 ,  A61K9/2893 ,  A61L2/0052 ,  C07C303/32 ,  C07C309/04 ,  C07C309/05 ,  C07C309/30 ,  C07C309/35 ,  C07D279/20 ,  Y02A50/393 ,  Y02A50/411

摘要： The invention relates to compounds of general formula (I): wherein: each of R1 and R9 is independently selected from: —H, C1-4alkyl, C2-4alkenyl, and halogenated C1-4alkyl; each of R3NA and R3NB is independently selected from: —H, C1-4alkyl, C2-4alkenyl, and halogenated C1-4alkyl; each of R7NA and R7NB is independently selected from: —H, C1-4alkyl, C2-4alkenyl, and halogenated C1-4alkyl; and wherein: each of RA and RB is independently selected from: C1-4alkyl, halogenated C1-4alkyl, and C6-10aryl; or RA and RB are linked to form a group selected from: C1-6 alkylene and C6-10 arylene; and pharmaceutically acceptable salts thereof, which are useful in the treatment of, for example, Alzheimer's disease. In other aspects the invention also relates to novel formulations of 3,7-diamino-10H-phenothiazinium salts.

摘要翻译： 本发明涉及通式（I）的化合物：其中：R 1和R 9各自独立地选自：-H，C 1-4烷基，C 2-4链烯基和卤代C 1-4烷基; R 3NA和R 3NB中的每一个独立地选自：-H，C 1-4烷基，C 2-4链烯基和卤代C 1-4烷基; R7NA和R7NB中的每一个独立地选自：-H，C 1-4烷基，C 2-4链烯基和卤代C 1-4烷基; 并且其中：RA和RB各自独立地选自：C 1-4烷基，卤代C 1-4烷基和C 6-10芳基; 或RA和RB连接形成选自以下的基团：C 1-6亚烷基和C 6-10亚芳基; 和其药学上可接受的盐，其可用于治疗例如阿尔茨海默氏病。 在其它方面，本发明还涉及3,7-二氨基-10H-吩噻嗪鎓盐的新配方。