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1. 发明公开

KR20180054900A 의약으로서 3,6-이중치환된 크산틸륨 염 审中-公开
公开(公告)号：KR20180054900A
公开(公告)日：2018-05-24
申请号：KR20187013290
申请日：2009-12-10
申请人： WISTA LAB LTD
发明人： CLUNAS SCOTT , STOREY JOHN MERVYN DAVID , RICKARD JANET ELIZABETH , HORSLEY DAVID , HARRINGTON CHARLES ROBERT , WISCHIK CLAUDE MICHEL
IPC分类号： C07D311/82 , A61K31/352 , A61K31/4353 , A61K31/4375 , A61K31/4745 , A61K31/498 , C07D241/46 , C07D311/90 , C07D335/12 , C07D491/22
CPC分类号： C07D311/82 , A61K9/0053 , A61K31/352 , A61K31/382 , A61K31/4025 , A61K31/4545 , A61K31/4745 , A61K31/498 , A61K31/5377 , A61K31/538 , A61K45/06 , A61K49/00 , C07D241/46 , C07D265/38 , C07D311/84 , C07D311/90 , C07D335/12 , C07D335/14 , C07D335/20 , C07D491/16 , C07D491/22 , C07D493/16 , C09B11/24 , C09B11/28 , C09B17/00 , C09B19/00 , C09B21/00 , C09B57/00 , G01N33/6896 , G01N2800/7047
摘要： 본발명은대체로본원에더욱정의한바와같은하기화학식 I 및화학식 II의화합물을포함하는, 특정크산틸륨화합물을이용하는공정, 용도, 방법및 재료에관한것이다. 이들화합물은, 약물, 예를들어타우병증, 예컨대알츠하이머병의치료에서의약물로서유용하다.

2. 发明公开

KR20200133394A 의약으로서 3,6-이중치환된 크산틸륨 염 审中-公开
公开(公告)号：KR20200133394A
公开(公告)日：2020-11-27
申请号：KR20207033404
申请日：2009-12-10
申请人： WISTA LAB LTD
发明人： CLUNAS SCOTT , STOREY JOHN MERVYN DAVID , RICKARD JANET ELIZABETH , HORSLEY DAVID , HARRINGTON CHARLES ROBERT , WISCHIK CLAUDE MICHEL
IPC分类号： C07D311/82 , A61K31/352 , A61K31/4353 , A61K31/4375 , A61K31/4745 , A61K31/498 , C07D241/46 , C07D311/90 , C07D335/12 , C07D491/22
摘要： 본발명은대체로본원에더욱정의한바와같은하기화학식 I 및화학식 II의화합물을포함하는, 특정크산틸륨화합물을이용하는공정, 용도, 방법및 재료에관한것이다. 이들화합물은, 약물, 예를들어타우병증, 예컨대알츠하이머병의치료에서의약물로서유용하다. JPEGpat00075.jpg24123

