Complex salts of hematoporphyrin and of its derivatives,...

C - Chemistry – Metallurgy – 07 – K

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C07K 5/10 (2006.01) A61K 31/40 (2006.01) A61K 38/04 (2006.01) A61K 41/00 (2006.01) A61K 49/00 (2006.01) C07D 487/22 (2006.01) C07D 519/00 (2006.01) C07K 5/06 (2006.01) C07K 5/08 (2006.01) C07K 7/06 (2006.01)

Patent

CA 2081605

New complex salts of hematoporphyrin and of its derivatives have general formula 1, in which R1 and R2 are identical or different and denote the -CH=CH2, -CH/OH/-CH3 or CH/OR3/-CH3 groups, where R3 represents the group forming the oligomer con- twining ethereal and/or ester bindings, this group comprising from 1 to 5 identical or different units derived from monomer of formula 2 or R1 and R2 are identical and denote the CH/R4/-CH3 group, where R4 represents the groups: carboxymethylamino, 1-carboxypenthylamino, 1-carboxy-2-methylpropylamino, 1-carboxy- -3-methyl-butylamino, 1-carboxy-2-methyl-butylamino, 1-carboxy- butylamino, 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-pyr- rolidinyl, 1-carboxy-5-amino-pentylamino, 1-carboxy-4-guanidyl- -butylamina, 1-carboxy-4-hydroxy-5-amino-pentylamino or 1-car- boxy-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 hematoporphy- rin derivatives of general formula 4, in which R1 and R2 have the above-stated meaning. The new complex salts are used as a therapeutic agent for detection and treatment of neoplasms,

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