23-IN-VITAMIN D DERIVATIVE Russian patent published in 2015 - IPC C07C401/00 A61K31/593 A61P19/10 C07F7/18 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to novel derivative of vitamin D₃, suitable as therapeutic means against osteoporosis, presented by formula (1) (2), where R₁ represents hydrogen atom, alkyl group with 1-6 carbon atoms, alkylcarbonyloxyalkyl group, and each alkyl has 1-6 carbon atoms, or arylcarbonyloxyalkyl group, and aryl has 6-10 carbon atoms and alkyl has 1-6 carbon atoms or together with other R₂ and carbon atom, which they are bound to, can form cyclic alkyl group with 3-6 carbon atoms; R₃ represents alkyl group with 1-6 carbon atoms or together with other R₃ and carbon atom, which they are bound to, can form cyclic alkyl group with 3-6 carbon atoms; X represents oxygen atom or methylene group; and n is equal to integer number 1 or 2.

EFFECT: invention relates to pharmaceutical composition, possessing affinity to vitamin D receptor (VDR), which contains compound of formula (1); as well as relates to intermediate compound, represented by formula (2), in which R₂, X and n are such, as given above, R₄ represents R₁ in formula (1), methoxymethyl group, methoxyethoxymethyl group, tetrahydrofuranyl group, tetrahydropyranyl group or benzyloxymethyl group; and R₅ represents protective group for hydroxyl group, selected from the group, which includes methoxymethyl group, acyl group with 1-3 carbon atoms (mentioned number of carbon atoms includes carbonyl carbon), trimethylsilyl group, triethylsilyl group, tret-butyldimethylsilyl group and tret-butyldiphenylsilyl group.

12 cl, 4 tbl, 14 ex