COMPLEX SALTS OF HAEMATOPORPHYRIN AND ITS DERIVATIVES, SYNTHESES THEREOF AND THERAPEUTIC AGENT

摘要

New complex salts of hematoporphyrin and of its derivatives have general formula 1, in which R<1> and R<2> are identical or different and denote the -CH=CH<6>, -CH/OH/-CH<7> or CH/OR<3>/-CH<7> groups, where R<3> represents the group forming the oligomer containing ethereal and/or ester bindings, this group comprising from 1 to 5 identical or different units derived from monomer of formula 2 or R<1> and R<2> are identical and denote the CH/R4/-CH<7> group, where R4 represents the groups: carboxymethylamino, 1-carboxypenthylamino, 1-carboxy-2-methylpropylamino, 1-carboxy-3-methyl-butylamino, 1-carboxy-2-methyl-butylamino, 1-carboxybutylamino, 1-carboxypentylamino, 1-carboxy-2-hydroxyethylamino, 1-carboxy-2-hydroxy-propylamino, 1-carboxy-2-mercapto-ethylamino, 1-carboxy-3-methylthio-propylamino, 1,2-dicarboxy-ethylamino, 1-carboxy-2-carbamoyl-ethylamino, 1,3-dicarboxy-propylamino, 1-carboxy-3-carbamoyl-propylamino, 1-carboxy-2-phenyl-ethylamino, 1-carboxy-2-/4-hydroxyphenyl/-ethylamino, 1-carboxy-2-indolyl-ethylamino, 2-carboxy-pyrrolidinyl, 2-carboxy-4-hydroxy-pyrrolidinyl, 1-carboxy-5-amino-pentylamino, 1-carboxy-4-guanidyl-butylamino, 1-carboxy-4-hydroxy-5-amino-pentylamino or 1-carboxy-2-/1H-imidazole/-ethylamino group; A signifies a basic amino acid; m amounts to 2-6, n is 1-5 are disclosed. The method for preparation of new complex salts of formula 1 consists of reacting, with a basic amino acid, of hematoporphyrin derivatives of general formula 4, in which R<1> and R<2> have the above-stated meaning. The new complex salts are used as a therapeutic agent for detection and treatment of neoplasms.