Patent TW-477699-B (TW)
Title: Pharmaceutical agents that contain perfluoroalkyl-containing metal complexes and their use in tumor therapy and interventional radiology
Inventor: PLATZEK JOHANNES DR
IPC: A61K33/244
Filed: 1997-02-22
Granted: 2002-03-01
Abstract: Pharmaceutical compositions for use in tumor therapy and/or interventional radiology, comprising one or more perfluoroalkyl-containing compound of general formula I: RF-L-A, in which RF is a perfluorinated, straight-chain or branched carbon chain with formula -CnF2nX, in which X represents a terminal fluorine, chlorine, bromine, iodine or hydrogen atom, and n stands for numbers 4-30, L means a direct bond, a methylene group, an -NHCO group, a group formula, whereby p means numbers 0 to 10, q and u, independently of one another, mean numbers 0 or 1 and R1 is a hydrogen atom, a methyl group, a -CH2-OH group, a -CH2-CO2H group or a C2-C15 chain, which optionally is interrupted by 1 to 3 oxygen atoms, 1 to 2 > CO groups or an optionally substituted phenyl group and/or is substituted with 1 to 4 hydroxyl groups, 1 to 2 C1-C4 alkoxy groups, 1 to 2 carboxy groups, a group -SO3H, or L is a straight-chain, branched, saturated or unsaturated C2-C30 carbon chain, which optionally contains 1 to 10 oxygen atoms, 1 to 3 -NR1 groups, 1 to 2 sulfur atoms, a piperazine, a -CONR1 group, a -NR1CO-group, an -SO2 group, an -NR1-CO2 group, 1 to 2 -CO groups, a group --CO--N--T-N(R1)--SO2--RF or 1 to 2 optionally substituted phenyl and/or is interrupted by optionally substituted phenylene and/or is optionally substituted with 1 to 3 -OR1 groups, 1 to 2 oxo groups, 1 to 2 -NH- COR1 groups, 1 to 2 -CONHR1 groups, 1 to 2 -(CH2)p-CO2H groups, 1 to 2 groups of -(CH2)p-(O)q-CH2CH2-RF, whereby R1, RF and p and q have the above-indicated meanings, and T means a C2-C10 chain, which optionally is interrupted by 1 to 2 oxygen atoms or 1 to 2 -NHCO groups, A means a metal complex or its salts of organic and/or inorganic bases or amino acids or amino acid amides, for a complex of general formula II, in which R3, Z1 and Y are independent of one another, and R3 has the meaning of R1 or means -(CH2)m-L-RF, whereby m is 0, 1 or 2 and L and RF have the above-mentioned meaning, Z1 means a metal ion equivalent of atomic numbers 12, 20-30, 39, 42, 44 or 57-83, Y means -OZ1 or whereby Z1, L, RF and R3 have the above-mentioned meanings, or A stands for a complex of general formula III, in which R3 and Z1 have the above-mentioned meanings and R2 has the meaning of R1, A stands for a complex of general formula IV, in which Z1 has the above-mentioned meaning, or A stands for a complex of general formula V, in which Z1 has the above-mentioned meaning, and o and q stand for numbers 0 to 1 and the sum o+q=1 results, or A stands for a complex of general formula VI, in which Z1 has the above-mentioned meaning or A stands for a complex of general formula VII, in which Z1 and Y have the above-mentioned meanings or A stands for a complex of general formula VIII, in which R3 and Z1 have the above-mentioned meanings, and R2 has the above-mentioned meaning of R1, or A stands for a complex of general formula IX, in which R3 and Z1 have the above-mentioned meanings, or A stands for a complexing agent or complex of general formula X, in which R3 and Z1 have the above-mentioned meanings, or A stands for a complexing agent or complex of general formula XI, in which Z1, p and q have the above-mentioned meanings and R2 has the meaning of R1, or A stands for a complex of general formula XII, in which L, RF and Z1 have the above-mentioned meanings, or A stands for a complex of general formula XIII, in which Z1 has the above-mentioned meaning, optionally with the additives that are commonly used in galenicals for tumor therapy and/or interventional radiology.