SUBSTITUTED [1,3]OXAZOLO[4,5-d]PYRIDAZINES AND COMBINATORY LIBRARY Russian patent published in 2004 - IPC

FIELD: organic chemistry. SUBSTANCE: invention relates to novel physiologically active substituted oxazolo[4,5-d]pyridazines of the general formula (1) , (2) or (3) and to combinatory library designated for the search physiologically active substances among them, compounds-leaders and candidates (drug-candidates) based on screening results. In testing these compounds showed ability to inhibit activity of protein kinase. In these compounds R¹ and R² each means independently of one another hydrogen atom, inert substituent taken among the group including optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted alkoxy-group, optionally substituted alkoxyalkyl, optionally substituted aralkyl, optionally substituted heterocyclylalkyl, optionally substituted alkaryl, optionally substituted cycloalkyl, optionally substituted cycloalkenyl, optionally substituted aryl, optionally substituted alkylsulfinyl, optionally substituted alkylsulfonyl, -(CH₂)_m-O-(C₁-C₇-alkyl), -(CH₂)_m-N-(C₁-C₇-alkyl)_n wherein n and m have values from 1 to 7,optionally substituted aryloxyalkyl, optionally substituted heterocyclyl; R³ and R⁴ each represents independently of one another: hydrogen atom, -CN, -Cl, -Br, -J, carboxyl group; optionally substituted carboxy-(C₁-C₆)-alkyl group; optionally substituted carbamoyl group; optionally substituted hydroxyl group; optionally hydroxy-(C₁-C₅)-alkyl; optionally substituted amino-(C₁-C₇)-alkyl; optionally substituted amino-group, azaheterocycle-N-yl or substituted azaheterocycle-N-yl, inert substituent taken among the group including optionally substituted alkyl optionally substituted alkenyl; optionally substituted alkynyl; optionally substituted alkoxy-group; optionally substituted alkoxyalkyl; optionally substituted aralkyl; optionally substituted heterocyclylalkyl; optionally substituted alkaryl; optionally substituted cycloalkyl; optionally substituted cycloalkenyl; optionally substituted aryl; optionally substituted alkylsulfinyl; optionally substituted alkylsulfonyl, -(CH₂)_m-O-(C₁-C₇-alkyl), -(CH₂)_m-N-(C₁-C₇-alkyl)_n wherein n and m have values from 1 to 7; optionally substituted aryloxyalkyl; optionally substituted heterocyclyl. EFFECT: new compounds indicated above. 8 cl, 1 dwg, 1 tbl, 17 ex