KR920701184A - 1,4,10,13-ketraoxa-7,16-diazacyclooctadecane derivatives, pharmaceutical compositions containing the derivatives and methods of using the same - Google Patents

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1,4,10,13-ketraoxa-7,16-diazacyclooctadecane derivatives, pharmaceutical compositions containing the derivatives and methods of using the same

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1 is a graph showing the change in the radioactivity of the biological tissues of the control and test animals after the administration of the radioactive isotope (Sr-85), Figure 2 is a radiographic strontium administered to the lungs of Wistar rats, A graph showing changes in the radioactivity of biological tissues in the control and test animals of the active compound of Example 6b), and FIG. 3 shows the control animals after administration of the radioisotope (Ce-144) to the lungs of female Wistar rats. It is a graph showing the change in the radioactive concentration of living tissue for the test animals.

Claims (10)

Compound of general formula (I). Provided that Q ¹ and Q ² are hydrogen or a group of formula (III) when at least one of them is not hydrogen, Wherein R in Formula (III) is hydrogen, linear or branched C _1-5 alkyl group, linear or branched C _2-5 alkenyl group, phenyl or phenyl-C _1-5 alkyl group, respectively The latter two have an aromatic moiety of 1 or 2 or more halogen, C _1-5 alkyl, C _1-5 alkoxy, cyano or nitro group; Me is an alkali metal, alkaline earth metal, or transition metal ion; q is 0 or 1; M and N are each independently hydrogen, alkali metal, alkaline earth metal, or substituted ammonium ions; m, n and p are the valences of N, M and Me, respectively; s and r are i) r, s and q may not be 0 at the same time, ii) when the number of hydrogens in M or N is 0,1 or 2, and M and N are each 0, 1, 2, 3 or 4 under the condition that they are other than sodium or lithium ion. The compound of formula (I) according to claim 1, wherein Q ¹ and Q ² are the same as each other and R is hydrogen. N-N′-bis (dicarboxymethyl) -1,4,10,13-tetraoxa-7,16-diazacyclooctadecane calcium complex disodium salt. A pharmaceutical composition containing an effective amount of at least one compound of general formula (I), which is suitable for the removal of metal ions, in particular radioisotopes, which are harmful to biological tissues. Wherein Q ¹ and Q ² mean hydrogen or a group of the general formula (III), However, in the general formula (III), R is hydrogen, linear or branched C _1-5 alkyl group, linear or branched C _2-5 alkenyl group, phenyl or phenyl-C _2-5 alkyl group Wherein the latter two have at least one of their aromatic moieties being at least one halogen, C _1-5 alkyl, C _1-5 alkoxy, cyano or nitro group, provided that at least one of Q ¹ and Q ² is Me is an alkali metal, alkaline earth metal, or transition metal ion; q is 0 or 1; M and N are each independently hydrogen, alkali metal, alkaline earth metal, or substituted ammonium ions; m, n and p are the valences of N, M and Me, respectively; s and r are not equal to i) r, s and q may be zero at the same time; Ii) The number of hydrogens of M or N is 0, 1, 2, 3 or 4 under the condition that 0, 1 or 2, respectively. The method of claim 4, wherein the pharmaceutical composition is in the form of a tablet, dragee, capsule, suppository, injectable solution, powder or liquid aerosol, or skin plaster. The pharmaceutical composition according to claim 4 or 5, wherein the pharmaceutical composition contains a compound of formula (I), wherein Q ¹ and Q ² are the same and R is hydrogen. Composition. 6. The pharmaceutical composition of claim 4 or 5, wherein the pharmaceutical composition comprises N, N'-bis (dicarboxymethyl) -1,4,10,13-tetraoxa-7,16-diazacyclooctadecane calcium complex disodium A composition comprising a salt as an active ingredient. Using a compound of formula (I) for the removal of metal ions, in particular radioactive isotopes, which are harmful to biological tissues; Provided that Q ¹ and Q ² are hydrogen or a group of formula (III) when at least one of them is not hydrogen, In the above general formula (III), R is hydrogen, linear or branched C _1-5 alkyl group, linear or branched C _2-5 alkenyl group, phenyl or phenyl-C _2-5 alkyl group The latter two have at least 1 or 2 halogen, C _1-5 alkyl, C _1-5 alkoxy, cyano or nitro group, and Me is an alkali metal, alkaline earth metal, or transition metal ion; q is 0 or 1; M and N are each independently hydrogen, alkali metal, alkaline earth metal, or substituted ammonium ions; m, n and p are the valences of N, M and Me, respectively; s and r are not equal to i) r, s and q may be zero at the same time; Ii) The number of hydrogens of M or N is 0, 1, 2, 3 or 4 under the condition that 0, 1 or 2, respectively. A method of using a compound of formula (I) wherein Q ¹ and Q ² are the same and R is hydrogen for the removal of metal ions, particularly radioactive isotopes, which are harmful to biological tissues. N, N′-bis (dicarboxymethyl) -1,4,10,13-tetraoxa-7,16-diazacyclooctadecane calcium complex disodium salts are detrimental to metal tissues, particularly radioactive isotopes How to use for removal. ※ Note: This is to be disclosed by the original application.