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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。
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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。
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公开(公告)号：US06706255B2
公开(公告)日：2004-03-16
申请号：US10243555
申请日：2002-09-13
IPC分类号： A61K900
CPC分类号： A61K31/195 , A61K9/006 , A61K47/10 , Y10S514/909
摘要： Liquid pharmaceutical compositions comprising at least one thyroid hormone, ethanol, a pH adjusting agent, and water are disclosed. The compositions may be delivered by a metered dosage delivery system such as an aerosol or pump-action spray, and are useful in the treatment of disorders associated with an impairment of thyroid hormone function in animals including human beings.
摘要翻译： 公开了包含至少一种甲状腺激素，乙醇，pH调节剂和水的液体药物组合物。 组合物可以通过计量剂量递送系统例如气雾剂或泵作用喷雾递送，并且可用于治疗与包括人在内的动物的甲状腺激素功能受损相关的疾病。
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公开(公告)号：US20130243858A1
公开(公告)日：2013-09-19
申请号：US13989953
申请日：2011-11-30
申请人： Karrar Ahmad Khan
发明人： Karrar Ahmad Khan
IPC分类号： A61K31/5415 , A61K9/20
CPC分类号： A61K31/5415 , A61K9/1652 , A61K9/20 , A61K9/2054 , A61K9/2095 , A61K9/4866 , C07D279/18
摘要： Solid dosage forms of methylthioninium chloride (MTC) further comprise at least one diluent suitable for direct compression. The MTC exists in a substantially pure and stable polymorphic form. The solid dosage forms may preferably be prepared by direct compression methods.
摘要翻译： 甲基硫堇（MTC）的固体剂型还包含至少一种适于直接压制的稀释剂。 MTC以基本上纯且稳定的多晶型形式存在。 固体剂型可优选通过直接压制方法制备。
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公开(公告)号：US06458842B1
公开(公告)日：2002-10-01
申请号：US08682779
申请日：1996-07-31
IPC分类号： A61K31195
CPC分类号： A61K31/195 , A61K9/006 , A61K47/10 , Y10S514/909
摘要： There is disclosed a liquid pharmaceutical composition comprising a therapeutic agent which comprises: one or more thyroid hormone or hormones; from about 40% to about 96% ethanol by volume; a pH adjusting agent so that the measured pH of the composition is from about 9 to about 12; and from about 4% to about 50% water by volume; which has utility in the treatment of disorders associated with an impairment of the thyroid hormone function in animals including human beings. The liquid composition may be delivered by a metered dosage delivery system such as an aerosol or pump-action spray.
摘要翻译： 公开了包含治疗剂的液体药物组合物，其包含：一种或多种甲状腺激素或激素; 约40％至约96％乙醇; pH调节剂，使得组合物的测量pH为约9至约12; 和约4％至约50％的水; 其可用于治疗与包括人在内的动物的甲状腺激素功能受损相关的疾病。 液体组合物可以通过计量剂量递送系统例如气溶胶或泵作用喷雾来递送。
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公开(公告)号：US09192611B2
公开(公告)日：2015-11-24
申请号：US13989953
申请日：2011-11-30
申请人： Karrar Ahmad Khan
发明人： Karrar Ahmad Khan
IPC分类号： A61K31/5415 , A61K9/16 , A61K9/20 , A61K9/48 , C07D279/18
CPC分类号： A61K31/5415 , A61K9/1652 , A61K9/20 , A61K9/2054 , A61K9/2095 , A61K9/4866 , C07D279/18
摘要： Solid dosage forms of methylthioninium chloride (MTC) further comprise at least one diluent suitable for direct compression. The MTC exists in a substantially pure and stable polymorphic form. The solid dosage forms may preferably be prepared by direct compression methods.
摘要翻译： 甲基硫堇（MTC）的固体剂型还包含至少一种适于直接压制的稀释剂。 MTC以基本上纯且稳定的多晶型形式存在。 固体剂型可优选通过直接压制方法制备。
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公开(公告)号：US5753254A
公开(公告)日：1998-05-19
申请号：US682783
申请日：1996-07-31
申请人： Karrar Ahmad Khan , Alan Smith
发明人： Karrar Ahmad Khan , Alan Smith
IPC分类号： A61K9/00 , A61K31/195 , A61K9/14
CPC分类号： A61K9/0056 , A61K31/195
摘要： There is disclosed a solid fast dispersing dosage form of a pharmaceutical composition suitable for oral administration comprising: a therapeutic agent which comprises one or more compound thyroid hormone or hormones; from about 80% to about 99.9% of disintegrating agent by mass; from about 0.01% to about 10% of flavoring agent by mass; and from about 0.1% to about 5% mass of lubricating agent by mass; which has utility in the treatment of disorders associated with the improvement of the thyroid hormone function in animals including human beings.
摘要翻译： PCT No.PCT / EP95 / 00321 Sec。 371日期：1996年7月31日 102（e）日期1996年7月31日PCT提交1995年1月30日PCT公布。 WO95 / 20953 PCT出版物 日期：1995年8月10日公开了适用于口服给药的药物组合物的固体快速分散剂型，其包含：包含一种或多种化合物甲状腺激素或激素的治疗剂; 约80％至约99.9％的崩解剂; 约0.01％至约10％的调味剂; 和约0.1质量％至约5质量％的润滑剂; 其可用于治疗与包括人在内的动物的甲状腺激素功能改善相关的病症。
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