| abstract |
FIELD: organic chemistry, biochemistry, pharmacy. SUBSTANCE: invention relates to l ortho-substituted compounds of the formula (I) or their pharmaceutically acceptable salts that are inhibitors of prostaglandin H-synthase. In compounds of the formula (I) J means CH or N, K and L mean CH; X means a simple bond, -C≡C-, -Z(CHR 5 ) p , where Z means O; R 1 means phenyl or 2-naphthyl substituted with O-2-substituents of R 7 , C 5 -C 7 -cycloalkyl or C 5 -C 7 -cycloalkenyl under condition that R 1 is bound with heteroatom directly where indicated heteroatom is not bound with carbon atom having a double bond in cycloalkene ring or 5-10-membered heterocyclic system taken among pyrrolyl, benzothienyl, 3-pyridyl optionally substituted with C 1 -C 4 -alkyl, quinolinyl or piperidinyl; R 2 means said groups (1) or (2) where Y means methyl; R 3 means H, F, Br, Cl, OH, NO 2 ,NR 15 R 16 ,C(=O)R 6 ; R 4 means hydrogen atom or alternatively when R 3 and R 4 are substituents near adjacent carbon atoms then R 3 and R 4 taken in common with carbon atoms with which they are bound form 5-7-membered carbocyclic system; R 5 means hydrogen atom; R 6 means C 1 -C 6 -alkyl; R 7 means a substituent at carbon atom taken among the group including fluorine, bromine, chlorine, iodine atom, C 1 -C 4 -alkyl, CH 2 OH,CH 2 OCH 3 , C 1 -C 4 -alkoxy-group, CHO, NR 15 R 16 ; means hydrogen atom; R 15 means hydrogen atom or C 1 -C 4 -alkyl; R 16 means hydrogen atom or C 1 -C 4 -alkyl; p = 0 or 1. Invention proposes also pharmaceutical compositions for inhibition of prostaglandin H-synthase and method of inhibition of prostaglandin H-synthase. EFFECT: new compounds, improved method of inhibition, valuable properties of compounds. 9 cl, 5 tbl |