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    • 1. 发明授权
    • High purity diaminophenothiazinium compounds including methylthioninium chloride (MTC)
    • 高纯度二氨基吩噻嗪鎓化合物,包括甲基硫堇(MTC)
    • US09242946B2
    • 2016-01-26
    • US12875465
    • 2010-09-03
    • John Mervyn David StoreyJames Peter SinclairColin MarshallHan Wan TanClaude Michel Wischik
    • John Mervyn David StoreyJames Peter SinclairColin MarshallHan Wan TanClaude Michel Wischik
    • C07D279/18C09B19/02
    • A61K31/5415A61K9/0019A61K49/006C07D279/18C09B19/02G01N33/52Y02A50/393
    • 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.
    • 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. 发明申请
    • METHODS OF CHEMICAL SYNTHESIS AND PURIFICATION OF DIAMINOPHENOTHIAZINIUM COMPOUNDS INCLUDING METHYLTHIONINIUM CHLORIDE (MTC)
    • 化学合成和纯化包括氯化亚甲基氯化铵(MTC)的二氨基苯甲酸盐化合物的方法
    • US20110021510A1
    • 2011-01-27
    • US12875465
    • 2010-09-03
    • John Mervyn David STOREYJames Peter SINCLAIRColin MARSHALLHan Wan TANClaude Michel WISCHIK
    • John Mervyn David STOREYJames Peter SINCLAIRColin MARSHALLHan Wan TANClaude Michel WISCHIK
    • A61K31/5415C07D279/20A01N43/84A61P31/12A61P33/02A61P35/00A61P31/14A61P31/18A61P25/28A61P31/04
    • A61K31/5415A61K9/0019A61K49/006C07D279/18C09B19/02G01N33/52Y02A50/393
    • 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.
    • 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。
    • 9. 发明申请
    • Neurofibrillary labels
    • 神经原纤维标签
    • US20100285605A1
    • 2010-11-11
    • US12662887
    • 2010-05-10
    • Claude Michel WischikCharles Robert HarringtonJanet Elizabeth RickardDavid Horsley
    • Claude Michel WischikCharles Robert HarringtonJanet Elizabeth RickardDavid Horsley
    • G01N33/566
    • C07D417/12C07D277/66C07D279/20G01N33/583G01N33/6896
    • 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.
    • 公开了用于确定被认为患有疾病的受试者中与tau蛋白病相关的神经原纤维变性的阶段的方法,该方法包括以下步骤:(i)将能够标记聚集的成对螺旋丝(PHF)的配体引入受试者, tau蛋白,(ii)确定与受试者的脑内侧颞叶中细胞外聚集的PHF tau结合的配体的存在和/或量,(iii)将(ii)中确定的测定结果与 的神经原纤维变性。 这些方法可用于妊娠前诊断和分期的阿尔茨海默病等tau蛋白病。 优选的配体包括磺化苯并噻唑类化合物和二氨基吩噻嗪。 还提供了新的配体(例如磺化的苯并噻唑类化合物)。 该方法还可以包括使用“阻断配体”来阻止竞争结合位点。 在其它方面,本发明提供了用于鉴定能够标记聚集的PHF tau蛋白的配体的体外方法,所述方法包括以下步骤:(i)提供疑似能够标记聚集的PHF tau蛋白的第一药剂,(ii) a)包含与固相结合的tau核心片段的tau蛋白或其衍生物,以暴露高亲和力tau捕获位点,(b)能够结合固相tau的液相tau蛋白或其衍生物 蛋白质或衍生物,和(c)所述选择的第一试剂和(d)已知为tau-tau结合抑制剂的第二药剂,(iii)选择完全或部分缓解液相tau蛋白结合抑制的第一药剂,或 (b)衍生物与固相tau蛋白或(a)的抑制剂(d)的衍生物。 也可以测试配体以确认它们本身不是抑制剂。
    • 10. 发明申请
    • METHODS OF SYNTHESIS AND/OR PURIFICATION OF DIAMINOPHENOTHIAZINIUM COMPOUNDS
    • 二氨基苯甲酸酯化合物的合成和/或纯化方法
    • US20090259040A1
    • 2009-10-15
    • US12373216
    • 2007-07-10
    • Claude Michel WischikJohn Mervyn David StoreyColin MarshallJames Peter SinclairThomas Craven Baddeley
    • Claude Michel WischikJohn Mervyn David StoreyColin MarshallJames Peter SinclairThomas Craven Baddeley
    • C07D279/18
    • A61K31/5415C07D279/18C07D279/20
    • 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).
    • 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/或纯化某些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,包括甲基硫堇 (MTC)(也称为亚甲蓝)。 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,以及医学治疗,预防和诊断等方法 ,tau病 tau蛋白聚集的疾病; 阿尔茨海默病(AD); 皮克病 进行性核核麻痹(PSP) 颞痴呆(FTD); 与17号染色​​体相关的帕金森综合征(FTDP-17); 去抑痴呆 - 帕金森综合征 - 肌萎缩综合征(DDPAC); 苍白球 - 黑质变性(PPND); 关岛ALS综合征 苍白球黑素瘤变性(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; 原生动物感染; 寄生虫感染; 疟疾; 内脏利什曼病 非洲昏睡病 弓形体病 贾第虫病 恰加斯病 丙型肝炎病毒(HCV)感染; 人类免疫缺陷病毒(HIV)感染; 西尼罗病毒(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); 药物引起的帕金森综合征 和纯自主神经衰竭(PAF)。