Production and use of dimers of hematoporophyrin, purpurins, chl

Details Production and use of dimers of hematoporophyrin, purpurins, chl Production and use of dimers of hematoporophyrin, purpurins, chl

1986-06-24

1989-10-31

Warden, Robert J.

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

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

530389, 534 15, 534 16, 514185, 514410, 436548, 935107, 935108, 935110, A61K 3140

Patent

active

048778729

ABSTRACT:
Dimers which are either esters or amides of (1) a purpurin, a chlorin or a metal complex and (2) hematoporphyrin or a purpurin, a chlorin or a metal complex are disclosed. The purpines and their metal complexes have the structures of FIGS. 1, 7, 14-18, 29-38, 44-48 and 54-58 of the attached drawings. The chlorins and their metal complexes have the formulas of FIGS. 2, 8, 19-28, 39-43 or 49-53 of the attached drawings. Solutions of the purpurins, chlorins and metal complexes which are physiologically acceptable for intravenous administration are also disclosed, as are emulsions or suspensions of the solutions. 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 dimers to the patient. For detection, the patient is then illuminated with ultra violet light; for treatment, the patient is illuminated with visible light of a wavelength at which the purpurin, chlorin or complex administered shows an absorption peak or with X rays or other ionizing radiation.
Dimers of purpurins, chlorine and metal complexes which can be detected by nuclear magnetic resonance or by an instrument that detects ionizing radiation are also disclosed. The purpurins, chlorins and coplexers of these dimers have the formula of one of FIGS. 1, 2, 7, 8, or 14-58 and a structure which is enriched in an atom that can be detected by nuclear magnetic resonance, e.g., C-13 or N-15, or by an instrument that detects ionizing radiation, e.g., C-14, I-131 or Tc-99m.

REFERENCES:
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patent: 4649151 (1987-03-01), Dougherty
patent: 4656186 (1987-04-01), Bommer
patent: 4675338 (1987-06-01), Bommer
Kessel--I Cancer Research 46, 2248-2251, (1986).
Kessel--II, Chemical Abstracts 106:46579f, (1987).
Angew. Chem. Internat.Edit./vol. 14, No. 5, pp. 361 et seq., 1975, Journal of the Chemical Society, Perkin Transactions I, pp. 1660, et seq., 1979.

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