FIELD: medicine, biotechnology.
SUBSTANCE: the invention relates to compounds of the formula (I) and their physiologically acceptable salts, where in the formula (I) R is-CH(R1)-COOH, where R1 and R5 are H; n is 1; Z is selected from-N(R2)(R3) and-NHR4; R2 is selected from a group consisting of a C5-C7 Cycloalkyl ring, a chain of the formula -(CH2)r-[(O-(CH2)r]m(CH2)sOH and C1-C7alkyl, optionally separated by one to three oxygen atoms and/or optionally replaced by one to three hydroxyl groups or a phenyl or cyclohexyl ring; R3 is selected from a group consisting of C5-C12hydroxyalkyl containing 3-6 hydroxyl groups; C2-C10hydroxyalkoxyalkylene of the formula - (CH2)r - [(O-(CH2)r]m (CH2)sOH; and the groups of the formula - (CH2)sCH(R5) - G; s is 0 or 1; r and m amount to 1 or 2 independently of each other; G is selected from -PO(OR6) 2 and -COOH; where R6 independently represents H or C1-C5 alkyl; or R2 and R3 together with the connecting nitrogen atom form a piperidine ring comprising 2 to 6 S substituents bound to one or more carbon atoms of the piperidine ring, each of which is independently selected from hydroxyl, C1-C3hydroxyalkyl and carboxyl; R4 is selected from a group consisting of C5-C12 hydroxyalkyl containing 3-6 hydroxyl groups; - (CH2)mPO(OR6) 2 and - (CH2)sCH(R8)G; R8 is phenyl-alkylene or cyclohexyl-alkylene having 1-3 carbon atoms in the alkylene chain. The invention also relates to a chelate complex of a compound of the formula (I) with the Gd3+ ion; a pharmaceutical composition containing a compound of the formula (I) or its chelate complex; compounds of the formula (I),
Formula (I)
,
where R is-CH(R1)-COOH, and each carboxyl group of these R groups is in a protected form as tert-butyl ester.
EFFECT: the technical result is the compounds of formula (I) for diagnostic imaging of organs or tissues of the human or animal body by using the MRI technique.
19 cl, 1 tbl, 21 ex
Authors
Dates
2021-02-15—Published
2016-12-12—Filed