Patent ID: 6136841
Filing Date: 2000-10-24
Classification: A61K,C07D

Abstract:
In a method of photodynamic therapy comprising administering to a patient a photodynamic agent, the improvement wherein said photodynamic agent is at least one porphyrin complex of formula I: ##STR4## wherein M stands for two hydrogen atoms or a diamagnetic metal ion,R.sup.1 stands for a hydrogen atom, a straight-chain C.sub.1 -C.sub.6 alkyl, a C.sub.7 -C.sub.12 aralkyl, or OR',R' is a hydrogen atom or C.sub.1 -C.sub.3 alkyl,R.sup.2 stands for --(C.dbd.Q)(NR.sup.4).sub.o --(A).sub.q --(NR.sup.5)--K, --CO--Z or --(NH).sub.o --(A).sub.q --NH--D,Z is --OL,L is an inorganic cation, an organic cation or a C.sub.1 -C.sub.4 alkyl,A means a phenylenoxy group, a C.sub.1 -C.sub.12 alkylene which is interrupted by one or more oxygen atoms, or a C.sub.7 -C.sub.12 aralkylene that is interrupted by one or more oxygen atoms,o and q, independently of one another, mean numbers 0 or 1,D means a hydrogen atom or --CO--A--(COOL).sub.o --(H).sub.m, with m equal to 0 or 1 and the sum of m and o is equal to 1,R.sup.3 stands for --(C.dbd.Q) (NR.sup.4).sub.o --(A).sub.q --(NR.sup.5)--K,Q stands for an oxygen atom or for two hydrogen atoms,R.sup.4 means a group --(A).sub.q --H,K means a complexing agent of general formula (IIa), (IIb), (IIc), (IId) or (IIe), whereby if K is a complexing agent of formula (IIa), R.sup.5 has the same meaning as R.sup.4, and if K is a complexing agent of formula (IIb), (lIc), (IId) or (IIe), R.sup.5 has the same meaning as D, provided that a direct oxygen-nitrogen bond is not allowed, ##STR5## A.sup.1 means a pbenylenoxy group, a C.sub.1 -C.sub.12 alkylene which is interrupted by one or more oxygen atoms, or a C.sub.7 -C.sub.12 aralkylene, which is interrupted by one or more oxygen atoms,R.sup.6 stands for a hydrogen atom, a straight-chain or branched C.sub.1 -C.sub.7 alkyl, a phenyl or benzyl group,A.sup.2 stands for a phenylene, a --CH.sub.2 --NHCO--CH.sub.2 --CH(CH.sub.2 COOH)--C.sub.6 H.sub.4 -.beta.-, a phenylenoxy group, or a C.sub.1 -C.sub.12 alkylene or C.sub.7 -C.sub.12 alkylene that is optionally interrupted by one or more oxygen atoms, 1 to 3 --NHCO, 1 to 3 --CONH and is optionally substituted by 1 to 3 --(CH.sub.2).sub.0-5 COOH, whereby .beta. stands for the binding site to X,X stands for a --CO-- or an NHCS group, andL.sup.1, L.sup.2, L.sup.3 and L.sup.4, independently of one another, stand for a hydrogen atom or a metal ion equivalent of an element of atomic numbers 20-32, 37-39, 42-51 or 57-83, provided that at least two of L.sup.1, L.sup.2, L.sup.3 and .sup.4 stand for said metal ion equivalents, and that other anions are present to compensate for optionally present charges in the metalloporphyrin, and free carboxylic acid groups that are not required for complexing are optionally present as salts with physiologically compatible inorganic cations, or organic cations, or as esters or amides.