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1. 发明授权

US07737138B2 Methods of treatment of a tauopathy condition comprising the use of thioninium compounds 有权
标题翻译：包括使用硫铊化合物的tau病变病况的治疗方法
公开(公告)号：US07737138B2
公开(公告)日：2010-06-15
申请号：US11391675
申请日：2006-03-29
申请人： Claude M. Wischik , Janet E. Rickard , Charles R. Harrington , David Horsley , John M. D. Storey , Colin Marshall , James P. Sinclair , Han Wan Tan
发明人： Claude M. Wischik , Janet E. Rickard , Charles R. Harrington , David Horsley , John M. D. Storey , Colin Marshall , James P. Sinclair , Han Wan Tan
IPC分类号： A61K31/5415
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-diaminophenothiazin-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). 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，包括氯化铁偶氮（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。

2. 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。

3. 发明授权

US07790881B2 Methods of chemical synthesis and purification of diaminophenothiazinium compounds including methylthioninium chloride (MTC) 有权
标题翻译：二氨基吩噻嗪鎓化合物的化学合成和纯化方法，包括甲基硫堇（MTC）
公开(公告)号：US07790881B2
公开(公告)日：2010-09-07
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
发明人： John Mervyn David Storey , James Peter Sinclair , Colin Marshall , Han Wan Tan
IPC分类号： C07D279/20 , A61K31/5415
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.
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包括甲基硫堇（MTC）在内的某些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，（也称为亚甲蓝）。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。其中R 1和R 9各自独立地选自：-H; C 1-4烯基; 和卤代C 1-4烷基; R3NA和R3NB中的每一个独立地选自：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：C 1-4烷基; C2-4烯基; 和卤代C 1-4烷基; 并且X是一种或多种阴离子抗衡离子以实现电中性。

4. 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.

5. 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。

6. 发明申请

US20060287523A1 Methods of chemical synthesis and purification of diaminophenothiazinium compounds including methylthioninium chloride (MTC) 有权
标题翻译：二氨基吩噻嗪鎓化合物的化学合成和纯化方法，包括甲基硫堇（MTC）
公开(公告)号：US20060287523A1
公开(公告)日：2006-12-21
申请号：US11391675
申请日：2006-03-29
申请人： Claude Wischik , Janet Rickard , Charles Harrington , David Horsley , John Storey , Colin Marshall , James Sinclair , Han Tan
发明人： Claude Wischik , Janet Rickard , Charles Harrington , David Horsley , John Storey , Colin Marshall , James Sinclair , Han Tan
IPC分类号： C07D279/18
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-diaminophenothiazin-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). 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，包括氯化铁偶氮（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。

7. 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。

8. 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。

9. 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。

10. 发明申请

US20110118242A1 3,7-DIAMINO-10H-PHINOTHIAZINE SALTS AND THEIR USE 有权
标题翻译： 3,7-DIAMINO-10H-PHINOTHIAZINE SALTS及其使用
公开(公告)号：US20110118242A1
公开(公告)日：2011-05-19
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： A61K31/5415 , A61P25/28
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。

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