ORTHO-SUBSTUTUTED COMPOUNDS Ц NOVEL INHIBITORS OF PROSTAGLANDIN SYNTHASE, PHARMACEUTICAL COMPOSITIONS COMPRISING THEREOF AND METHOD OF INHIBITION OF PROSTAGLANDIN H-SYNTHASE Russian patent published in 2002 - IPC

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