KR920702235A - All-cis-1,3,5-triamino-2,4,6-cyclohexanetriol and its derivatives with radioactive metal ions for radiological diagnostic purposes and for tumor therapy, for radiological diagnostic purposes and for tumor therapy For the preparation of reagents - Google Patents

Abstract

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Description

All-cis-1,3,5-triamino-2,4,6-cyclohexanetriol and its derivatives with radioactive metal ions for radiological diagnostic purposes and for tumor therapy, for radiological diagnostic purposes and for tumor therapy For the preparation of reagents

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Claims (15)

As a ligand, all-cis-1,3,5-triamino-2,4,6-trihydroxycyclohexane of the formula (I) or a derivative thereof, and a salt or pharmacologically pharmacologically common inorganic or organic acid All-cis-1,3 of the following general formulas (III) and (IV) as complexes of the available anions and quaternary ammonium salts of the following general formulas (II), (IIa) or (IIb) and radioactive metal ions, or ligands; For the purpose of radiological diagnosis and tumor treatment of complexes of 5-triamino-2,4,6-trihydroxycyclohexane derivatives and radioactive metal ions and for the purpose of radiodiagnostic purposes and for the preparation of reagents for tumor treatment: Wherein R ₁ , R ₂ , R ₃ , R ₄ , R ₅ or R ₆ are the same or different and represent a hydrogen atom, an alkyl group or a -CO-alkyl group, and alkyl in the alkyl or -CO-alkyl group is 1-18 carbon atoms. And alkyl and —CO-alkyl groups each contain, independently of one another, one or more identical or different functional groups, Wherein R ₁ -R ₆ and R ₇ , R ₈ and R ₉ are each independently an unsubstituted or substituted alkyl group or a -CO-alkyl group as defined above. Substituents of the nitrogen atom in the above formula are independently of each other H or CH ₃ . Use according to claim 1, characterized in that it is a radioactive metal ion α, β or γ release agent. Use according to claim 1 or 2, characterized in that the radioactive metal ion is an ion of a radioisotope of iron, copper, gallium, yttrium, ruthenium, technetium, rhodium, indium, dysprosium, samarium, tulium, ytterbium or rhenium. 4. Use according to any one of claims 1 to 3, characterized in that the river complex is used for the diagnosis of radioactivity of the heart and for the preparation of reagents therefor. 5. Use according to claim 4, characterized in that a complex with a ligand of formula (II), (IIa), (IIb) or (IV) according to claim 1 is used. 6. Use according to claim 5, wherein in the general formulas (II), (IIa) and (IIb), the radicals R ₁ -R ₉ are each a methyl group and the nitrogen atom substituents of the general formula (IV) are methyl groups. 6. Use according to claim 5, wherein in formulas (II), (IIa) and (IIb) the radicals R ₁ -R ₆ are each methyl and the radicals R ₇ , R ₈ , and R ₉ are each H. The use according to any one of claims 1 to 4, characterized in that the alkyl group or -CO-alkyl group contains one or more functional groups capable of coordinating with metal ions. The ligand of formula (I) is used, wherein at least one of the radicals R ₁ , R ₃ , and R ₅ is the following general formula, wherein the radicals R ₂ , R ₄ , and R ₆ are hydrogen atoms; Or an alkyl group having 1-18 carbon atoms. -(CH ₂ ) _n -N (R) ₃ Wherein n = 1, 2 or 3, especially 2, and R is an alkyl group having 1,2,3 or 4 carbon atoms. The alkyl group according to any one of claims 1 to 4, wherein a ligand of the general formula (I), (II), (IIa) or (IIb) is used, wherein the radical R ₁ , R ₃ or R ₅ has a functional group and Use of the formula-(CH ₂ ) _n -COOH (n = 1, 2 or 3, especially 2), wherein the radicals R ₂ , R ₄ and R ₆ -R ₉ are each H. Use according to claim 10, characterized in that for the treatment of tumors or the manufacture of reagents for the treatment of tumors. An aqueous solution or suspension of a derivative of formula (I), (II), (IIa), (IIb), (III) or (IV) as defined in claim 1, 7, 8, 9 or 10 is a salt of radioactive metal. Method for producing a complex of radioactive metal ions for radiological diagnostic purposes and tumor treatment, characterized in that it is half with an aqueous solution or suspension of hydroxide or oxide. 13. A process according to claim 12, characterized in that a salt, hydroxide or oxide of a metal which is an α, β or γ release agent is used. 14. Salts, hydrides, metals according to claim 12 or 13, consisting of one or more radioactive isotopes of iron, copper, gallium, yttrium, ruthenium, technetium, rhodium, indium, dysprosium, samarium, tulium, ytterbium or rhenium Characterized by the use of oxy or oxides. The aqueous solution obtained according to any one of claims 12 to 14 for preparing a reagent suitable for radiodiagnostic purposes or for the treatment of tumors, wherein the aqueous solution is suitably combined with conventional pharmacological additives. Method characterized by mixing. ※ Note: The disclosure is based on the initial application.