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1. 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）。

2. 发明申请

WO2002059150A2 MATERIALS AND METHODS RELATING TO PROTEIN AGGREGATION IN NEURODEGENERATIVE DISEASE 审中-公开
标题翻译：与神经退行性疾病中蛋白质聚集有关的材料和方法
公开(公告)号：WO2002059150A2
公开(公告)日：2002-08-01
申请号：PCT/GB2002/000005
申请日：2002-01-02
申请人： THE UNIVERSITY COURT OF THE UNIVERSITY OF ABERDEEN , WISCHIK, Claude, Michel , RICKARD, Janet, Elizabeth , HORSLEY, David , HARRINGTON, Charles, Robert , THEURING, Franz , STAMER, Karsten , ZABKE, Claudia
发明人： WISCHIK, Claude, Michel , RICKARD, Janet, Elizabeth , HORSLEY, David , HARRINGTON, Charles, Robert , THEURING, Franz , STAMER, Karsten , ZABKE, Claudia
IPC分类号： C07K14/705
CPC分类号： C12N15/8509 , A01K67/0275 , A01K2207/15 , A01K2217/00 , A01K2217/05 , A01K2217/20 , A01K2227/105 , A01K2267/0312 , A01K2267/0318 , C07K14/4711 , C07K2319/00 , G01N33/6896 , G01N2500/00
摘要： Disclosed are methods of inducing or modelling the pathological state of an aggregating disease protein (ADP - e.g. tau protein) which is associated with a disease state in which the ADP aggregates pathologically (e.g. Alzheimer's disease) through an induced conformational polymerisation interaction, the method being characterised by the step of providing a membrane-localisable fusion protein comprising (i) an aggregating portion, which is derived from the ADP, or from a protein which initiates pathological aggregation of the ADP, (ii) a heterologous membrane-localising portion. Membrane-localisation of the ADP-based fusion protein is believed to cause the high-affinity capture site of the ADP protein to become exposed such that aggregation of further ADP, which may be native or heterologous to the system, to be promoted. The method can be carried out in vitro, or in cell- and animal-models, and may be used to screen for modulators of the aggregation process by monitoring aggregation e.g. by monitoring the production of the ADP-related degradation products resulting from the aggregation. Also provided are materials, processes for use in or with the methods.
摘要翻译：公开了诱导或模拟聚集性疾病蛋白（ADP-例如tau蛋白）的病理状态的方法，所述聚集性疾病蛋白与疾病状态相关，所述疾病状态中ADP通过病理学方式（例如阿尔茨海默氏病）聚集诱导构象聚合相互作用，所述方法的特征在于提供膜 - 可定位融合蛋白的步骤，所述融合蛋白包含（i）衍生自ADP的聚集部分或来自引发ADP病理性聚集的蛋白质，（ii）异源膜定位部分。据信ADP基融合蛋白的膜定位导致ADP蛋白的高亲和力捕获位点暴露，从而促进进一步ADP的聚集，所述ADP可为体系天然或异源的。该方法可以在体外进行，或者在细胞模型和动物模型中进行，并且可以用于通过监测聚集来筛选聚集过程的调节剂。通过监测由聚集产生的ADP相关降解产物的产生。还提供了用于或与这些方法一起使用的材料，过程。

