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1. 发明公开

EP2205245A1 THERAPEUTIC USE OF DIAMINOPHENOTHIAZINES 有权转让
标题翻译： DIAMINOPHENOTHIAZINEN的治疗用途
公开(公告)号：EP2205245A1
公开(公告)日：2010-07-14
申请号：EP08806465.4
申请日：2008-10-01
申请人： Wista Laboratories Ltd.
发明人： WISCHIK, Claude, Michel , WISCHIK, Damon, Jude , STOREY, John, Mervyn, David , HARRINGTON, Charles, Robert
IPC分类号： A61K31/542 , A61P25/28
CPC分类号： A61K31/5415 , A61K9/0065 , A61K31/542 , A61K45/06
摘要： The present invention relates generally to methods and materials for use in the treatment or prophylaxis of diseases, for example cognitive disorders, using diaminophenothiazines. In particular it relates to treatments having optimised pharmacokinetic properties, and dosage forms are intended to improve the relative cognitive or CNS benefits of the diaminophenothiazines, for instance compared to haematological effects.

2. 发明授权

EP2338059B1 Ligands for aggregated tau molecules 有权转让
标题翻译：配体聚集τ分子
公开(公告)号：EP2338059B1
公开(公告)日：2015-04-08
申请号：EP09785147.1
申请日：2009-09-23
申请人： WisTa Laboratories Ltd.
发明人： KEMP, Steven, John , STOREY, Lynda, Jane , STOREY, John, Mervyn, David , RICKARD, Janet , HARRINGTON, Charles, Robert , WISCHIK, Claude, Michel , CLUNAS, Scott , HEINRICH, Tobias, Kerst
IPC分类号： G01N33/68 , C07D417/12 , C07D471/04 , C07D487/04 , C07D277/66 , C07D513/04
CPC分类号： G01N33/6896 , C07D277/66 , C07D417/12 , C07D471/04 , C07D487/04 , C07D513/04 , G01N2333/4709 , G01N2800/2821 , Y10T436/14 , Y10T436/147777 , Y10T436/17 , Y10T436/18

3. 发明公开

EP2673266A1 PHENOTHIAZINE DIAMINIUM SALTS AND THEIR USE 有权转让
标题翻译：尼日利亚VERWENDUNG公司的PHENOTHIAZIN-DIAMINIUM-SALZE
公开(公告)号：EP2673266A1
公开(公告)日：2013-12-18
申请号：EP11749476.5
申请日：2011-08-15
申请人： WisTa Laboratories Ltd.
发明人： 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 , MARSHALL, Colin , 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 , 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。

4. 发明公开

EP2338059A1 LIGANDS FOR AGGREGATED TAU MOLECULES 有权转让
标题翻译：配体聚集τ分子
公开(公告)号：EP2338059A1
公开(公告)日：2011-06-29
申请号：EP09785147.1
申请日：2009-09-23
申请人： Wista Laboratories Ltd.
发明人： KEMP, Steven, John , STOREY, Lynda, Jane , STOREY, John, Mervyn, David , RICKARD, Janet , HARRINGTON, Charles, Robert , WISCHIK, Claude, Michel , CLUNAS, Scott , HEINRICH, Tobias, Kerst
IPC分类号： G01N33/68 , C07D275/04 , C07D277/66 , C07D279/06
CPC分类号： G01N33/6896 , C07D277/66 , C07D417/12 , C07D471/04 , C07D487/04 , C07D513/04 , G01N2333/4709 , G01N2800/2821 , Y10T436/14 , Y10T436/147777 , Y10T436/17 , Y10T436/18
摘要： Provided are certain benzothiazole, imidazothiazole, imidazopyrimidine and imidazopyridine compounds, including, for example:formula (I) and pharmaceutically and physiologically acceptable salts, hydrates, and solvates thereof. Such compounds can be used as diagnostic ligands or labels of tau protein and PHF.

