Biologically active methylene blue derivatives
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Abstract
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.
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Citations
75 Claims
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1-42. -42. (canceled)
- 43. A method of inducing a photocytoxic effect, comprising applying to an area to be treated an effective amount of a compound of formula
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44. A method of photodynamic therapy which comprises applying to an area to be treated an effective amount of a compound of formula
- 45. A method of treatment of microbial infections, the method comprising systemic administration or applying to an area to be treated, a therapeutically effective amount of a compound of formula
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46. A method of prevention of microbial infections, the method comprising systemic administration or applying to an area to be treated, a therapeutically effective amount of a compound of formula
- 47. A method of sterilising a surface or a fluid comprising contacting or applying a compound of formula
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48. A method of treatment or prevention of microbial infection at any stage in a wound, surgical incision or burn wound, comprising applying to an area to be treated a composition comprising a therapeutically effective amount of a compound of formula
- 49. A method of treatment of microbial infections, burn wounds and other lesions and of dental bacterial disease, the method comprising applying to the area to be treated a therapeutically effective amount of a compound of formula
- 50. A method of sterilising a surface or a fluid comprising applying a compound of formula
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51. A method of killing, or deactivating any Candida albicans, E. coli, P. aeruginosa, S. aureus or methicillin resistant S. aureus present on a surface or in a fluid comprising:
contacting or applying a compound of the formula
Specification