3. 发明申请

WO02055720A2 MATERIALS AND METHODS RELATING TO PROTEIN AGGREGATION IN NEURODEGENERATIVE DISEASE 审中-公开
标题翻译：相关蛋白质聚集在神经病变疾病中的材料与方法
公开(公告)号：WO02055720A2
公开(公告)日：2002-07-18
申请号：PCT/GB0200153
申请日：2002-01-15
申请人： UNIV ABERDEEN , WISCHIK CLAUDE MICHEL , HORSLEY DAVID , RICKARD JANET ELIZABETH , HARRINGTON CHARLES ROBERT
发明人： WISCHIK CLAUDE MICHEL , HORSLEY DAVID , RICKARD JANET ELIZABETH , HARRINGTON CHARLES ROBERT
IPC分类号： G01N33/50 , A61K31/00 , A61K31/5415 , A61K45/00 , A61K47/22 , A61P25/14 , A61P25/28 , C07K14/47 , C12N5/10 , C12N15/09 , C12Q1/02 , G01N27/447 , G01N33/15 , G01N33/53 , G01N33/577 , G01N33/68 , C12N15/85
CPC分类号： G01N33/6896 , A61K31/00 , A61K31/5415
摘要： Disclosed are methods of proteolytically converting a precursor protein (e.g. tau) to a product fragment (e.g. a 12 kd fragment) in a stable cell line, wherein the precursor protein is associated with a disease state in which the precursor protein aggregates pathologically (e.g. a tauopathy), and the methods comprise:(a) providing a stable cell line transfected with nucleic acid encoding: (i) a template fragment of the precursor protein such that the template fragment is constitutively expressed in the cell at a level which is not toxic to the cell; and (ii) the precursor protein, which protein is inducibly expressed in the cell in response to a stimulus, whereby interaction of the template fragment with the precursor protein causes a conformational change in the precursor protein such as to cause aggregation and proteolytic processing of the precursor protein to the product fragment. The method is preferably used to screen for modulators of the aggregation process by monitoring production (or modulation of production) of the product band or bands. Also provided are materials for used in the assays, plus medicaments, and related uses and processes, based on compounds which show high activity in the assay of the invention e.g. reduced diaminophenothiazines.
摘要翻译：公开了在稳定细胞系中将前体蛋白质（例如tau）蛋白水解转化成产物片段（例如12kd片段）的方法，其中前体蛋白质与其中前体蛋白质在病理学上聚集的疾病状态相关（例如， tau蛋白病），并且所述方法包括：（a）提供用核酸转染的稳定的细胞系，其编码：（i）前体蛋白的模板片段，使得模板片段在细胞中以不具有毒性的水平组成型表达到细胞; 和（ii）前体蛋白质，该蛋白质响应于刺激而在细胞中可诱导表达，由此模板片段与前体蛋白质的相互作用导致前体蛋白质的构象变化，从而导致蛋白质的聚集和蛋白水解加工前体蛋白到产物片段。该方法优选用于通过监测产品带或带的生产（或调制生产）来筛选聚集过程的调制器。还提供了用于测定中的材料，以及基于在本发明的测定中显示高活性的化合物的药物以及相关用途和方法，例如。还原二氨基吩噻嗪。

4. 发明申请

WO1989003993A1 PAIRED HELICAL FILAMENT CORE AND ANTIBODY THERETO USEFUL IN DIAGNOSING ALZHEIMER'S DISEASE 审中-公开
标题翻译：有用的诊断阿尔茨海默病的配对的螺旋纤维核和抗体
公开(公告)号：WO1989003993A1
公开(公告)日：1989-05-05
申请号：PCT/GB1988000867
申请日：1988-10-19
申请人： MEDICAL RESEARCH COUNCIL , WISCHIK, Claude, Michel , MILSTEIN, Cesar , KLUG, Aaron
发明人： MEDICAL RESEARCH COUNCIL
IPC分类号： G01N33/53
CPC分类号： C07K16/18 , C07K14/4711
摘要： Brain tissues of patients suffering from Alzheimer's disease show characteristic lesions, including those called neurofibrillary tangles. The tangles comprise dense accumulations of paired helical filaments (PHFs). This invention provides a pronase-resistant PHF core which remains after removal of peripheral PHF constituents by pronase. Unlike whole PHFs, the PHF core provides an antigen uniquely associated with neurofibrillary tangles. The invention includes antibodies to the PHF core useful in immunoassays for the core and further includes the diagnosis of Alzheimer's disease using such an immunoassay.
摘要翻译：患有阿尔茨海默病的患者的脑组织显示特征性病变，包括称为神经原纤维缠结的那些。缠结包括成对的螺旋丝（PHF）的密集堆积。本发明提供了通过链霉蛋白酶去除外周PHF成分后仍然保留的耐逆转酶PHF核心。与整个PHF不同，PHF核心提供与神经原纤维缠结唯一相关的抗原。本发明包括可用于核心免疫测定的PHF核心的抗体，并且还包括使用这种免疫测定法诊断阿尔茨海默氏病。

5. 发明申请

WO2021224144A1 METHYLTHIONINIUM COMPOUNDS FOR USE IN THE TREATMENT OF COVID-19 审中-公开
公开(公告)号：WO2021224144A1
公开(公告)日：2021-11-11
申请号：PCT/EP2021/061480
申请日：2021-04-30
申请人： WISTA LABORATORIES LTD. , WISCHIK, Claude Michel
发明人： ARASTOO, Mohammad , MAZANETZ, Michel Philip
IPC分类号： A61K31/5415 , A61K45/06 , A61P31/14
摘要： The present invention provides methods of treating COVID-19 in a subject using methylthioninium compounds.