3. 发明申请

WO2007110627A3 3,7-DIAMINO-10H-PHENOTHIAZINE SALTS AND THEIR USE 审中-公开
标题翻译： 3,7-二氨基-10H-苯并恶嗪盐及其用途
公开(公告)号：WO2007110627A3
公开(公告)日：2007-11-22
申请号：PCT/GB2007001103
申请日：2007-03-28
申请人： WISTA LAB LTD , WISCHIK CLAUDE MICHEL , RICKARD JANET ELIZABETH , HARRINGTON CHARLES ROBERT , HORSLEY DAVID , STOREY JOHN MERVYN DAVID , MARSHALL COLIN , SINCLAIR JAMES PETER , BADDELEY THOMAS CRAVEN
发明人： WISCHIK CLAUDE MICHEL , RICKARD JANET ELIZABETH , HARRINGTON CHARLES ROBERT , HORSLEY DAVID , STOREY JOHN MERVYN DAVID , MARSHALL COLIN , SINCLAIR JAMES PETER , BADDELEY THOMAS CRAVEN
IPC分类号： C07D279/20 , A61K31/5415 , A61P25/28
CPC分类号： A61K31/5415 , C07D279/20 , C07D279/22 , C09B21/00
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 R 1 and R 9 is independently selected from: -H; C 1-4 alkyl; C 2-4 alkenyl; and halogenated C 1-4 alkyl; each of R 3NA and R 3NB is independently selected from: -H; C 1-4 alkyl; C 2-4 alkenyl; and halogenated C 1-4 alkyl; each of R 7NA and R 7NB is independently selected from: -H; C 1-4 alkyl; C 2-4 alkenyl; and halogenated C 1-4 alkyl; each of HX 1 and HX 2 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，特别是下式的某些3,7-二氨基-10H-吩噻嗪（DAPTZ）化合物，其中：每个R 1，其中R 9和R 9独立地选自：-H; ç_{1-4 烷基; ç_{2-4 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; ç_{1-4 烷基; ç_{2-4 烯基; 和卤代C 1-4烷基; R 7NA和R 7NB中的每一个独立地选自：-H; ç_{1-4 烷基; ç_{2-4 烯基; 和卤代C 1-4烷基; HX 1和HX 2各自独立地为质子酸; 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，以及还用作相应的氧化th drugs类药物（例如甲硫in氯化物，MTC）的前体药物。}}}}}}

4. 发明申请

WO2011036561A8 PROCESS 审中-公开
标题翻译：处理
公开(公告)号：WO2011036561A8
公开(公告)日：2012-04-19
申请号：PCT/IB2010002543
申请日：2010-09-23
申请人： WISTA LAB LTD , HILFIKER ROLF , RAGER TIMO
发明人： HILFIKER ROLF , RAGER TIMO
IPC分类号： C07D279/18 , A61K31/5415 , A61P31/00 , A61P35/00
CPC分类号： C07D279/18
摘要： Substantially pure methylthioninium chloride pentahydrate form A is prepared from methylthioninium chloride by phase equilibration of suspensions, crystallization or solvent evaporation, whereby the water content of the solvent corresponds to a water activity of at least 0.4 at 25°C, and controlled drying of said methylthioninium chloride pentahydrate form A within its stability ranges of humidity, pressure and temperature.
摘要翻译：基本上纯的甲基硫酸镧五水合物形式A由甲基硫堇氯化物通过悬浮液的相平衡，结晶或溶剂蒸发制备，其中溶剂的水含量对应于在25℃下至少为0.4的水活度，并控制所述甲基硫堇氯化物五水合物形式A在其稳定的湿度，压力和温度范围内。

5. 发明申请

WO2008155533A2 COMPOUNDS FOR TREATMENT 审中-公开
标题翻译：化合物治疗
公开(公告)号：WO2008155533A2
公开(公告)日：2008-12-24
申请号：PCT/GB2008002066
申请日：2008-06-17
申请人： WISTA LAB LTD , WISCHIK CLAUDE MICHEL , HARBARAN DOMINIC VENAY , RIEDEL GERNOT , DEIANA SERENA , GOATMAN ELIZABETH ANNE , WISCHIK DAMON JUDE , MURRAY ALISON DOROTHY , STAFF ROGER TODD
发明人： WISCHIK CLAUDE MICHEL , HARBARAN DOMINIC VENAY , RIEDEL GERNOT , DEIANA SERENA , GOATMAN ELIZABETH ANNE , WISCHIK DAMON JUDE , MURRAY ALISON DOROTHY , STAFF ROGER TODD
IPC分类号： A61K31/5415 , A61P25/28
CPC分类号： A61K31/5415
摘要： The present invention relates generally to methods and materials based on diaminophenothiazines for use in the treatment of Mild Cognitive Impairment (MCI).
摘要翻译：本发明一般涉及用于治疗轻度认知障碍（MCI）的二氨基吩噻嗪的方法和材料。

