HETEROCYCLIC DERIVATIVE AND PHARMACEUTICAL MEANS Russian patent published in 2017 - IPC C07D235/06 C07D235/08 C07D235/10 C07D235/12 C07D235/14 C07D235/26 C07D235/30 C07D231/56 C07D263/56 C07D401/12 C07D403/04 C07D403/12 C07D405/12 C07D409/12 C07D413/12 C07D417/12 C07D307/79 A61K31/343 A61K31/416 A61K31/4184 A61K31/423 A61K31/428 A61K31/433 A61K31/4439 A61K31/454 A61K31/5377 C07D405/04 

FIELD: pharmacology.

SUBSTANCE: invention relates to a heterocyclic derivative or a pharmaceutically acceptable salt thereof, of the general formula

, wherein ring A is a group represented by the general formulas , or , where X¹ is NH, NC₁-₆alkyl or O; A¹ is hydrogen; A² is i) hydrogen; ii) halogen; iii) C₁-₆alkyl optionally substituted by one to three groups selected from a group consisting of halogen, amino, mono(C₁-₆alkyl)amino, di(C₁-₆alkyl)amino, carbamoyl, mono(C₁-₆alkyl)aminocarbonyl, di(C₁-₆alkyl)aminocarbonyl, saturated cyclic aminocarbonyl, wherein the "saturated cyclic amino group" of the "saturated cyclic aminocarbonyl" part is 1-pyrrolidinyl, C₁-₆alkoxy and C₁-₆alkoxy-C₁-₆alkoxy; iv) C₃-₆cycloalkyl, optionally substituted by C₁-₆alkyl optionally substituted by one to three halogens; vi) a 4 to 5-membered saturated heterocyclic group containing one nitrogen or oxygen atom in the ring, optionally substituted by C₁-₆alkyl, (C₁-₆alkyloxy)carbonyl, (C₁-₆alkyl)carbonyl or hydroxy; (vii) C₁-₆alkylthio; (viii) C₁-₆alkylsulfonyl; ix) C₁-₆alkylsulfinyl; x) -NR³R⁴, where R³ and R⁴ are the same or different groups selected from a) hydrogen, b) optionally substituted C₁-₆alkyl, or c) C₃-₆cycloalkyl; or xi) saturated cyclic amino, wherein the "saturated cyclic amino" is piperidino, 1-piperazinyl or 4-morpholino, optionally substituted by C₁-₆alkyl, amino, mono(C₁-₆alkyl)amino, di(C₁-₆alkyl)amino, C₁-₆alkoxy or hydroxyl; R¹ is phenyl, benzyl, naphthyl, C₃-₆cycloalkyl, C₃-₆cycloalkylmethyl, heteroaryl wherein heteroaryl is benzothiadiazolyl, benzothiazolyl, indolyl, 1,1-dioxobenzothiophenyl, quinolyl or 1,3-benzoxazol-2-yl, 1,2,3,4-tetrahydronaphthalen-5-yl, 1,2, 3,4-tetrahydronaphthalen-6-yl, 2,3-dihydro-1H-inden-4-yl, 2,3-dihydro-1H-inden-5-yl or C₁-₆alkyl, wherein the said phenyl, benzyl, cycloalkyl, cycloalkylmethyl and heteroaryl are optionally substituted; R² is phenyl or pyridyl, wherein the said phenyl and pyridyl are optionally substituted. The invention also relates to a pharmaceutical composition and to an agent having the ability to inhibit mPGES-1 comprising a compound selected from the group consisting of a heterocyclic derivative of formula 1 and a pharmaceutically acceptable salt thereof as an active ingredient.

EFFECT: heterocyclic derivatives possessing the inhibitory activity of mPGES-1.

10 cl, 18 tbl, 257 ex