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1. 发明授权

US07888350B2 3,7-diamino-10H-phenothiazine salts and their use 有权
标题翻译： 3,7-二氨基-10H-吩噻嗪盐及其用途
公开(公告)号：US07888350B2
公开(公告)日：2011-02-15
申请号：US12294599
申请日：2007-03-28
申请人： Claude Michel Wischik , Janet Elizabeth Rickard , Charles Robert Harrington , David Horsley , John Mervyn David Storey , Colin Marshall , James Peter Sinclair , Thomas Craven Baddeley
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： C07D279/18 , A61K31/5415
CPC分类号： A61K31/5415 , C07D279/20 , C07D279/22 , C09B21/00 , Y02A50/393 , Y02A50/411
摘要： This invention pertains generally to the field of phenothiazine compounds, and more particularly to certain stably reduced phenothiazine compounds, specifically, certain 3,7 diamino-10H-phenothiazine (DAPTZ) compounds of the following formula wherein: each of R1 and R9 is 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 compounds are useful as drugs, for example, in the treatment of tauopathies, such as Alzheimer's disease, and also as prodrugs for the corresponding oxidized thioninium drugs (for example, methythioninium chloride, MTC).
摘要翻译：本发明一般涉及吩噻嗪化合物领域，更具体地涉及某些稳定还原的吩噻嗪化合物，具体地，下列通式的某些3,7-二氨基-10H-吩噻嗪（DAPTZ）化合物其中：R 1和R 9各自独立地选自从：-H; C 1-4烷基; C2-4烯基; 和卤代C 1-4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。这些化合物可用作药物，例如用于治疗tau蛋白病如阿尔茨海默氏病，以及作为相应的氧化硫堇药物（例如氯化甲硫氨酸，MTC）的前药。

2. 发明授权

US07956183B2 Methods of synthesis and/or purification of diaminophenothiazinium compounds 有权
标题翻译：二氨基吩噻嗪鎓化合物的合成和/或纯化方法
公开(公告)号：US07956183B2
公开(公告)日：2011-06-07
申请号：US12373216
申请日：2007-07-10
申请人： Claude Michel Wischik , John Mervyn David Storey , Colin Marshall , James Peter Sinclair , Thomas Craven Baddeley
发明人： Claude Michel Wischik , John Mervyn David Storey , Colin Marshall , James Peter Sinclair , Thomas Craven Baddeley
IPC分类号： C07D279/28
CPC分类号： A61K31/5415 , C07D279/18 , C07D279/20
摘要： A method for the synthesis of a diaminophenothiazinium compound of the following formula: comprising (a) purifying a corresponding reduced compound which is N-acylated at the heterocyclic nitrogen; (b) deacylating the purified compound to provide the corresponding reduced compound; and (c) oxidizing the reduced compound to provide the diaminophenothiazinium compound. Optional purification may performed, for example, after deacylating and after oxidizing. The method provides high purity diaminophenothiazinium compounds which are suitable for pharmaceutical and related therapeutic uses. Such uses include inactivating pathogens, the treatment of the infectious diseases, and for the treatment of diseases of protein aggregation, such as tauopathies, including Alzheimer's disease.
摘要翻译：一种用于合成下式的二氨基吩噻嗪鎓化合物的方法：包括（a）在杂环氮中纯化相应的N-酰化的还原化合物; （b）将纯化的化合物去酰化以提供相应的还原化合物; 和（c）氧化还原的化合物以提供二氨基吩噻嗪鎓化合物。任选的纯化可以例如在脱酰基后和氧化后进行。该方法提供了适用于药物和相关治疗用途的高纯度二氨基吩噻嗪鎓化合物。这样的用途包括灭活病原体，感染性疾病的治疗以及治疗蛋白质聚集的疾病，诸如包括阿尔茨海默病在内的tau蛋白病。

