1,4,10,13-tetraoxa-7,16-diazacyclooctadecane derivatives,...

C - Chemistry – Metallurgy – 07 – D

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C07D 273/08 (2006.01) A61K 31/395 (2006.01) C07D 273/00 (2006.01)

Patent

CA 2048627

1,4,10,13-TETRAOXA-7,16-DIAZACYCLOOCTADECANE DERIVATIVES PHARMA- CEUTICAL COMPOSITIONS CONTAINING THEM AND THEIR USE FOR THE DECORPORATION OF METAL IONS, MAINLY RADIOACTIVE ISOTOPES DAMAGING THE LIVING ORGANISM Abstract The invention relates to partially novel metal complexes, salts and double salts of 1,4,10,13-tetraoxa-7,16-diazacycloocta- decane compounds of the formula (I), Image (I) wherein Q1 and Q2 mean hydrogen or a group of the formula (III), Image (III) in the groups of the formula (III) the R subtituents independently represent hydroyen, a C1_5 straight or branched chain alkyl group, a C2-5 straight or branched chain alkenyl group, phenyl or phenyl-C1-5alkyl group, the two latter ones optionally being substituted on their aro- matic part by one or more halogen(s), C1-5alkyl, C1-5alk- oxy, cyano or nitro group(s), with the proviso that at least one of Q1 and Q2 is other than hydrogen; Me stands for an alkaline metal or alkaline earth metal or transition metal ion; q is 0 or 1; - 2 - M and N, independently from each other, stand for hydrogen or an alkaline metal, alkaline earth metal or optionally substi- tuted ammonium ion; m, n and p are integers each being equal to the charge of M, N or Me, respectively; s and r are, independently from each other, O, 1, 2, 3 or with the proviso that (i) r, s and q cannot simultaneously be 0; and (ii) the number of hydrogens in the meaning of M or N may be 0, 1 or 2, as well as pharmaceutical compositions containing these com- pounds. The compounds and compositions according to the invention can be used for the decorporation of metal ions, mainly radio- active isotopes such as radioactive strontium or cerium being harmful to the living organism. The active agents according to the invention exert their effects either in intravenous or local, transdermal or rectal route of administration.

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