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1. 发明授权

US07737138B2 Methods of treatment of a tauopathy condition comprising the use of thioninium compounds 有权
标题翻译：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
申请人： Claude M. Wischik , Janet E. Rickard , Charles R. Harrington , David Horsley , John M. D. Storey , Colin Marshall , James P. Sinclair , Han Wan Tan
发明人： Claude M. Wischik , Janet E. Rickard , Charles R. Harrington , David Horsley , John M. D. Storey , Colin Marshall , James P. Sinclair , Han Wan Tan
IPC分类号： A61K31/5415
CPC分类号： C09B19/02 , C07D279/18
摘要： 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.
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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