CYTIDINE DERIVATIVES AND METHODS OF PRODUCING CYTIDINE DERIVATIVES Russian patent published in 2024 - IPC C07H19/06 C07H19/73 A61K31/7068 A61P35/00 

FIELD: pharmaceutics.

SUBSTANCE: invention relates to a method of producing 4(N)-substituted derivatives of compounds of formula (IB), where the method involves reacting a compound of formula (IB) with a chloroformate of formula (II) to obtain a compound of formula (IIIB), where R₁ is selected from the structures specified in the claim; R_2B represents fragments specified in the claim; R_3B is hydrogen or halogen; and R_4B is hydrogen; where the chloroformate of formula (II) is presented in the method in amount of 0.3 to 0.7 equivalents (by moles). Invention also relates to a method of producing a compound of formula (III), where the method involves reacting gemcitabine (I) with a chloroformate of formula (II) to obtain a compound of formula (III), where R₁ is selected from the radicals indicated above. Invention also relates to a compound of formula (IV) and a method for production thereof, where n denotes 0.1 or 2, where the method involves obtaining compound (III) with a subsequent step of reacting compound (III) in N,N-diisopropylethylamine to form a compound of formula (IV). Invention also relates to a pharmaceutical composition based on a compound of formula (IV) and using a compound of formula (IV) or a pharmaceutical composition for treating malignant growths.

EFFECT: treatment of malignant neoplasms, which include breast cancer, ovarian cancer, non-small cell lung cancer, pancreatic cancer and bladder cancer.

13 cl, 7 tbl, 18 dwg