申请人:Brown Stanley Beames
公开号:US20080261960A1
公开(公告)日:2008-10-23
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 X
P−
is a counteranion and P is 1, 2 or 3;
except for the compounds in which A and B are both either —N(CH
3
)
2
or —N(CH
2
CH
3
)
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)的苯并噻吩化合物:其中:A和B各自独立地为-CH2-或-NR'-,其中R'和R''各自独立地为线性、支链或环烃基,或R'和R''与它们所连接的N原子一起形成一个可选的取代的5、6或7元环;XP-为一种计数阴离子,P为1、2或3;除了A和B都是-N(CH3)2或-N(CH2CH3)2的化合物用于需要去除、失活或杀死不需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,选择的式(I)化合物,使用式(I)化合物作为药物和作为光动力治疗剂或光诊断剂,以及在化合物(I)和聚合物之间形成的共轭物或复合物;以及在照明时将流体通过共轭物或复合物以灭菌的方法。这些化合物是具有生物活性的光敏剂,具有强烈的光细胞毒性,在光动力疗法(PDT)领域以及用于医学状况的诊断和检测以及与内部光化学作用有关的用途中,如癌症疫苗的生产、微生物感染的治疗和预防以及光消毒或光灭菌等方面有应用。