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公开(公告)号：US20200246350A1
公开(公告)日：2020-08-06
申请号：US16751811
申请日：2020-01-24
发明人： Colin Marshall , 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 , Karrar Ahmad Khan , Christopher Paul Larch
IPC分类号： A61K31/5415 , A61K9/00 , C07D279/20 , A61K9/20 , A61L2/00
摘要： Disclosed are compounds of general formula (I): and pharmaceutically acceptable salts thereof, formulations, methods and uses in, for example, the treatment of disease.
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公开(公告)号：US20190046537A1
公开(公告)日：2019-02-14
申请号：US15912166
申请日：2018-03-05
发明人： Colin Marshall , 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 , Karrar Ahmad Khan , Christopher Paul Larch
IPC分类号： A61K31/5415 , A61L2/00 , A61K9/00 , A61K9/20 , C07D279/20 , A61K9/28 , C07C309/04 , C07C309/05 , C07C309/30 , C07C309/35 , C07C303/32
摘要： Disclosed are compounds of general formula (I): and pharmaceutically acceptable salts thereof, formulations, methods and uses in, for example, the treatment of disease.
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公开(公告)号：US20160237048A1
公开(公告)日：2016-08-18
申请号：US15056610
申请日：2016-02-29
发明人： COLIN MARSHALL , 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 , Karrar Ahmad Khan , Christopher Paul Larch
IPC分类号： C07D279/20 , C07C303/32 , A61L2/00 , C07C309/04
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： Disclosed are compounds of general formula (I): and pharmaceutically acceptable salts thereof, formulations, methods and uses in, for example, the treatment of disease.
摘要翻译： 公开了通式（I）的化合物及其药学上可接受的盐，在例如治疗疾病中的制剂，方法和用途。
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公开(公告)号：US09174954B2
公开(公告)日：2015-11-03
申请号：US14248730
申请日：2014-04-09
发明人： Claude Michel Wischik , Janet Elizabeth Rickard , Charles Robert Harrington , David Horsley , John Mervyn David Storey , Colin Marshall , James Peter Sinclair , Thomas Craven Baddeley
IPC分类号： A61K31/54 , C07D279/18 , C07D279/20 , A61K31/5415 , A61K49/00 , A61K51/04 , G01N33/68
CPC分类号： C07D279/20 , A61K31/5415 , A61K49/0002 , A61K49/003 , A61K51/0465 , G01N33/6896 , G01N2800/2835 , Y02A50/393 , Y02A50/411
摘要： Described are methods of preparing reduced 3,7-diamino-10H-phenothiazine (DAPTZ) compounds of formula: wherein: R1 and R9 are 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; each of HX1 and HX2 is independently a protic acid; and pharmaceutically acceptable salts, solvates, and hydrates thereof. These methods are particularly useful for producing stable reduced forms, and with high purity. The stability and purity are especially relevant for pharmaceutical compositions for the treatment of disease. The compounds are useful for treatment of e.g. tauopathies, such as Alzheimer's disease, and also as prodrugs for the corresponding oxidized thioninium drugs.
摘要翻译： 描述了制备下式的还原的3,7-二氨基-10H-吩噻嗪（DAPTZ）化合物的方法：其中：R 1和R 9独立地选自：-H; C 1-4烷基; C2-4烯基; 和卤代C1-4烷基; R3NA和R3NB中的每一个独立地选自：-H; C 1-4烷基; C2-4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; C2-4烯基; 和卤代C 1-4烷基; HX1和HX2各自独立地是质子酸; 及其药学上可接受的盐，溶剂化物和水合物。 这些方法对于生产稳定的还原形式和高纯度特别有用。 稳定性和纯度与治疗疾病的药物组合物特别相关。 该化合物可用于治疗例如 tau病，如阿尔茨海默病，以及相应的氧化型硫堇药物的前药。
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