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    • 5. 发明申请
    • Biologically active methylene blue derivatives
    • 生物活性亚甲蓝衍生物
    • US20080261960A1
    • 2008-10-23
    • US12078805
    • 2008-04-04
    • Stanley Beames BrownCassandra Claire O'GradyJohn GriffithsKirste Joanne MellishRichard George TunstallDavid John Howard RobertsDavid Ian Vernon
    • Stanley Beames BrownCassandra Claire O'GradyJohn GriffithsKirste Joanne MellishRichard George TunstallDavid John Howard RobertsDavid Ian Vernon
    • A61K31/5415A61P31/04A61P31/10A01P1/00A01P3/00A01N43/84
    • A61K49/003A61K8/4986A61K41/0057A61L2/0029A61L2/0082A61L2/08A61L2/232A61Q11/00C07D279/18
    • The present invention relates to a phenothiazinium compound of Formula (I): wherein: A and B each independently is in which R′ and R″ each independently is a linear, branched or cyclic hydrocarbon group, or R′ and R″ together with the N atom to which they are attached form an optionally substituted 5-, 6- or 7-membered ring; and where XP− is a counteranion and P is 1, 2 or 3; except for the compounds in which A and B are both either —N(CH3)2 or —N(CH2CH3)2 for use in a treatment that requires removal, deactivation or killing of unwanted tissues or cells. The invention also relates to compositions comprising the compounds of Formula I, to selected compounds of Formula I, use of the compounds of Formula I as medicaments and as a PDT agent or a photodiagnostic agent, a conjugate or composite formed between a compound of Formula I and a polymer; and to a method for sterilising fluids in which the fluid is passed over the conjugate or composite whilst it is illuminated.The compounds are biologically active photosensitisers which are strongly photocytotoxic and have application in the areas of photodynamic therapy (PDT), as well as for the diagnosis and detection of medical conditions and related uses in photochemical internalisation, in the production of cancer vaccines, in the treatment and prevention of microbial infections and in photodisinfection or photosterilisation.
    • 本发明涉及式(I)的吩噻嗪鎓化合物:其中:A和B各自独立地是其中R'和R“各自独立地是直链,支链或环状烃基,或者R'和R”在一起 与它们所连接的N原子形成任选取代的5-,6-或7-元环; 并且其中X-P-P为抗衡阴离子,P为1,2或3; 除了其中A和B均为-N(CH 3)2 - 或-N(CH 2 CH 2) 3 ,用于需要去除,失活或杀死不想要的组织或细胞的治疗。 本发明还涉及包含式I化合物的组合物,所选择的式I化合物,式I化合物用作药物和作为PDT剂或光诊断剂,在式I化合物之间形成的缀合物或复合物 和聚合物; 以及用于对液体进行灭菌的方法,其中流体在其被照射时通过共轭物或复合物。 这些化合物是具有强烈光细胞毒性并且在光动力疗法(PDT)领域中的应用的生物活性光敏剂,以及用于诊断和检测光化学内化中的医学病症和相关用途,在癌症疫苗的生产中 治疗和预防微生物感染和光消毒或光化学。