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    3, 7-DIAMINO-10H-PHENOTHIAZINE SALTS AND THEIR USE
    1.
    发明申请
    3, 7-DIAMINO-10H-PHENOTHIAZINE SALTS AND THEIR USE 审中-公开
    3，7-二氨基-10H-邻苯二甲酸盐及其用途

    公开(公告)号：US20160051559A1

    公开(公告)日：2016-02-25

    申请号：US14929111

    申请日：2015-10-30

    申请人： WisTa Laboratories Ltd.

    发明人： Claude Michel WISCHIK ,  Janet Elizabeth RICKARD ,  Charles Robert HARRINGTON ,  David HORSLEY ,  John Mervyn David STOREY ,  Colin MARSHALL ,  James Peter SINCLAIR ,  Thomas Craven BADDELEY

    IPC分类号： A61K31/5415

    CPC分类号： A61K31/5415 ,  C07D279/20 ,  C07D279/22 ,  C09B21/00 ,  Y02A50/393 ,  Y02A50/411

    摘要： Described are methods of preparing reduced 3,7-diamino-10H-phenothiazine (DAPTZ) compounds of formula: wherein: R1 and R9 are 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 methods are particularly useful for producing stable reduced forms, and with high purity. The stability and purity are especially relevant for pharmaceutical compositions for the treatment of disease. The compounds are useful for treatment of e.g. tauopathies, such as Alzheimer's disease, and also as prodrugs for the corresponding oxidized thioninium drugs.

    摘要翻译： 描述了制备下式的还原的3,7-二氨基-10H-吩噻嗪（DAPTZ）化合物的方法：其中：R 1和R 9独立地选自：-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。 这些方法对于生产稳定的还原形式和高纯度特别有用。 稳定性和纯度与治疗疾病的药物组合物特别相关。 该化合物可用于治疗例如 tau病，如阿尔茨海默病，以及相应的氧化型硫堇药物的前药。