3. 发明申请

US20090259040A1 METHODS OF SYNTHESIS AND/OR PURIFICATION OF DIAMINOPHENOTHIAZINIUM COMPOUNDS 有权
标题翻译：二氨基苯甲酸酯化合物的合成和/或纯化方法
公开(公告)号：US20090259040A1
公开(公告)日：2009-10-15
申请号：US12373216
申请日：2007-07-10
申请人： Claude Michel Wischik , John Mervyn David Storey , Colin Marshall , James Peter Sinclair , Thomas Craven Baddeley
发明人： Claude Michel Wischik , John Mervyn David Storey , Colin Marshall , James Peter Sinclair , Thomas Craven Baddeley
IPC分类号： C07D279/18
CPC分类号： A61K31/5415 , C07D279/18 , C07D279/20
摘要： This invention pertains generally to the field of chemical synthesis and purification, and more specifically to methods of synthesis and/or purification of certain 3,7 diamino-phenothiazin-5-ium compounds (referred to herein as “diaminophenothiazinium compounds”) including Methylthioninium Chloride (MTC) (also known as Methylene Blue). 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, prophylaxis, and diagnosis, etc., for example, a tauopathy; a disease of tau protein aggregation; Alzheimer's disease (AD); Pick's disease; Progressive Supranuclear Palsy (PSP); fronto temporal dementia (FTD); parkinsonism linked to chromosome 17 (FTDP-17); disinhibition-dementia-parkinsonism-amyotrophy complex (DDPAC); pallido-ponto-nigral degeneration (PPND); Guam-ALS syndrome; pallido-nigro-luysian degeneration (PNLD); cortico-basal degeneration (CBD); mild cognitive impairment (MCI); skin cancer; melanoma; methemoglobinemia; a viral infection; a bacterial infection; a protozoal infection; a parasitic infection; malaria; visceral leishmaniasis; African sleeping sickness; toxoplasmosis; giardiasis; Chagas' disease; Hepatitis C virus (HCV) infection; human immunodeficiency virus (HIV) infection; West Nile virus (WNV) infection; a synucleinopathy; Parkinson's disease (PD); dementia with Lewy bodies (DLB); multiple system atrophy (MSA); drug-induced parkinsonism; and pure autonomic failure (PAF).
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/或纯化某些3,7-二氨基吩噻嗪-5-肟化合物（本文称为“二氨基吩噻嗪鎓化合物”）的方法，包括甲基硫堇（MTC）（也称为亚甲蓝）。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，以及医学治疗，预防和诊断等方法，tau病 tau蛋白聚集的疾病; 阿尔茨海默病（AD）; 皮克病进行性核核麻痹（PSP）颞痴呆（FTD）; 与17号染色体相关的帕金森综合征（FTDP-17）; 去抑痴呆 - 帕金森综合征 - 肌萎缩综合征（DDPAC）; 苍白球 - 黑质变性（PPND）; 关岛ALS综合征苍白球黑素瘤变性（PNLD）; 皮质基底变性（CBD）; 轻度认知障碍（MCI）; 皮肤癌; 黑色素瘤高铁血红蛋白血症; 病毒感染; 细菌感染; 原生动物感染; 寄生虫感染; 疟疾; 内脏利什曼病非洲昏睡病弓形体病贾第虫病恰加斯病丙型肝炎病毒（HCV）感染; 人类免疫缺陷病毒（HIV）感染; 西尼罗病毒（WNV）感染; 突触核蛋白病帕金森病（PD）; 路易体痴呆（DLB）; 多系统萎缩（MSA）; 药物引起的帕金森综合征和纯自主神经衰竭（PAF）。

4. 发明授权

US09283230B2 Phenothiazine diaminium salts and their use 有权
标题翻译：吩噻嗪二胺盐及其用途
公开(公告)号：US09283230B2
公开(公告)日：2016-03-15
申请号：US13984841
申请日：2011-08-15
申请人： 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 , Colin Marshall , Karrar Ahmad Khan
发明人： 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 , Colin Marshall , Karrar Ahmad Khan
IPC分类号： A61K31/5415 , C07D279/20 , C07D309/04 , C07C309/05 , A61K9/20 , C07C309/04 , A61K9/28 , C07C309/30 , C07C309/35
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： The invention relates to compounds of general formula (I): wherein: each of R1 and R9 is 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; and wherein: each of RA and RB is independently selected from: C1-4alkyl, halogenated C1-4alkyl, and C6-10aryl; or RA and RB are linked to form a group selected from: C1-6 alkylene and C6-10 arylene; and pharmaceutically acceptable salts thereof, which are useful in the treatment of, for example, Alzheimer's disease. In other aspects the invention also relates to novel formulations of 3,7-diamino-10H-phenothiazinium salts.
摘要翻译：本发明涉及通式（I）的化合物：其中：R 1和R 9各自独立地选自：-H，C 1-4烷基，C 2-4链烯基和卤代C 1-4烷基; R 3NA和R 3NB中的每一个独立地选自：-H，C 1-4烷基，C 2-4链烯基和卤代C 1-4烷基; R7NA和R7NB中的每一个独立地选自：-H，C 1-4烷基，C 2-4链烯基和卤代C 1-4烷基; 并且其中：RA和RB各自独立地选自：C 1-4烷基，卤代C 1-4烷基和C 6-10芳基; 或RA和RB连接形成选自以下的基团：C 1-6亚烷基和C 6-10亚芳基; 和其药学上可接受的盐，其可用于治疗例如阿尔茨海默氏病。在其它方面，本发明还涉及3,7-二氨基-10H-吩噻嗪鎓盐的新配方。

