NOVEL MONOMERS AND OLIGOMERS OF PEPTIDE NUCLEIC ACIDS Russian patent published in 2019 - IPC C07K14/00 C07D239/02 C07D239/42 C07D239/46 C07D473/18 C07D473/34 C12N15/113 A61K38/04 

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of general formula (I):

in which K is an active ester group of a carboxylic acid or -O-R_M; where R_M denotes an H atom, a methyl, ethyl, benzyl or tert-butyl group; Pr is an H atom or an amino-protecting group; # denotes asymmetric atom C; E is an adenine, cytosynyl, pseudo-isocytosynyl, guaninyl, thymine, uracilyl or phenyl group, optionally substituted with a protective group for the nucleotide base; R¹ denotes a group of general formula (II):

in which R² denotes a phosphonic ester group or a phosphonic acid group; R³ denotes an amino-protecting group; m is 1, 2, 3 or 4; and h denotes 0, 1, 2 or 3; provided that the sum of m and h in general formula (II) is within: 2≤x≤5. Also disclosed are a compound of formula (VI), such as specified in the patent claim, and a pharmaceutical composition.

EFFECT: disclosed compounds of formula (I) are novel monomers for producing oligomers of peptide nucleic acids of formula (VI), which can be used as a diagnostic agent or in antisense therapy.

10 cl, 7 dwg, 8 tbl, 24 ex