6. 发明申请

WO2012072977A8 FORMULATIONS COMPRISING METHYLTHIONINIUM CHLORIDE 审中-公开
标题翻译：包含甲基氯化铵的配方
公开(公告)号：WO2012072977A8
公开(公告)日：2012-09-20
申请号：PCT/GB2011001662
申请日：2011-11-30
申请人： WISTA LAB LTD , KHAN KARRAR AHMAD
发明人： KHAN KARRAR AHMAD
IPC分类号： A61K9/14 , A61K9/20 , A61K31/5415 , A61P25/28
CPC分类号： A61K31/5415 , A61K9/1652 , A61K9/20 , A61K9/2054 , A61K9/2095 , A61K9/4866 , C07D279/18
摘要： Solid dosage forms of methylthioninium chloride (MTC) further comprise at least one diluent suitable for direct compression. The MTC exists in a substantially pure and stable polymorphic form. The solid dosage forms may preferably be prepared by direct compression methods.
摘要翻译：甲基硫堇（MTC）的固体剂型还包含至少一种适于直接压制的稀释剂。 MTC以基本上纯且稳定的多晶型形式存在。固体剂型可优选通过直接压制方法制备。

7. 发明申请

WO2012072977A3 FORMULATIONS COMPRISING METHYLTHIONIUM CHLORIDE 审中-公开
标题翻译：包含甲基氯化铝的配方
公开(公告)号：WO2012072977A3
公开(公告)日：2012-08-16
申请号：PCT/GB2011001662
申请日：2011-11-30
申请人： WISTA LAB LTD , KHAN KARRAR AHMAD
发明人： KHAN KARRAR AHMAD
IPC分类号： A61K9/14 , A61K9/20 , A61K31/5415 , A61P25/28
CPC分类号： A61K31/5415 , A61K9/1652 , A61K9/20 , A61K9/2054 , A61K9/2095 , A61K9/4866 , C07D279/18
摘要： Solid dosage forms of methylthioninium chloride (MTC) further comprise at least one diluent suitable for direct compression. The MTC exists in a substantially pure and stable polymorphic form. The solid dosage forms may preferably be prepared by direct compression methods.
摘要翻译：甲基硫堇（MTC）的固体剂型还包含至少一种适于直接压制的稀释剂。 MTC以基本上纯且稳定的多晶型形式存在。固体剂型可优选通过直接压制方法制备。

8. 发明申请

WO2010067085A3 SYNTHESIS OF 9-(ARYLALKYL)-1,2,3,4-TETRAHYDRO-?-CARBOLINE AND ANALOGUES AND INTERMEDIATES 审中-公开
标题翻译： 9-（芳基烷基）-1,2,3,4-四氢-α-咔啉及其类似物和中间体的合成
公开(公告)号：WO2010067085A3
公开(公告)日：2010-08-12
申请号：PCT/GB2009002873
申请日：2009-12-11
申请人： WISTA LAB LTD , WILLIAMSON CRAIG , STOREY JOHN MERVYN DAVID
发明人： WILLIAMSON CRAIG , STOREY JOHN MERVYN DAVID
IPC分类号： C07D213/06 , C07D401/12 , C07D413/06 , C07D471/04 , C07D491/04 , C07D495/04
CPC分类号： C07D213/06 , C07D401/12 , C07D413/06 , C07D471/04 , C07D491/04 , C07D495/04
摘要： The present invention pertains generally to methods of preparing certain 9-(arylalkyl)- 1,2,3,4-tetrahydro-?-carboline compounds and their analogues, and especially to methods of preparing dimebon. The present invention also pertains to methods of preparing certain intermediate compounds which find use in the synthesis of the 9-(arylalkyl)-1,2,3,4-tetrahydro-?-carboline compounds.
摘要翻译：本发明一般涉及制备某些9-（芳基烷基）-1,2,3,4-四氢-α-咔啉化合物及其类似物的方法，特别涉及制备Dimebon的方法。本发明还涉及制备用于合成9-（芳基烷基）-1,2,3,4-四氢-α-咔啉化合物的某些中间体化合物的方法。

