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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：US11759469B2
公开(公告)日：2023-09-19
申请号：US17349427
申请日：2021-06-16
IPC分类号： A61K31/5415 , A23L33/12 , A23L33/105 , A23P10/28 , A23P10/30 , A23L33/15 , A61P25/28 , A61K45/06 , B65D75/36
CPC分类号： A61K31/5415 , A23L33/105 , A23L33/12 , A23L33/15 , A23P10/28 , A23P10/30 , A61K45/06 , A61P25/28 , B65D75/36 , A23V2002/00 , B65D2203/02
摘要： The invention provides novel regimens for treatment of neurodegenerative disorders utilising methylthioninium (MT)-containing compounds. The regimens are based on novel findings in relation to the dosage of MT compounds, and their interaction with symptomatic treatments based on modulation of acetylcholinesterase levels.
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公开(公告)号：US20220370470A1
公开(公告)日：2022-11-24
申请号：US17620966
申请日：2020-06-29
IPC分类号： A61K31/5415 , A61K31/445 , A61K31/27 , A61K31/55 , A61K31/13 , A61P25/18 , A61P25/24 , A61P25/16 , A61P27/06 , A61P25/08 , A61P25/28
摘要： The present invention relates generally to methods and materials for treating synaptopathies, based on the use of Leu-co-methylthioninium acid salts, which are disclosed herein to increase synaptophysin levels in various brain regions at therapeutically relevant doses both in animal models of neurodegenerative disease, and in normal animals.
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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：US11116772B2
公开(公告)日：2021-09-14
申请号：US16697907
申请日：2019-11-27
发明人： John Mervyn David Storey , James Peter Sinclair , Colin Marshall , Han Wan Tan , Claude Michel Wischik
IPC分类号： A61K31/5415 , C09B19/02 , C07D279/18 , A61K9/00 , A61K49/00 , G01N33/52
摘要： This disclosure pertains generally to the field of chemical synthesis and purification, and more specifically to methods of synthesizing and purifying certain 3,7 diamino-phenothiazin-5-ium compounds (referred to herein as “diaminophenothiazinium compounds”) including Methythioninium Chloride (MTC) (also known as Methylene Blue). In one embodiment, the method comprises the steps of, in order: nitrosylation (NOS); nitrosyl reduction (NR); thiosulfonic acid formation (TSAF); oxidative coupling (OC); Cr(VI) reduction (CR); isolation and purification of zwitterionic intermediate (IAPOZI); ring closure (RC); chloride salt-formation (CSF); one of: sulphide treatment (ST); dimethyldithiocarbamate treatment (DT); carbonate treatment (CT); ethylenediaminetetraacetic acid treatment (EDTAT); organic extraction (OE); and recrystallisation (RX). Also disclosed resulting (high purity) compounds, compositions comprising them (e.g., tablets, capsules), and their use in methods of inactivating pathogens, and methods of medical treatment and diagnosis, etc., for example, for tauopathies, Alzheimer's disease (AD), skin cancer, melanoma, viral diseases, bacterial diseases, or protozoal diseases.
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37.发明授权公开(公告)号：US10421733B2
公开(公告)日：2019-09-24
申请号：US16040964
申请日：2018-07-20
IPC分类号： C07D279/18 , C07C381/02
摘要： Methods of synthesizing and purifying certain 3,7-diamino-phenothiazin-5-ium compounds (referred to herein as “diaminophenothiazinium compounds”) including Methylthioninium Chloride (MTC) (also known as Methylene Blue) are provided.
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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：US20190151329A1
公开(公告)日：2019-05-23
申请号：US16248746
申请日：2019-01-15
发明人： Claude Michel WISCHIK , Damon Jude WISCHIK , John Mervyn David STOREY , Charles Robert HARRINGTON
IPC分类号： A61K31/5415 , A61K45/06 , A61K31/542 , A61K9/00
摘要： Described are methods and materials for use in the treatment or prophylaxis of diseases, for example cognitive disorders, using diaminophenothiazines. In particular it relates to treatments having optimised pharmacokinetic properties, and dosage forms are intended to improve the relative cognitive or CNS benefits of the diaminophenothiazines, for instance compared to haematological effects.
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公开(公告)号：US20180263999A1
公开(公告)日：2018-09-20
申请号：US15987354
申请日：2018-05-23
发明人： Claude Michel WISCHIK , John Mervyn David STOREY , Colin MARSHALL , James Peter SINCLAIR , Thomas Craven BADDELEY
IPC分类号： A61K31/5415 , C07D279/18 , C07D279/20
摘要： Disclosed are methods of synthesis and/or purification of certain 3,7-diamino-phenothiazin-5-ium compounds (“diaminophenothiazinium compounds”) including Methylthioninium Chloride (MTC) (Methylene Blue), and the resulting high purity characterized by a purity greater than 98%, and very low levels of heavy metals and organic impurities Azure A, B, C and MVB. Also disclosed are methods of treatment of a tauopathy or methemoglobinemia in a patient in need thereof, comprising administering to the patient a therapeutically effective amount of the high-purity diaminophenothiazinium compound.
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