5. 发明授权

EP2004155B1 INHIBITORS OF PROTEIN AGGREGATION 有权转让
标题翻译：蛋白质聚集抑制剂
公开(公告)号：EP2004155B1
公开(公告)日：2018-02-21
申请号：EP07712961.7
申请日：2007-03-28
申请人： WisTa Laboratories Ltd.
发明人： WISCHIK, Claude, Michel , RICKARD, Janet, Elizabeth , HARRINGTON, Charles, Robert , HORSLEY, David
IPC分类号： A61K31/5415 , A61P25/28 , A61P25/16 , A61K51/04 , A61K49/00
CPC分类号： C07D279/20 , A61K31/5415 , A61K49/0002 , A61K49/003 , A61K51/0465 , G01N33/6896 , G01N2800/2835 , Y02A50/393 , Y02A50/411
摘要： The invention relates generally to the use of diaminophenothiazine compounds to inhibit or reverse the aggregation of synuclein, and for their use in the manufacture of medicaments for this purpose (e.g. for the treatment of Parkinson's Disease). Also provided are related methods of detecting or labelling of aggregated synuclein.

6. 发明授权

EP2057136B1 METHODS OF SYNTHESIS AND/OR PURIFICATION OF DIAMINOPHENOTHIAZINIUM COMPOUNDS 有权转让
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：EP2057136B1
公开(公告)日：2013-05-22
申请号：EP07733509.9
申请日：2007-07-10
申请人： Wista Laboratories Ltd.
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); FTD and 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 (MCl); 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).

7. 发明公开

EP2057136A2 METHODS OF SYNTHESIS AND/OR PURIFICATION OF DIAMINOPHENOTHIAZINIUM COMPOUNDS 有权转让
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：EP2057136A2
公开(公告)日：2009-05-13
申请号：EP07733509.9
申请日：2007-07-10
申请人： Wista Laboratories Ltd.
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); FTD and 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 (MCl); 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）。

8. 发明公开

EP2001556A1 THIONINIUM COMPOUNDS AND THEIR USE 有权转让
标题翻译：锍化合物及其用途
公开(公告)号：EP2001556A1
公开(公告)日：2008-12-17
申请号：EP07712962.5
申请日：2007-03-28
申请人： Wista Laboratories Ltd.
发明人： WISCHIK, Claude, Michel , RICKARD, Janet, Elizabeth , HARRINGTON, Charles, Robert , HORSLEY, David , STOREY, John, Mervyn, David , MARSHALL, Colin , SINCLAIR, James, Peter
IPC分类号： A61P25/28 , A61K31/5415
CPC分类号： A61K31/5415
摘要： This invention pertains generally to processes, uses, methods and materials utilising particular diaminophenothiazinium compounds, specifically, ETC, DEMTC, DMETC, DEETC, MTZ, ETZ, MTI, MTI.HI, ETI, ETI.HI, MTN, and ETN. These compounds are useful as drugs, for example, in the treatment of tauopathies, such as Alzheimer's disease.

9. 发明授权

EP2013191B3 3,7-DIAMINO-10H-PHENOTHIAZINE SALTS AND THEIR USE 有权转让
公开(公告)号：EP2013191B3
公开(公告)日：2019-02-27
申请号：EP07732164.4
申请日：2007-03-28
申请人： Wista Laboratories Ltd.
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

10. 发明授权

EP2205245B1 THERAPEUTIC USE OF DIAMINOPHENOTHIAZINES 有权转让
标题翻译：二氨基苯并噻嗪类的治疗应用
公开(公告)号：EP2205245B1
公开(公告)日：2015-06-24
申请号：EP08806465.4
申请日：2008-10-01
申请人： WisTa Laboratories Ltd.
发明人： WISCHIK, Claude, Michel , WISCHIK, Damon, Jude , STOREY, John, Mervyn, David , HARRINGTON, Charles, Robert
IPC分类号： A61K31/5415 , A61P25/28
CPC分类号： A61K31/5415 , A61K9/0065 , A61K31/542 , A61K45/06

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