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公开(公告)号：US20220098161A1
公开(公告)日：2022-03-31
申请号：US17499498
申请日：2021-10-12
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 , A61K31/5415 , A61K9/00 , A61P35/00 , A61P33/06 , A61P33/02 , A61P31/12 , A61P31/18 , A61P31/04 , A61P31/14 , 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：US11344558B2
公开(公告)日：2022-05-31
申请号：US14929111
申请日：2015-10-30
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： A61K31/5415 , C07D279/22 , C07D279/20 , C09B21/00
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.
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公开(公告)号：US09907804B2
公开(公告)日：2018-03-06
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： A61K31/5415 , A61K9/00 , A61K9/20 , A61L2/00 , C07D279/20 , A61K9/28 , C07C309/04 , C07C309/05 , C07C309/30 , C07C309/35 , C07C303/32
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.
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公开(公告)号：US20240245700A1
公开(公告)日：2024-07-25
申请号：US18595985
申请日：2024-03-05
发明人： Claude Michel Wischik , Janet Elizabeth Rickard , Charles Rober Harrington , David Horsley , John Mervyn David Storey , Colin Marshall , James Peter Sinclair , Thomas Craven Baddeley
IPC分类号： A61K31/5415 , C07D279/20 , C07D279/22 , C09B21/00
CPC分类号： A61K31/5415 , C07D279/20 , C07D279/22 , C09B21/00 , Y02A50/30
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; C2-4 alkenyl; and halogenated C1-4 alkyl; each of R3NA and R3NB is independently selected from: —H; C1-4 alkyl; C2-4 alkenyl; and halogenated C1-4 alkyl; each of R7NA and R7NB is independently selected from: —H; C1-4 alkyl; C2-4 alkenyl; and halogenated C1-4 alkyl; 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.-
公开(公告)号：US20220152038A1
公开(公告)日：2022-05-19
申请号：US17591306
申请日：2022-02-02
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： A61K31/5415 , C07D279/22 , C07D279/20 , C09B21/00
摘要： Described are methods of prepraing 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 usefull 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.
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公开(公告)号：US11180464B2
公开(公告)日：2021-11-23
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： C07D279/20 , A61K31/5415 , A61K9/00 , A61P35/00 , A61P33/06 , A61P33/02 , A61P31/12 , A61P31/18 , A61P31/04 , A61P31/14 , A61K9/20 , A61L2/00 , 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：US10399955B2
公开(公告)日：2019-09-03
申请号：US15373224
申请日：2016-12-08
发明人： Scott Clunas , John Mervyn David Storey , Janet Elizabeth Rickard , David Horsley , Charles Robert Harrington , Claude Michel Wischik
IPC分类号： C07D311/82 , C07D335/12 , C07D241/46 , C07D265/38 , C07D311/90 , C07D491/22 , C07D493/16 , A61K31/352 , A61K31/382 , A61K31/4545 , A61K31/4745 , A61K31/498 , A61K31/5377 , A61K31/538 , A61K45/06 , C07D491/16 , G01N33/68 , A61K9/00 , A61K31/4025 , A61K49/00 , C09B11/24 , C09B11/28 , C09B17/00 , C09B19/00 , C09B21/00 , C09B57/00 , C07D311/84 , C07D335/14 , C07D335/20
摘要： Described are a compound of formula (II) or (III): The compounds are effective in the treatment of disease, including a tauopathy condition or a disease of tau protein aggregation.
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公开(公告)号：US09549933B2
公开(公告)日：2017-01-24
申请号：US14181234
申请日：2014-02-14
发明人： Scott Clunas , John Mervyn David Storey , Janet Elizabeth Rickard , David Horsley , Charles Robert Harrington , Claude Michel Wischik
IPC分类号： A61K31/538 , A61K31/352 , A61K31/382 , A61K31/498 , C07D241/46 , C07D265/38 , C07D311/82 , C07D311/90 , C07D335/12 , C07D491/22 , C07D493/16 , A61K31/4545 , A61K31/4745 , A61K31/5377 , A61K45/06 , C07D491/16 , G01N33/68
CPC分类号： C07D311/82 , A61K9/0053 , A61K31/352 , A61K31/382 , A61K31/4025 , A61K31/4545 , A61K31/4745 , A61K31/498 , A61K31/5377 , A61K31/538 , A61K45/06 , A61K49/00 , C07D241/46 , C07D265/38 , C07D311/84 , C07D311/90 , C07D335/12 , C07D335/14 , C07D335/20 , C07D491/16 , C07D491/22 , C07D493/16 , C09B11/24 , C09B11/28 , C09B17/00 , C09B19/00 , C09B21/00 , C09B57/00 , G01N33/6896 , G01N2800/7047
摘要： Described are a compound of formula (II) or (III): The compounds are effective in the treatment of disease, including a tauopathy condition or a disease of tau protein aggregation.
摘要翻译： 这些化合物在治疗疾病中是有效的，包括tau蛋白病变或tau蛋白聚集的疾病。
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公开(公告)号：US20140161731A1
公开(公告)日：2014-06-12
申请号：US14181234
申请日：2014-02-14
发明人： Scott Clunas , John Mervyn David Storey , Janet Elizabeth Rickard , David Horsley , Charles Robert Harrington , Claude Michel Wischik
IPC分类号： A61K31/538 , C07D491/16 , C07D311/82 , A61K31/352 , C07D335/12 , A61K31/382 , C07D241/46 , A61K31/498 , C07D265/38 , C07D311/90 , A61K31/5377 , A61K31/4545 , A61K45/06 , G01N33/68 , A61K31/4745
CPC分类号： C07D311/82 , A61K9/0053 , A61K31/352 , A61K31/382 , A61K31/4025 , A61K31/4545 , A61K31/4745 , A61K31/498 , A61K31/5377 , A61K31/538 , A61K45/06 , A61K49/00 , C07D241/46 , C07D265/38 , C07D311/84 , C07D311/90 , C07D335/12 , C07D335/14 , C07D335/20 , C07D491/16 , C07D491/22 , C07D493/16 , C09B11/24 , C09B11/28 , C09B17/00 , C09B19/00 , C09B21/00 , C09B57/00 , G01N33/6896 , G01N2800/7047
摘要： Described are a compound of formula (II) or (III): The compounds are effective in the treatment of disease, including a tauopathy condition or a disease of tau protein aggregation.
摘要翻译： 描述了式（II）或（III）的化合物：该化合物在治疗疾病中是有效的，包括tau蛋白病变或tau蛋白聚集的疾病。
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公开(公告)号：US12064439B2
公开(公告)日：2024-08-20
申请号：US17499498
申请日：2021-10-12
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 , A61K9/20 , A61P31/04 , A61P31/12 , A61P31/14 , A61P31/18 , A61P33/02 , A61P33/06 , A61P35/00 , C07D279/20 , A61K9/28 , A61L2/00 , C07C303/32 , C07C309/04 , C07C309/05 , C07C309/30 , C07C309/35
CPC分类号： A61K31/5415 , A61K9/0053 , A61K9/2095 , A61P31/04 , A61P31/12 , A61P31/14 , A61P31/18 , A61P33/02 , A61P33/06 , A61P35/00 , C07D279/20 , A61K9/2893 , A61L2/0052 , C07C303/32 , C07C309/04 , C07C309/05 , C07C309/30 , C07C309/35 , Y02A50/30
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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