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1. 发明申请

US20220098161A1 PHENOTHIAZINE DIAMINIUM SALTS AND THEIR USE 有权
公开(公告)号：US20220098161A1
公开(公告)日：2022-03-31
申请号：US17499498
申请日：2021-10-12
申请人： WisTa Laboratories Ltd
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.

2. 发明授权

US09675621B2 Methods of synthesis and/or purification of diaminophenothiazinium compounds 有权
公开(公告)号：US09675621B2
公开(公告)日：2017-06-13
申请号：US15185803
申请日：2016-06-17
申请人： WisTa Laboratories Ltd.
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.

3. 发明授权

US11344558B2 3, 7-diamino-10H-phenothiazine salts and their use 有权
公开(公告)号：US11344558B2
公开(公告)日：2022-05-31
申请号：US14929111
申请日：2015-10-30
申请人： WisTa Laboratories Ltd.
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.

4. 发明授权

US10537578B2 Medical methods utilising high purity diaminophenothiazinium compounds 有权
公开(公告)号：US10537578B2
公开(公告)日：2020-01-21
申请号：US15718662
申请日：2017-09-28
申请人： WisTa Laboratories Ltd.
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.

5. 发明授权

US09907804B2 Phenothiazine diaminium salts and their use 有权
公开(公告)号：US09907804B2
公开(公告)日：2018-03-06
申请号：US15056610
申请日：2016-02-29
申请人： WisTa Laboratories Ltd.
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.

6. 发明授权

US09801890B2 Medical methods utilising high purity diaminophenothiazinium compounds 有权
公开(公告)号：US09801890B2
公开(公告)日：2017-10-31
申请号：US15419763
申请日：2017-01-30
申请人： WisTa Laboratories Ltd.
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.

7. 发明申请

US20160129009A1 HIGH PURITY DIAMINOPHENOTHIAZINIUM COMPOUNDS INCLUDING METHYLTHIONINIUM CHLORIDE (MTC) 审中-公开
标题翻译：包括氯化亚甲基氯化铵（MTC）的高纯度二氨基苯并噻唑化合物
公开(公告)号：US20160129009A1
公开(公告)日：2016-05-12
申请号：US15000723
申请日：2016-01-19
申请人： WisTa Laboratories Ltd.
发明人： John Storey , James Peter Sinclair , Colin Marshall , Han Wan Tan , Claude Michael Wischik
IPC分类号： A61K31/5415 , A61K9/00
CPC分类号： A61K31/5415 , A61K9/0019 , A61K49/006 , C07D279/18 , C09B19/02 , G01N33/52 , Y02A50/393
摘要： This invention 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). The present invention also pertains to the 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.
摘要翻译：本发明一般涉及化学合成和纯化领域，更具体地涉及合成和纯化某些3,7-二氨基 - 吩噻嗪-5-肟化合物（本文中称为“二氨基吩噻嗪鎓化合物”）的方法，包括氯化亚铁（MTC）（MTC）（也称为亚甲基蓝）。在一个实施方案中，该方法包括以下步骤：按顺序：亚硝基化（NOS）; 亚硝酰还原（NR）; 硫代磺酸形成（TSAF）; 氧化偶合（OC）; Cr（VI）还原（CR）; 两性离子中间体（IAPOZI）的分离和纯化; 闭环（RC）; 氯化物形成（CSF）; 一种：硫化物处理（ST）; 二甲基二硫代氨基甲酸酯处理（DT）; 碳酸盐处理（CT）; 乙二胺四乙酸处理（EDTAT）; 有机萃取（OE）; 和重结晶（RX）。本发明还涉及所得的（高纯度）化合物，包含它们的组合物（例如片剂，胶囊）及其在灭活病原体的方法中的用途，以及治疗和诊断方法等，例如对于tau蛋白病，阿尔茨海默病（AD），皮肤癌，黑素瘤，病毒性疾病，细菌性疾病或原生动物疾病。

8. 发明授权

US11045477B2 Methods of synthesis and/or purification of diaminophenothiazinium compounds 有权
公开(公告)号：US11045477B2
公开(公告)日：2021-06-29
申请号：US16685420
申请日：2019-11-15
申请人： WisTa Laboratories Ltd.
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.

9. 发明申请

US20200246350A1 PHENOTHIAZINE DIAMINIUM SALTS AND THEIR USE 审中-公开
公开(公告)号：US20200246350A1
公开(公告)日：2020-08-06
申请号：US16751811
申请日：2020-01-24
申请人： WisTa Laboratories Ltd.
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.

10. 发明授权

US10323010B2 Methods of chemical synthesis of substituted 10H-phenothiazine-3,7-diamine compounds 有权
公开(公告)号：US10323010B2
公开(公告)日：2019-06-18
申请号：US15746338
申请日：2016-07-20
申请人： WisTa Laboratories Ltd.
发明人： John Mervyn David Storey , Christopher Paul Larch , Steven John Kemp , Scott Clunas , Sarah Louise Nicoll , Helen Sarah Gibbard , Michael Simpson , James Peter Sinclair , Colin Marshall
IPC分类号： C07D279/20
摘要： The present invention pertains generally to the field of chemical synthesis, and more particularly to methods of chemical synthesis which include the step of preparing a substituted 10H-phenothiazine-3,7-diamine compound of Formula (1) by a step of selective alkylation by reductive amination, in which the corresponding unsubstituted diamine of Formula (4) is reacted with aldehyde/ketone, under reductive amination conditions. The present invention also relates to such methods which incorporate additional subsequent and/or preceding steps, for example, to prepare compounds of Formulae (2) and (3) from compounds of Formula (1), and to prepare compounds of Formula (4) from, for example, compounds of Formulae (5), (6), (7), (8), and (9). Compounds of Formula (1), Formula (2), and Formula (3) are useful, for example, in the treatment of diseases of protein aggregation, such as Alzheimer's disease.

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