FIELD: pharmaceutics.
SUBSTANCE: invention relates to a compound of formula I: in which X is O; Y is Q-R3, where Q is N, and R3 is selected from the group containing C1-6alkyl or a hydrogen atom; Z is Q-R3-(L-R4), where Q is N or CH, and R3 is C1-20hydroxyalkyl, C1-6alkyl or hydrogen atom, and L is an optional linker, selected from a group comprising C1-6alkylene, C1-6hydroxyalkylene and polyethylene glycol (PEG) linker, R4 is selected from a group comprising C1-6alkyl-R5, C3-6aryl-R5, hydroxy, -O-C1-3alkyl-R5, sulphonyl, 5–6-membered heterocyclic ring selected from an N-acetylneuraminic acid residue, dihydropyrimidine-2,4(1H,3H)-dione, tetrahydrothiophene-1,1-dioxide, imidazolidine-2,4-dione and morpholine, a carbohydrate group, selected from monosaccharide and disaccharide residues, chelate group
amino acid group, wherein R5 is one or more optional substitutes, selected from hydroxy, amino, oxo, sulphonamide or -C(=O)-NH-C1-6hydroxyalkyl; or Z itself forms part of a carbohydrate group selected from monosaccharide and disaccharide residues, or 5–6 membered heterocyclic ring selected from an N-acetylneuraminic acid residue, dihydropyrimidine-2,4(1H,3H)-dione, tetrahydrothiophene-1,1-dioxide, imidazolidine-2,4-dione and morpholine; R1 is C1-3alkyl; R2 is absent; and each n is integer from 1 to 6; wherein the compound of formula I contains at least two hydroxy groups. Also disclosed is a pharmaceutical composition, a method of forming MR images and/or MR spectra using a compound of formula I.
EFFECT: disclosed compounds of formula (I) are a polyase-macrocycle with side "arms" in the form of carboxylic acid residues, which provide formation of a complex with manganese as a core metal, and are suitable for use as contrast agents in magnetic resonance imaging (MRI).
18 cl, 26 ex
Title | Year | Author | Number |
---|---|---|---|
METAL COMPLEXES WITH BICYCLIC POLYAMINO ACIDS, METHOD FOR THEIR PREPARING AND THEIR APPLICATION IN MEDICINE FOR IMAGE PREPARING | 2000 |
|
RU2232763C2 |
TETRAHYDROTRIAZOLOPYRIMIDINE DERIVATIVES AS INHIBITORS OF HUMAN NEUTROPHIL ELASTASE | 2012 |
|
RU2622643C2 |
HETEROBICYCLIC COMPOUND, PHARMACEUTICAL COMPOSITION, METHODS OF SYNTHESIS OF HETEROBICYCLIC COMPOUND | 1993 |
|
RU2128656C1 |
IMPROVED CONJUGATES N4 OF CHELATING AGENTS | 2005 |
|
RU2360701C2 |
ALKYL SULPHONAMIDE QUINOLINES WITH AFFINITY TO NK-3 RECEPTORS | 2006 |
|
RU2421447C2 |
METHOD OF TREATING FLUORIDE | 2008 |
|
RU2475448C2 |
MACROCYCLIC COMPOUNDS AS TRK KINASE INHIBITORS | 2011 |
|
RU2735545C2 |
BENZIMIDAZOLE DERIVATIVES IN TREATING DISORDERS ASSOCIATED WITH VANILLOID RECEPTOR TRPV1 | 2007 |
|
RU2458055C2 |
MACROCYCLIC COMPOUNDS AS TRK KINASE INHIBITORS | 2011 |
|
RU2594742C2 |
1-[PYRIDO(3,4-B)-1,4-OXAZINYL-4-YL]-1H-INDOLES, METHOD OF THEIR SYNTHESIS, COMPOSITION ON THEIR BASIS AND DERIVATIVE OF N-(4-PYRIDINYL)-1H-INDOLE-1-AMINE | 1992 |
|
RU2042680C1 |
Authors
Dates
2022-04-05—Published
2017-12-21—Filed