5. 发明授权

US08710051B2 3,7-diamino-10H-phenothiazine salts and their use 有权
标题翻译： 3,7-二氨基-10H-吩噻嗪盐及其用途
公开(公告)号：US08710051B2
公开(公告)日：2014-04-29
申请号：US13011797
申请日：2011-01-21
申请人： Claude Michel Wischik , Janet Elizabeth Rickard , Charles Robert Harrington , David Horsley , John Mervyn David Storey , Colin Marshall , James Peter Sinclair , Thomas Craven Baddeley
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
CPC分类号： C07D279/20 , A61K31/5415 , A61K49/0002 , A61K49/003 , A61K51/0465 , G01N33/6896 , G01N2800/2835 , Y02A50/393 , Y02A50/411
摘要： This invention pertains generally to the field of phenothiazine compounds, and more particularly to certain stably reduced phenothiazine compounds, specifically, certain 3,7-diamino-10H-phenothiazine (DAPTZ) compounds of the following formula: wherein: each of R1 and R9 is 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 compounds are useful as drugs, for example, in the treatment of tauopathies, such as Alzheimer's disease, and also as prodrugs for the corresponding oxidized thioninium drugs (for example, methylthioninium chloride, MTC).
摘要翻译：本发明一般涉及吩噻嗪化合物领域，更具体地涉及某些稳定还原的吩噻嗪化合物，具体地，下列通式的某些3,7-二氨基-10H-吩噻嗪（DAPTZ）化合物：其中：R 1和R 9各自为独立选自：-H; C 1-4烷基; C2-4烯基; 和卤代C 1-4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。这些化合物可用作药物，例如用于治疗tau蛋白病，例如阿尔茨海默氏病，以及作为相应的氧化硫堇药物（例如，甲基硫堇，MTC）的前药。

6. 发明申请

US20130315992A1 PHENOTHIAZINE DIAMINIUM SALTS AND THEIR USE 有权
标题翻译：双酚钠金属盐及其使用
公开(公告)号：US20130315992A1
公开(公告)日：2013-11-28
申请号：US13984841
申请日：2011-08-15
申请人： 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 , Colin Marshall , Karrar Ahmad Khan
发明人： 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 , Colin Marshall , Karrar Ahmad Khan
IPC分类号： C07D279/20 , C07C309/30 , A61K9/28 , C07C309/35 , A61K9/20 , C07C309/04 , C07C309/05
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： The invention relates to compounds of general formula (I): wherein: each of R1 and R9 is 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; and wherein: each of RA and RB is independently selected from: C1-4alkyl, halogenated C1-4alkyl, and C6-10aryl; or RA and RB are linked to form a group selected from: C1-6 alkylene and C6-10 arylene; and pharmaceutically acceptable salts thereof, which are useful in the treatment of, for example, Alzheimer's disease. In other aspects the invention also relates to novel formulations of 3,7-diamino-10H-phenothiazinium salts.
摘要翻译：本发明涉及通式（I）的化合物：其中：R 1和R 9各自独立地选自：-H，C 1-4烷基，C 2-4链烯基和卤代C 1-4烷基; R 3NA和R 3NB中的每一个独立地选自：-H，C 1-4烷基，C 2-4链烯基和卤代C 1-4烷基; R7NA和R7NB中的每一个独立地选自：-H，C 1-4烷基，C 2-4链烯基和卤代C 1-4烷基; 并且其中：RA和RB各自独立地选自：C 1-4烷基，卤代C 1-4烷基和C 6-10芳基; 或RA和RB连接形成选自以下的基团：C 1-6亚烷基和C 6-10亚芳基; 和其药学上可接受的盐，其可用于治疗例如阿尔茨海默氏病。在其它方面，本发明还涉及3,7-二氨基-10H-吩噻嗪鎓盐的新配方。

7. 发明授权

US08440821B2 Methods of synthesis and/or purification of diaminophenothiazinium compounds 有权
标题翻译：二氨基吩噻嗪鎓化合物的合成和/或纯化方法
公开(公告)号：US08440821B2
公开(公告)日：2013-05-14
申请号：US13149164
申请日：2011-05-31
申请人： Claude Michel Wischik , John Mervyn David Storey , Colin Marshall , James Peter Sinclair , Thomas Craven Baddeley
发明人： Claude Michel Wischik , John Mervyn David Storey , Colin Marshall , James Peter Sinclair , Thomas Craven Baddeley
IPC分类号： C07D279/28
CPC分类号： A61K31/5415 , C07D279/18 , C07D279/20
摘要： Described is a method for the synthesis and/or purification of a high purity diaminophenothiazinium compound of the following formula: characterized by a purity of greater than 98% and less than 1% Azure B, 0.15% Azure A, 0.15% Azure C and 0.05% Methylene Violet Bernthsen (MVB), as impurities. Also described are related high purity compounds, compositions, and methods of using such compounds and compositions. The compounds and compositions are useful in the treatment of diseases caused by tau aggregation, such as Alzheimer's disease and other dementias, and infection.
摘要翻译：描述了用于合成和/或纯化下式的高纯度二氨基吩噻嗪鎓化合物的方法：其特征在于纯度大于98％且小于1％的Azure B，0.15％的Azure A，0.15％的Azure C和0.05 ％亚甲基紫伯氏（MVB），作为杂质。还描述了相关的高纯度化合物，组合物和使用这些化合物和组合物的方法。化合物和组合物可用于治疗由tau聚集引起的疾病，例如阿尔茨海默病和其他痴呆以及感染。

