PHOSPHONATE DERIVATIVES Russian patent published in 2005 - IPC

FIELD: organophosphorus compounds, medicine.

SUBSTANCE: invention relates to new biologically active phosphonate compounds. Invention describes phosphonate compound of the formula:

wherein R₁ and R'₁ represent independently hydrogen atom (-H) substituted possibly with -O-(C₁-C₂₄)-alkyl, -O-(C₁-C₂₄)-alkenyl, -O-(C₁-C₂₄)-acyl, -S-(C₁-C₂₄)-alkyl, -S-(C₁-C₂₄)-alkenyl or -S-(C₁-C₂₄)-acyl wherein at least one among R and R'₁ doesn't represent -H and wherein indicated alkenyl or acyl comprise from 1 to 6 double bonds; R₂ and R'₂ represent independently -H substituted possibly with -O-(C₁-C₇)-alkyl, -O-(C₁-C₇)-alkenyl, -S-(C₁-C₇)-alkyl, -S-(C₁-C₇)-alkenyl, -O-(C₁-C₇)-acyl, -S-(C₁-C₇)-acyl, -N-(C₁-C₇)-acyl, -NH-(C₁-C₇)-alkyl, -N-((C₁-C₇)alkyl)₂, oxo-group, halogen atom, -NH₂, -OH or -SH; R₃ represents phosphonate derivative of nucleoside or biphosphonate; X represents compound of the formula:

L represents a valence bond or a bifunctional binding molecule of the formula: -J-(CR₂)_t-G- wherein t is a whole number from 1 to 24; J and G represent independently -O-, -S-, -C(O)O- or -NH-; R represents -H, unsubstituted or substituted alkyl or alkenyl; m means a whole number from 0 to 6; n = 0 or 1. Also, invention describes pharmaceutical compositions comprising phosphonate compounds, method for treatment of osteoporosis in mammal, method for increasing mineral osseous density, method for prophylaxis of apoptosis of osteoblasts and osteocytes in mammal, method for treatment of viral infection in mammal, method for treatment of growing neoplasm in mammal and method for proliferation of cells. Invention provides preparing new compounds eliciting useful biological properties.

EFFECT: valuable medicinal properties of phosphonate compounds.

17 cl, 2 dwg, 7 tbl, 21 ex