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    METHOD FOR PREVENTION OF PREMATURE POLYMERIZATION
    2.
    发明公开
    METHOD FOR PREVENTION OF PREMATURE POLYMERIZATION 审中-公开
    VERFAHREN ZUR VERHINDERUNG DER VORZEITIGEN POLYMERISATION

    公开(公告)号：EP3072879A1

    公开(公告)日：2016-09-28

    申请号：EP15000894.4

    申请日：2015-03-26

    申请人： NITTO EUROPE N.V

    发明人： Bossaert, Greet ,  Gomes, Monica ,  Forier, Bart

    IPC分类号： C07C69/54 ,  C07C7/20 ,  C07C57/04 ,  C07D279/18

    CPC分类号： C07D279/20 ,  C07C67/03 ,  C07C67/62 ,  C07D279/18 ,  C08F220/18 ,  C08G2261/58 ,  C08L33/08 ,  C09B17/00 ,  C09B19/00 ,  C09B21/00 ,  C09B49/06 ,  C07C69/54

    摘要： The present invention relates to a method for prevention of premature polymerization during the preparation, purification, transportation and storage of a polymerizable compound with at least one conjugated unsaturated group in the presence of an azine dye-based compound as inhibitor. Further the present invention relates to methods of preparing such inhibitors as well as to the inhibitors itself, as well as to methods of improving solubility and stability of dissolved inhibitors.

    摘要翻译： 本发明涉及在作为抑制剂的吖嗪类染料类化合物的存在下，在具有至少一个共轭不饱和基团的聚合性化合物的制备，精制，输送和储存过程中，防止过早聚合的方法。 此外，本发明还涉及制备这种抑制剂以及抑制剂本身的方法，以及提高溶解性抑制剂的溶解性和稳定性的方法。

    Methods of synthesis and/or purification of diaminophenothiazinium compounds
    4.
    发明公开
    Methods of synthesis and/or purification of diaminophenothiazinium compounds 有权
    一种用于Diaminophenothiaziniumverbindungen的合成和/或纯化过程

    公开(公告)号：EP2457905A1

    公开(公告)日：2012-05-30

    申请号：EP11173338.2

    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).

    Methods of synthesis and/or purification of diaminophenothiazinium compounds
    5.
    发明公开
    Methods of synthesis and/or purification of diaminophenothiazinium compounds 有权
    二氨基吩噻嗪鎓化合物的合成和/或纯化方法

    公开(公告)号：EP2457904A1

    公开(公告)日：2012-05-30

    申请号：EP11173334.1

    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-diaminophenothiazin-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); disinhibitiondementia-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FTD和帕金森综合征（FTDP-17）; 去抑制性痴呆 - 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）。

    NEUROFIBRILLARY LABELS
    6.
    发明授权
    NEUROFIBRILLARY LABELS 有权
    神经纤维MARKER

    公开(公告)号：EP1421389B1

    公开(公告)日：2012-05-02

    申请号：EP02720102.9

    申请日：2002-03-20

    申请人： WisTa Laboratories Ltd.

    发明人： WISCHIK, Claude, Michel ,  HARRINGTON, Charles, Robert ,  RICKARD, Janet, Elizabeth ,  HORSLEY, David

    IPC分类号： G01N33/68 ,  C07D277/62 ,  G01N33/58 ,  C07D279/18

    CPC分类号： C07D417/12 ,  C07D277/66 ,  C07D279/20 ,  G01N33/583 ,  G01N33/6896

    摘要： Disclosed are methods for determining the stage of neurofibrillary degeneration associated with a tauopathy in a subject believed to suffer from the disease, which methods comprise the steps of: (i) introducing into the subject a ligand capable of labelling aggregated paired helical filament (PHF) tau protein, (ii) determining the presence and/or amount of ligand bound to extracellular aggregated PHF tau in the medial temporal lobe of the brain of the subject, (iii) correlating the result of the determination made in (ii) with the extent of neurofibrillary degeneration in the subject. The methods can be used for pre-mortem diagnosis and staging of tauopathies such as Alzheimer's Disease. Preferred ligands include sulphonated-benzothiazole-like compounds and diaminophenothiazines. Novel ligands (e.g. sulphonated-benzothiazole-like compounds) are also provided. The method may also include the use of 'blocking ligands' to block competing binding sites. In other aspects the invention provides in vitro methods for identifying ligands capable of labeling aggregated PHF tau protein, the methods comprising the steps of: (i) providing a first agent suspected of being capable of labeling aggregated PHF tau protein, (ii) contacting (a) a tau protein or a derivative thereof containing the tau core fragment bound to a solid phase so as to expose a high affinity tau capture site, with (b) a liquid phase tau protein or derivative thereof capable of binding to the solid phase tau protein or derivative, and (c) said selected first agent and (d) a second agent known to be tau-tau binding inhibitor, (iii) selecting first agent which fully or partially relieves the inhibition of binding of the liquid phase tau protein or derivative of (b) to the solid phase tau protein or derivative of (a) by the inhibitor (d). Ligands may also be tested to confirm that they are not themselves inhibitors.

    PHENOTHIAZINES IN PRILL FORM
    7.
    发明授权
    PHENOTHIAZINES IN PRILL FORM 有权
    苯丙胺酸盐

    公开(公告)号：EP1250329B1

    公开(公告)日：2010-02-03

    申请号：EP00977769.9

    申请日：2000-12-01

    申请人： Cytec Industries Inc.

    发明人： VANZIN, David, Alan

    IPC分类号： C07D279/20 ,  B01J2/04

    CPC分类号： B01J2/04 ,  C07D279/20 ,  C09K15/30

    摘要： The invention relates to (a) phenothiazine or a phenothiazine analog or derivative (phenothiazine material) in the form of prills of a generally spherical shape containing very low levels of fines and also (b) a method of forming a phenothiazine material in prill form having a generally spherical shape. The prilled phenothiazine material exhibits improved handling, flowability and dissolation times, while minimizing the generation of fines, and the problems of irritation and sensitization through exposure to such fines.