Indium photosensitizers for PDT
AssigneeMiravant Pharmaceuticals, Inc.
InventorsByron C. Robinson, Avinash S. Phadke
Life of this patent
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Abstract
The invention disclosed herein involves a phototherapeutic pyrrolic core complexed with a non-radioactive Indium atom. Complexation of Indium by the pyrrolic core forms a metalopyrrolic compound which influences enables these compounds to localize at target sites a phototherapy. Such functionally aids in both detection and phototherapy of disease sites, or provides functionality that binds to site specific receptors of a target area such that the therapy is improved.
Claims87
A phototherapeutic compound composed of an atom of In113 or of In115 complexed with the inner nitrogens of a pyrrolic core or a phototherapeutic composition consisting essentially of a mixture of In113 and of In115 atoms complexed with the inner nitrogens of a pyrrolic core where, in both instances, the core is composed of at least two pyrroles whose pyrrole linking atoms may be carbon or nitrogen or combinations thereof, with the proviso that indium-monoacetylethylene glycol mono-10b-pheophorbate, indium-di-2,4-(1-ethanalcoholoxyethl)-deuteroporohyrinindium;
- indium deuteroporphyrin;
- indium hematoporphyrin;
- 2-[1-(diethylenetriamine-tetraacetic acidacetyloxyethane)oxyethyl]-4-[1-(2-hydroxyethyl)oxyethyl]In deuteroporphyrin;
- 2,4-Bis[1-(diethylenetriamine-tetraacetic acidacetyloxyethane)oxyethyl]In deuteroporphyrin;
- 2-[1-(In-diethylenetriamine-tetracaetic acidacetyloxyethane)oxyethyl]-4-[1-(2-hydroxyethyl)oxyethyl]In-deuteroporphyrin;
- 2,4-Bis[(1-(In-diethylenetriamine-tetracaetic-acetyloxyethane)oxyethyl]In-deuteroporphyrin;
- In-Hematoporphinyl diglycine;
- In-Hematoporphinyl diglutamic acid;
- In-Diacetylhematoporphinyl diglycine;
- In-Diacetylhematoporphinyl diglutamic acid;
- fully unsaturated porphyrins having the structure:
- where R1 is CH(OR)Me, R is alkyl, R2 is a residue derived by removing H from an amino acid or from diethylenetriaminepentaacetic acid, and M is In;
- and porphyrin derivatives having the structure
- where R1 is pyridyl, R2 is a substituted phenyl group and M is indium, are excluded.
A method which comprises administering intravenously, intramuscularly, subcutaneously intraperitineally or topically to a human or animal patient a given amount of a phototherapeutic compound composed of an atom of In113 or of In115 complexed with the inner nitrogens of a pyrrolic core or a given amount of a phototherapeutic composition consisting essentially of a mixture of In113 and of In115 atoms complexed with the inner nitrogens of a pyrrolic core where, in both instances, the core is composed of at least two pyrroles whose pyrrole linking atoms are carbon, nitrogen or carbon and nitrogen, and, after a period of time, (a) examining the patient under illumination which causes amounts of the phototherapeutic compound associated with the tissue to be detected to fluoresce, or (b) irradiating target tissue in the patient with light of a wavelength which causes the phototherapeutic compound or composition associated therewith to undergo a desired reaction, the given amount of the phototherapeutic compound being sufficient to enable fluorescence or the desired reaction, but less than the amount of a compound composed of an atom of Sn complexed with the inner nitrogens of the same pyrrolic core which would be required to enable fluorescence or the desired reaction.
A method for treating a human or animal patient, which method comprises administering to the patient, intravenously, intramuscularly, subcutaneously, intraperitineally or topically, an effective amount of a phototherapeutic compound composed of an atom of In133 or of In115 complexed with the inner nitrogens of a pyrrolic core or of a phototherapeutic composition consisting essentially of a mixture of In113 and of In115 atoms complexed with the inner nitrogens of a pyrrolic core where, in both instances, the core is composed of at least two pyrroles whose pyrrole linking atoms may be carbon or nitrogen or combinations thereof, and, after sufficient time, irradiating target tissue with light of a wavelength which causes a reaction which destroys the target tissue, with the proviso that the amount of the phototherapeutic compound or composition administered is less than the minimum amount of a phototherapeutic compound composed of an atom of Sn complexed with the inner nitrogens of the same pyrrolic core which would be required for irradiation, after sufficient time, of the target tissue with light of a suitable wavelength to cause a reaction which would destroy the target tissue.
A method for detecting tissue in a human or animal patient, which method comprises administering to the patient, intravenously, intramuscularly, intraperitineally, subsutaneously or topically, an effective amount of a phototherapeutic compound composed of an atom of In113 or of In115 complexed with the inner nitrogens of a pyrrolic core or of a phototherapeutic composition consisting essentially of a mixture of In113 and of In115 atoms complexed with the inner nitrogens of a pyrrolic core where, in both instances, the core is composed of at least two pyrroles whose pyrrole linking atoms may be carbon or nitrogen or combinations thereof, and, after sufficient time, examining the patient under illumination which causes residual amounts of the phototherapeutic compound or composition to fluoresce, with the proviso that the amount of the phototherapeutic compound or composition administered is less than the minimum amount of a phototherapeutic compound composed of an atom of Sn complexed with the inner nitrogens of the same pyrrolic core which would be required for the illumination to cause residual amounts of the phototherapeutic compound to fluoresce.
Dependencies are inferred from the claim text.