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    3,7-diamino-10H-phenothiazine salts and their use
    6.
    发明授权
    3,7-diamino-10H-phenothiazine salts and their use 有权
    3,7-二氨基-10H-吩噻嗪盐及其用途

    公开(公告)号：US07888350B2

    公开(公告)日：2011-02-15

    申请号：US12294599

    申请日：2007-03-28

    Applicant: Claude Michel Wischik ,  Janet Elizabeth Rickard ,  Charles Robert Harrington ,  David Horsley ,  John Mervyn David Storey ,  Colin Marshall ,  James Peter Sinclair ,  Thomas Craven Baddeley

    Inventor： Claude Michel Wischik ,  Janet Elizabeth Rickard ,  Charles Robert Harrington ,  David Horsley ,  John Mervyn David Storey ,  Colin Marshall ,  James Peter Sinclair ,  Thomas Craven Baddeley

    IPC: C07D279/18 ,  A61K31/5415

    CPC classification number: A61K31/5415 ,  C07D279/20 ,  C07D279/22 ,  C09B21/00 ,  Y02A50/393 ,  Y02A50/411

    Abstract: 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 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; each of HX1 and HX2 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).

    Abstract translation: 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，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和R 9各自独立地选自 从：-H; C 1-4烷基; C2-4烯基; 和卤代C 1-4烷基; R3NA和R3NB中的每一个独立地选自：-H; C 1-4烷基; C2-4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; C2-4烯基; 和卤代C 1-4烷基; HX1和HX2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，例如用于治疗tau蛋白病如阿尔茨海默氏病，以及作为相应的氧化硫堇药物（例如氯化甲硫氨酸，MTC）的前药。

    SYSTEMS FOR CLINICAL TRIALS
    7.
    发明申请
    SYSTEMS FOR CLINICAL TRIALS 审中-公开
    临床试验系统

    公开(公告)号：US20100280975A1

    公开(公告)日：2010-11-04

    申请号：US12741342

    申请日：2008-11-05

    Applicant: Claude Michel Wischik ,  Damon Jude Wischik ,  Roger Todd Staff ,  Alison Dorothy Murray

    Inventor： Claude Michel Wischik ,  Damon Jude Wischik ,  Roger Todd Staff ,  Alison Dorothy Murray

    IPC: G06Q90/00 ,  A61B5/00

    CPC classification number: G06Q99/00 ,  G16H10/20 ,  G16H50/50

    Abstract: The invention provides methods and systems for assessing the efficacy of a pharmaceutical which is putatively disease modifying of a cognitive disorder, for use in the treatment or prophylaxis of that cognitive disorder, the method comprising the steps of: (1) stratifying a subject group into at least 2 sub-groups according to a baseline indicator of likely disease progression, (2) treating members of each subject group with the pharmaceutical for a treatment time frame, (3) deriving psychometric and optionally physiological outcome measures for each treated patient group, (4) comparing the outcomes at (3) with a comparator arm of said sub-groups which is optionally a placebo or minimal efficacy comparator arm, (5) using the comparison in (4) to derive an efficacy measure for the pharmaceutical. The methods and systems of the invention address problems such as low rate of decline over the treatment time-frame of patients who have mild-disease severity at baseline and biased withdrawal, particularly in the placebo/comparator treatment arm.

    Abstract translation: 本发明提供了用于评估药物的功效的方法和系统，所述药物是推定的认知障碍的疾病改变，用于治疗或预防该认知障碍，所述方法包括以下步骤：（1）将受试者组分成 根据可能的疾病进展的基线指标，至少2个亚组，（2）用药物处理每个受试者群体的治疗时间框架，（3）为每个治疗的患者组导出心理测量和任选的生理学结果测量， （4）比较（3）与所述亚组的比较组比较，其可选地是安慰剂或最小功效比较组，（5）使用（4）中的比较来得出药物的功效测定。 本发明的方法和系统解决了诸如在基线时具有轻度疾病严重程度和偏倚戒断的患者的治疗时间范围内的下降率降低的问题，特别是在安慰剂/比较治疗组中。

    Methods of treatment of a tauopathy condition comprising the use of thioninium compounds
    8.
    发明授权
    Methods of treatment of a tauopathy condition comprising the use of thioninium compounds 有权
    包括使用硫铊化合物的tau病变病况的治疗方法

    公开(公告)号：US07737138B2

    公开(公告)日：2010-06-15

    申请号：US11391675

    申请日：2006-03-29

    Applicant: Claude M. Wischik ,  Janet E. Rickard ,  Charles R. Harrington ,  David Horsley ,  John M. D. Storey ,  Colin Marshall ,  James P. Sinclair ,  Han Wan Tan

    Inventor： Claude M. Wischik ,  Janet E. Rickard ,  Charles R. Harrington ,  David Horsley ,  John M. D. Storey ,  Colin Marshall ,  James P. Sinclair ,  Han Wan Tan

    IPC: A61K31/5415

    CPC classification number: C09B19/02 ,  C07D279/18

    Abstract: This invention pertains generally to the field of chemical synthesis and purification, and more specifically to methods of synthesizing and purifying certain 3,7-diaminophenothiazin-5-ium compounds (referred to herein as “diaminophenothiazinium compounds”) including Methythioninium 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.

    Abstract translation: 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-肟化合物（本文中称为“二氨基吩噻嗪鎓化合物”）的方法，包括氯化铁偶氮（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。

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