2,3,4,9-TETRAHYDRO-1H-CARBAZOLE DERIVATIVES AS CRTH2 RECEPTOR ANTAGONISTS Russian patent published in 2010 - IPC C07D209/88 A61K31/404 A61P37/08 A61P37/00 

FIELD: chemistry.

SUBSTANCE: invention relates to novel compounds selected from a group comprising 2,3,4,9-tetrahydro-1H-carbazoles of formula I

,

where R¹, R², R³ and R⁴ independently denote hydrogen, alkyl, alkoxy, halogen, nitro, cyano, trifluoromethyl or formyl, R⁵ denotes hydrogen, alkyl or -CF₃, R⁶ denotes alkoxy, arylalkoxy, selected from benzyloxy and 1-phenylethoxy, or -NR⁷R⁸, R⁷ and R⁸ independently denote hydrogen, alkyl, cyanoalkyl, alkenyl, where alkenyl is ethenyl, 2-propenyl, 2-methyl-2-propenyl, 3-butenyl, 4-pentenyl or 5-hexenyl; aryl, where aryl is a phenyl or naphthyl radical, where said radicals can optionally be monosubstituted with a halogen, alkyl, alkoxy, -CF₃, -OCF₃, phenylalkyl or phenylcarbonyl; or disubstituted with a substitute independently selected from halogen, alkoxy and phenyl; arylalkyl, where arylalkyl is phenylalkyl, where the alkyl group can optionally be substituted with phenyl; phenylalkyl, where the phenyl ring can optionally be substituted with methylenedioxy; phenylalkyl which is disubstituted with a halogen; phenylalkyl which is monosubstituted with a halogen, -CF₃, -OCHF₂, alkyl or alkylsulfanyl; or naphthylalkyl; phenylcarbonyl; cycloalkyl, where cycloalkyl is a cyclopentyl or cyclohexyl radical, where said radicals can optionally be substituted with a condensed benzene ring; pyridylalkyl; thienylalkyl; or R⁷ and R⁸ together with a nitrogen atom to which they are bonded form a heterocyclic 5-, 6-, 7- or 8-member ring system containing 1-3 heteroatoms selected from nitrogen, oxygen and sulphur atoms, wherein said cyclic system can optionally be substituted with (1) one or two condensed benzene rings, where the benzene rings are unsubstituted or substituted with one or two substitutes independently selected from a group comprising C₁-C₄alkyl, C₁-C₄alkoxy, halogen, -CF₃ and -OCF₃; (2) unsubstituted phenyl ring, (3) mono- or disubstituted phenyl ring, where the substitutes are independently selected from a group comprising halogen, C₁-C₄alkyl, C₁-C₄alkoxy, -CF₃ and -OCF₃; or (4) phenylalkyl, where the alkyl group is substituted with phenyl; where the term "alkyl", separately or in any combination, denotes a saturated straight or branched hydrocarbon chain containing 1-7 carbon atoms; where the said alkyl group is unsubstituted unless stated otherwise; or to pharmaceutically acceptable salts thereof. Invention also relates to a pharmaceutical composition and to use of compounds in claim 1.

EFFECT: obtaining novel biologically active compounds having CRTH2 receptor antagonist activity.

13 cl, 5 tbl