PYRIDINE DERIVATIVE Russian patent published in 2018 - IPC C07D401/04 C07D401/14 C07D409/14 A61K31/4439 A61P3/10 A61P9/10 

FIELD: pharmacology.

SUBSTANCE: invention relates to a pyridine derivative of formula (I) , a prodrug thereof, wherein A is a single bond or an oxygen atom; R₁ represents a nitrogen atom or CH; one of X₁-X₅ is a nitrogen atom, and the remaining four are CR₂; R₂ each independently represent a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, an alkenyl group having 2 to 6 carbon atoms, an alkynyl group having 2 to 6 carbon atoms, a halogen atom, a trifluoromethyl group, a difluoromethyl group, a cyano group, an alkylcarbonyl group having 2 to 7 carbon atoms, an alkylsulfonyl group having 1 to 6 carbon atoms, a nitro group, an amino group, a dialkylamino group having 1 to 6 carbon atoms which optionally can form a ring, a formyl group, an alkoxy group having 1 to 6 carbon atoms (which may optionally have one or more substituents selected from a hydroxyl group, a phenyl group, a cyclohexyl group and a halogen atom), an alkylthio group having 1 to 6 carbon atoms, a phenyl a group (which may optionally have one or more substituents selected from an alkyl group having 1 to 6 carbon atoms, an alkoxy group having 1 to 6 carbon atoms and a halogen atom) or a phenoxy group (which may optionally have one or more substituents selected from an alkyl group having 1-6 carbon atoms, an alkoxy group having 1-6 carbon atoms, and a halogen atom), provided that when two CR₂ are located side by side, two R₂ substituents can be optionally combined with cycle formation; R₃ represents a hydrogen atom, an alkyl group having 1 to 6 carbon atoms (which may optionally have one or more substituents selected from a hydroxyl group, an amino group, a dialkylamino group having 1 to 6 carbon atoms which can optionally form a ring, an imidazole ring, a pyrazole ring, a pyrrolidine ring, a piperidine ring, a morpholine ring and a piperazine ring (which may optionally have one or more substituents selected from an alkyl group having 1 to 6 carbon atoms and alkylsulfonyl group containing from 1 to 6 carbon atoms), an alkenyl group having 2 to 6 carbon atoms, an alkynyl group having 2 to 6 carbon atoms, an alkoxy group having 1 to 6 carbon atoms (which may optionally have one or more substituents selected from a hydroxyl group and a halogen atom), an alkylcarbonyl group having 2-7 carbon atoms, an alkylthio group having 1-6 carbon atoms, an alkylsulfinyl group having 1-6 carbon atoms, a halogen atom, a trifluoromethyl group, a difluoromethyl group, a cyano group, a phenyl group (which may optionally have one or more substituents selected from an alkyl group having 1 to 6 carbon atoms, an alkoxy group having 1 to 6 carbon atoms and a halogen atom), a pyridyl group (which may optionally have one or more substituents selected from an alkyl group having 1 to 6 carbon atoms, an alkoxy group having 1 to 6 carbon atoms and a halogen atom), a phenoxy group (which may optionally have one or more substituents selected from an alkyl group having 1 to 6 carbon atoms, an alkoxy group having 1 to 6 carbon atoms and a halogen atom), a carboxyl group, or -CO₂ R₅; R₄ represents a carboxyl group, a tetrazolyl group, -CONHSO₂R₅, -CO₂R₅ or any of the following substituents: , provided that when R₃ represents an alkyl group having 1 to 6 carbon atoms substituted by a hydroxyl group, and when R₄ represents a carboxyl group, then R₃ and R₄ can optionally be combined to form a lactone cycle; R₅ in R₃ and R₄ each independently represents an alkyl group having 1 to 6 carbon atoms; Z is any of the following substituents, designated as Z1-Z7 (their meanings are defined in claim 1) that can be used to treat or prevent diseases associated with URAT1 such as gout, hyperuricemia, hypertension, kidney diseases such as interstitial nephritis, diabetes, arteriosclerosis and Lesch-Nyhan syndrome.

EFFECT: compound application efficiency increase.

23 cl, 55 tbl, 303 ex