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(CHR5)p, where Z means O; R1 means phenyl or 2-naphthyl substituted with O-2-substituents of R7, C5-C7-cycloalkyl or C5-C7-cycloalkenyl under condition that R1 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 C1-C4-alkyl, quinolinyl or piperidinyl; R2 means said groups (1)
or (2)
where Y means methyl; R3 means H, F, Br, Cl, OH, NO2,NR15R16,C(=O)R6; R4 means hydrogen atom or alternatively when R3 and R4 are substituents near adjacent carbon atoms then R3 and R4 taken in common with carbon atoms with which they are bound form 5-7-membered carbocyclic system; R5 means hydrogen atom; R6 means C1-C6-alkyl; R7 means a substituent at carbon atom taken among the group including fluorine, bromine, chlorine, iodine atom, C1-C4-alkyl, CH2OH,CH2OCH3, C1-C4-alkoxy-group, CHO, NR15R16;
means hydrogen atom; R15 means hydrogen atom or C1-C4-alkyl; R16 means hydrogen atom or C1-C4-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
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Authors
Dates
2002-06-27—Published
1995-09-26—Filed