NOVEL PRODRUGS OF NUCLEIC ACIDS AND THEIR APPLICATION METHODS Russian patent published in 2017 - IPC A61K31/7076 C07H19/06 C07H19/16 A61K31/7088 A61P35/00 

FIELD: medicine.

SUBSTANCE: invention relates to applicable in medicine oligonucleotides of formula 1:

,

where R¹ is -OH or -SH; R² represents H, -OH or -OR^b, where R^b is locking group, which temporarily masks reactivity of functional group and can be removed; Ba is adenine, cytosine, 5-methylcytosine, guanine, thymine or uracil; fragment X is selected from -OCH₂CH₂S-S(O)₂R₁₀, -OCH₂CH₂S-SCH₂CH₂OH, -OCH₂CH₂CO₂H, , , , , , , , , ,, , , , , и ,

R₁₀ is C_1-4 alkyl; R₁₁ is C_1-10 alkyl or C_3-10 cycloalkyl; R₁₂ is H or C_1-10 alkyl; R³ is H; n equals integer number from 10 to 200; and X-phosphonate fragment in each case independently is formed with more than 98 % of diastereomeric purity according to ³¹P NMR spectroscopy or reverse-phase HPLC.

EFFECT: novel oligonucleotide is proposed promising for treating cancer.

7 cl, 4 dwg, 2 tbl, 395 ex