DERIVATIVES OF PYRIDAZIN-3(2H)-ON AND THEIR APPLICATION AS INHIBITORS OF FDE4 Russian patent published in 2009 - IPC C07D237/24 C07D401/12 C07D401/14 C07D409/12 C07D409/14 A61K31/501 A61P39/00 

FIELD: medicine.

SUBSTANCE: invention is related to compound of formula (I) , where

R¹ -C₁-₈alkyl; R² - pyridynyl, unnecessarily substituted with C₁-₈alkyl, quinolyl or isoquinolyl; R³ - hydrogen or C₁-₈alkylcarbonyl; R⁴ means group of formula G-L1-(CRR')n-, in which n is integer number from 0 to 3; R and R' are independently selected from group that includes atoms of hydrogen and lower alkyl groups; L1 means connection group, selected from group, which includes direct connection, groups -O-, -CO-, -NR"-, -O(CO)O-, -O-(CO)-, -(CO)O- and -NR"-(CO)-, where R" is lower alkyl; G is selected from group, including atoms of hydrogen, C₁-₈alkyl, C₂-₈alkenyl, C₃-₇dicloalkyl, phenylC₁-₈alkyl, pyridinyl, thiophenyl or residue of indan, and also phenyl, unnecessarily substituted with atom of halogen, C₁-₈alkoxy, cyano- or C₁-₈alkyl, which, in its turn, unnecessarily contains one or more atoms of halogen. Specified compounds are active and selective inhibitors of phosphodiesterase 4 (FDE4), therefore, they are applicable for treatment, prevention or suppression of pathological conditions, diseases or disorders, for which it is known that their behavior is relieved by inhibition of FDE4, such as asthma, chronic obstructive lung disease, rheumatoid arthritis, atopic dermatitis, psoriasis or syndrome of sore large gut. Invention is related also to pharmaceutical compositions on the basis of mentioned compounds, application of compounds, method for treatment of subject, when efficient amount of specified compounds is introduced to them. Besides invention is related to combined product for treatment or prevention of pathological condition or disease, behavior of which is relieved by inhibition of phosphodiesterase 4, including specified compound and another compound, selected from the group that includes (a) steroids, (b) immunosuppressive agents, (c) blockers of T-cells receptors, (d) anti-inflammatory medicinal agents, (e) β2-adrenergic agonists and (f) antagonists of muscarine receptors M3, for single-time, separate or serial use.

EFFECT: improved efficiency of compounds use.

11 cl, 2 tbl, 77 ex