8. 发明申请

US20090054419A1 3,7-DIAMINO-10H-PHENOTHIAZINE SALTS AND THEIR USE 有权
标题翻译： 3,7-DIAMINO-10H-PHENOTHIAZINE SALTS及其使用
公开(公告)号：US20090054419A1
公开(公告)日：2009-02-26
申请号：US12294599
申请日：2007-03-28
申请人： Claude Michel Wischik , Janet Elizabeth Rickard , Charles Robert Harrington , David Horsley , John Mervyn David Storey , Colin Marshall , James Peter Sinclair , Thomas Craven Baddeley
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 , C07D279/30 , C07D279/20 , C07K1/113
CPC分类号： A61K31/5415 , C07D279/20 , C07D279/22 , C09B21/00 , Y02A50/393 , Y02A50/411
摘要： This invention pertains generally to the field of phenothiazine compounds, and more particularly to certain stably reduced phenothiazine compounds, specifically, certain 3,7 diamino-10H-phenothiazine (DAPTZ) compounds of the following formula wherein: each of R1 and R9 is 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 compounds are useful as drugs, for example, in the treatment of tauopathies, such as Alzheimer's disease, and also as prodrugs for the corresponding oxidized thioninium drugs (for example, methythioninium chloride, MTC).
摘要翻译：本发明一般涉及吩噻嗪化合物领域，更具体地涉及某些稳定还原的吩噻嗪化合物，具体地，下列通式的某些3,7-二氨基-10H-吩噻嗪（DAPTZ）化合物其中：R 1和R 9各自独立地选自从：-H; C 1-4烷基; C2-4烯基; 和卤代C 1-4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。这些化合物可用作药物，例如用于治疗tau蛋白病如阿尔茨海默氏病，以及作为相应的氧化硫堇药物（例如氯化甲硫氨酸，MTC）的前药。

9. 发明授权

US09242946B2 High purity diaminophenothiazinium compounds including methylthioninium chloride (MTC) 有权
标题翻译：高纯度二氨基吩噻嗪鎓化合物，包括甲基硫堇（MTC）
公开(公告)号：US09242946B2
公开(公告)日：2016-01-26
申请号：US12875465
申请日：2010-09-03
申请人： John Mervyn David Storey , James Peter Sinclair , Colin Marshall , Han Wan Tan , Claude Michel Wischik
发明人： John Mervyn David Storey , James Peter Sinclair , Colin Marshall , Han Wan Tan , Claude Michel Wischik
IPC分类号： C07D279/18 , C09B19/02
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 Methylhioninium 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-鎓化合物（本文称为“二氨基吩噻嗪鎓化合物”）的方法，包括甲基氯化铑（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）; 氯化物盐形成（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。

10. 发明申请

US20080207603A1 Methods of Chemical Synthesis and Purification of Diaminophenothiazinium Compounds Including Methylthioninium Chloride (Mtc) 有权
公开(公告)号：US20080207603A1
公开(公告)日：2008-08-28
申请号：US11575845
申请日：2005-09-21
申请人： John Mervyn David Storey , James Peter Sinclair , Colin Marshall , Han Wan Tan , Claude Michel Wischik
发明人： John Mervyn David Storey , James Peter Sinclair , Colin Marshall , Han Wan Tan , Claude Michel Wischik
IPC分类号： A61K31/5415 , C07D279/20 , C12N13/00 , A61P25/28 , A61P35/04 , A61P31/00
CPC分类号： C09B19/02 , C07D279/18
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 “diaminophenothiazinium compounds”) including Methylthioninium 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. Wherein: each of R1 and R9 is independently selected from: —H; C1-4 alkenyl; and halogenated C1-4alkyl; each of R3NA and R3NB is independently selected from: C1-4 alkyl; C2-4alkenyl; and halogenated C4-1 alkyl; each of R7NA and R7NB is independently selected from: C1-4 alkyl; C2-4alkenyl; and halogenated C1-4 alkyl; and X is one or more anionic counter ions to achieve electrical neutrality.

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