SPIRO-6,7-DIHYDRO-5H-PYRAZOLO[1,2-a]PYRAZOLE-1-ONES THAT REGULATE INFLAMMATORY CYTOKINES, PHARMACEUTICAL COMPOSITION AND METHOD FOR INHIBITION Russian patent published in 2006 - IPC C07D491/20 C07D495/20 A61K31/4162 A61P29/00 

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to new compounds able to prevent the extracellular release of inflammatory cytokines. Proposed compounds including their diastereomeric forms and their pharmaceutically acceptable salts correspond to the formula: wherein R means: (a) -O[CH₂]_kR³ or (b) -NR^4aR^4b; R³ means a substituted or unsubstituted (C₁-C₄)-alkyl, a substituted or unsubstituted phenyl wherein substitutes are taken among halogen atom, cyano-group, trihalidemethyl, (C₁-C₄)-alkyl, (C₁-C₄)-alkylsulfonyl, -NR^4aR^4b, -O[CH₂]_kR³ wherein R³ means hydrogen atom each among R^4a and R^4b means independently hydrogen atom or (C₁-C₄)-alkyl-CO- or benzo(1,3)dioxol; index k has a value from 0 to 5; each among R^4a and R^4b means independently: (a) hydrogen atom or (b) -[C(R^5aR^5b)₂]_mR⁶ wherein each R^a means hydrogen atom, and R^5b means hydrogen atom, linear or branched (C₁-C)-alkyl; R⁶ means vinyl, the group -OR⁷, -CO₂R⁷, cyclic (C₃-C)-alkyl, unsubstituted phenyl or phenyl substituted with (C₁-C₄)-alkyl, (C₁-C₄)-alkylsulfonyl, -NR^4aR^4b, -O[CH₂]_kR³ wherein each among R³, R^4a and R^4b means independently hydrogen atom, or unsubstituted 6-membered nitrogen-containing heteroaryl; R⁷ means hydrogen atom, water-soluble cation or (C₁-C₄)-alkyl; index m has a value from 0 to 5. Also, invention relates to a pharmaceutical composition comprising the effective dose of compounds corresponding to abovementioned formula, and to a method for inhibition of extracellular release of inflammatory cytokines.

EFFECT: valuable medicinal properties of compounds and composition.

14 cl, 1 sch, 6 tbl, 3 ex