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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：US20200016165A1
公开(公告)日：2020-01-16
申请号：US16320148
申请日：2017-07-25
IPC分类号： A61K31/5415 , A61K45/06 , A61P25/28 , A23L33/15 , A23L33/105 , A23L33/12 , A23P10/28 , A23P10/30 , B65D75/36
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：US10047062B2
公开(公告)日：2018-08-14
申请号：US15674229
申请日：2017-08-10
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 Methythioninium Chloride (MTC) (also known as Methylene Blue) are provided.
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公开(公告)号：US09675621B2
公开(公告)日：2017-06-13
申请号：US15185803
申请日：2016-06-17
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
CPC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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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：US20220008431A1
公开(公告)日：2022-01-13
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
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：US10537578B2
公开(公告)日：2020-01-21
申请号：US15718662
申请日：2017-09-28
发明人： John Mervyn David Storey , James Peter Sinclair , Colin Marshall , Han Wan Tan , Claude Michel Wischik
IPC分类号： C07D279/18 , A61K31/5415 , C09B19/02 , 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 “diaminophenothiaziniumcompounds”) 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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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：US09801890B2
公开(公告)日：2017-10-31
申请号：US15419763
申请日：2017-01-30
发明人： John Mervyn David Storey , James Peter Sinclair , Colin Marshall , Han Wan Tan , Claude Michel Wischik
IPC分类号： A61K31/5415 , G01N33/52 , A61K49/00
CPC分类号： A61K31/5415 , A61K9/0019 , A61K49/006 , C07D279/18 , C09B19/02 , G01N33/52 , Y02A50/393
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 recrystallization (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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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.
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