CONTRAST AGENTS Russian patent published in 2021 - IPC C07D257/02 C07D401/06 A61K49/10 C07F9/38 C07F9/40 

Abstract RU 2743167 C2

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

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RU 2 743 167 C2

Authors

Lattuada, Luciano

Napolitano, Roberta

Boi, Valeria

Visigalli, Massimo

Aime, Silvio

Giovenzana, Giovanni, Battista

Fringuello Mingo, Alberto

Dates

2021-02-15Published

2016-12-12Filed