6. 发明申请

WO2008155533A3 PHENOTHIAZINE COMPOUNDS FOR TREATING MILD COGNITIVE IMPAIRMENT 审中-公开
公开(公告)号：WO2008155533A3
公开(公告)日：2008-12-24
申请号：PCT/GB2008/002066
申请日：2008-06-17
申请人： WISTA LABORATORIES 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
摘要： The present invention relates generally to methods and materials based on diaminophenothiazines for use in the treatment of Mild Cognitive Impairment (MCI).

7. 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。

8. 发明申请

WO2007110627A2 3,7-DIAMINO-10H-PHENOTHIAZINE SALTS AND THEIR USE 审中-公开
标题翻译： 3,7-DIAMINO-10H-PHENOTHIAZINE SALTS及其使用
公开(公告)号：WO2007110627A2
公开(公告)日：2007-10-04
申请号：PCT/GB2007/001103
申请日：2007-03-28
申请人： WISTA LABORATORIES 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 , 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 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，更具体地说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， R SUP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 3 3 N 3和R 3NB各自独立地选自：-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H 2 O 2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，例如治疗tau蛋白病，例如阿尔茨海默氏病，还可用作相应的氧化硫堇药物（例如，氯化甲硫氨酸，MTC）的前药。}}}}}}

9. 发明申请

WO02055720A9 MATERIALS AND METHODS RELATING TO PROTEIN AGGREGATION IN NEURODEGENERATIVE DISEASE 审中-公开
公开(公告)号：WO02055720A9
公开(公告)日：2002-12-27
申请号：PCT/GB0200153
申请日：2002-01-15
申请人： UNIV ABERDEEN , WISCHIK CLAUDE MICHEL , HORSLEY DAVID , RICKARD JANET ELIZABETH , HARRINGTON CHARLES ROBERT
发明人： WISCHIK CLAUDE MICHEL , HORSLEY DAVID , RICKARD JANET ELIZABETH , HARRINGTON CHARLES ROBERT
IPC分类号： G01N33/50 , A61K31/00 , A61K31/5415 , A61K45/00 , A61K47/22 , A61P25/14 , A61P25/28 , C07K14/47 , C12N5/10 , C12N15/09 , C12Q1/02 , G01N27/447 , G01N33/15 , G01N33/53 , G01N33/577 , G01N33/68 , C12N15/85 , A61K31/54
CPC分类号： G01N33/6896 , A61K31/00 , A61K31/5415
摘要： Disclosed are methods of proteolytically converting a precursor protein (e.g. tau) to a product fragment (e.g. a 12 kd fragment) in a stable cell line, wherein the precursor protein is associated with a disease state in which the precursor protein aggregates pathologically (e.g. a tauopathy), and the methods comprise:(a) providing a stable cell line transfected with nucleic acid encoding: (i) a template fragment of the precursor protein such that the template fragment is constitutively expressed in the cell at a level which is not toxic to the cell; and (ii) the precursor protein, which protein is inducibly expressed in the cell in response to a stimulus, whereby interaction of the template fragment with the precursor protein causes a conformational change in the precursor protein such as to cause aggregation and proteolytic processing of the precursor protein to the product fragment. The method is preferably used to screen for modulators of the aggregation process by monitoring production (or modulation of production) of the product band or bands. Also provided are materials for used in the assays, plus medicaments, and related uses and processes, based on compounds which show high activity in the assay of the invention e.g. reduced diaminophenothiazines.

10. 发明申请

WO2021224146A1 METHYLTHIONINIUM COMPOUNDS FOR USE IN THE TREATMENT OF HYPOXEMIA 审中-公开
公开(公告)号：WO2021224146A1
公开(公告)日：2021-11-11
申请号：PCT/EP2021/061485
申请日：2021-04-30
申请人： WISTA LABORATORIES LTD. , WISCHIK, Claude Michel
发明人： ARASTOO, Mohammad , MAZANETZ, Michael Philip
IPC分类号： A61K31/5415 , A61K33/00 , A61P7/00 , A61P11/00 , A61P43/00
摘要： The present invention provides methods of alleviating hypoxemia in a subject through oral administration of a methylthioninium compound.

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