Production and use of porphyrin derivatives and of compositions

Details Production and use of porphyrin derivatives and of compositions Production and use of porphyrin derivatives and of compositions

1992-01-08

1993-10-05

Raymond, Richard L.

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

534 11, 534 12, 534 13, 534 15, 534 16, C07F 108, C07F 306, C07F 1500, C07F 1502

Patent

active

052506681

ABSTRACT:
A family of benzochlorins, a family of verdins, a family of porphyrin derivatives and metal complexes thereof are disclosed. The benzochlorins have the formula of FIG. 3 of the attached drawings; their metal complexes have the formula of FIG. 1 . The verdins have the formulas of FIGS. 4 and 6 of the attached drawings; their metal complexes have the formulas of FIGS. 2 and 5. The porphyrin derivatives have the formula of FIG. 9 of the attached drawings; their metal complexes have the formula of FIG. 10 . Solutions of the benzochlorins, verdins, porphyrin derivatives and metal complexes which are physiologically acceptable for intravenous administration are also disclosed, as are emulsions or suspensions of the solutions, and compositions which additionally include cyclodextrin, and wherein the molecules of the benzochlorin, verdin, porphyrin derivative or metal complex are encapsulated within the molecules of the cyclodextrin. The solvent for the solutions can be a product of the reaction of ethylene oxide with castor oil. A method for detecting and treating tumors in human and animal patients is also disclosed. The method comprises administering one of the benzochlorins, verdins, porphyrin derivatives or metal complexes to the patient. For detection, the tumor area is then illuminated with ultra violet light; for treatment, the tumor area is illuminated with visible light of a wavelength at which the benzochlorin, verdin, porphyrin derivative or complex administered shows an absorption peak.

REFERENCES:
Porphyrin Photosensitization, edited by David Kassel and Thomas J. Dougherty, 1983, pp. 3-13.
J.C. S. Perkins I, Arnold et al, 1979, pp. 1660.varies.1670.
The Porphyrin, vol. II, edited by David Dolphin, 1978, pp. 137 & 138.
Woodward et al, JACS, vol. 82 (1960) pp. 3800-3802.
Hoffman, J. Org. Chem., vol. 30, No. 10 (1965) pp. 3512-3516.
Morgan et al, J. Org. Chem., vol. 51, No. 8 (1986) pp. 1347-1350.

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