9. 发明申请

WO2008007074A3 METHODS OF SYNTHESIS AND/OR PURIFICATION OF DIAMINOPHENOTHIAZINIUM COMPOUNDS 审中-公开
标题翻译：二氨基苯并噻唑鎓化合物的合成和/或纯化方法
公开(公告)号：WO2008007074A3
公开(公告)日：2008-02-28
申请号：PCT/GB2007002570
申请日：2007-07-10
申请人： WISTA LAB LTD , WISCHIK CLAUDE MICHEL , STOREY JOHN MERVYN DAVID , MARSHALL COLIN , SINCLAIR JAMES PETER , BADDELEY THOMAS CRAVEN
发明人： WISCHIK CLAUDE MICHEL , STOREY JOHN MERVYN DAVID , MARSHALL COLIN , SINCLAIR JAMES PETER , BADDELEY THOMAS CRAVEN
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”）的合成和/或纯化方法，包括甲基硫堇鎓氯化物（MTC）（也称为亚甲蓝）。本发明还涉及所得（高纯度）化合物，包含它们的组合物（例如片剂，胶囊），以及它们在灭活病原体的方法中的用途，以及医学治疗，预防和诊断等的方法，一种tau蛋白病; τ蛋白质聚集的疾病; 阿尔茨海默病（AD）; 皮克氏病; 进行性核上性麻痹（PSP）; 额颞叶痴呆（FTD）; 与17号染色体相关的帕金森综合征（FTDP-17）; 去抑制 - 痴呆 - 帕金森病 - 肌萎缩综合征（DDPAC）; 苍白球 - 黑质变性（PPND）; 关岛 - ALS综合征; pallido-nigro-luysian degeneration（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; 原虫感染; 寄生虫感染; 疟疾; 内脏利什曼病; 非洲昏睡病; 弓形虫病; 贾第虫病; 南美锥虫病; 丙型肝炎病毒（HCV）感染; 人类免疫缺陷病毒（HIV）感染; 西尼罗河病毒（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）; 药物性帕金森综合征; 和纯自主神经衰竭（PAF）。

10. 发明申请

WO2012107706A8 PHENOTHIAZINE DIAMINIUM SALTS AND THEIR USE 审中-公开
标题翻译：双酚钠金属盐及其使用
公开(公告)号：WO2012107706A8
公开(公告)日：2013-09-19
申请号：PCT/GB2011001221
申请日：2011-08-15
申请人： WISTA LAB LTD , MARSHALL COLIN , CLUNAS SCOTT , STOREY JOHN MERVYN DAVID , SINCLAIR JAMES PETER , BADDELEY THOMAS CRAVEN , ISHAQ AHTSHAM , SIMPSON MICHAEL , WILLIAMSON CRAIG , WOOD BARRY ALAN , WISCHIK CLAUDE MICHEL , HARRINGTON CHARLES ROBERT , RICKARD JANET ELIZABETH , HORSLEY DAVID , LOH YIN SZE , KHAN KARRAR AHMAD
发明人： MARSHALL COLIN , CLUNAS SCOTT , STOREY JOHN MERVYN DAVID , SINCLAIR JAMES PETER , BADDELEY THOMAS CRAVEN , ISHAQ AHTSHAM , SIMPSON MICHAEL , WILLIAMSON CRAIG , WOOD BARRY ALAN , WISCHIK CLAUDE MICHEL , HARRINGTON CHARLES ROBERT , RICKARD JANET ELIZABETH , HORSLEY DAVID , LOH YIN SZE , KHAN KARRAR AHMAD
IPC分类号： C07D279/20 , A61K31/5415 , A61P25/00
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
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。

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