COMPOUNDS AND COMPOSITIONS AS ITPKb INHIBITORS Russian patent published in 2011 - IPC C07D231/12 C07D401/12 C07D401/14 C07D403/12 C07D413/14 C07D491/48 A61K31/415 A61K31/44 A61P17/00 A61P19/02 

FIELD: chemistry.

SUBSTANCE: invention relates to novel pyrazole derivatives of general formula I

and pharmaceutically acceptable salts thereof, where n equals 1 or 2, m equals 0, 1 or 2, A contains in the ring a group selected from -CR₁=, -CR₂=, -CR₃=, -CR₄= and -CR₅=, where 0 or 1 in these groups is replaced with N, R₁, R₂, R₃, R₄ and R₅ are independently selected from a group comprising hydrogen, hydroxy, halogen, cyano, cyano(C₁-C₆)alkyl, C₄-C₆ heterocycloalkyl-C₀-alkyl, where the said heterocycloalkyl contains 1-2 heteroatoms selected from nitrogen and oxygen atoms, C₅heteroaryl-(C₀-C₄)alkyl, where the said heteroaryl contains 1-4 heteroatoms selected from nitrogen atoms, -XSO₂R₁₁, -XSO₂NR₁₁R₁₂, -XSO₂NR₁₁C(O)R₁₂, -XC(NR₁₁)NR₁₁OR₁₂, -XCR₁₁=NOR₁₂, -XC(O)R₁₁, -XC(O)OR₁₁, -XNR₁₁R₁₂, -XC(O)NR₁₁R₁₂, -XOC(O)NR₁₁R₁₂, -XNR₁₁C(O)NR₁₁R₁₂, -XNR₁₁XOR₁₂; -XN(XOR₁₂)₂, -XNR₁₁XC(O)OR₁₂ -XNR₁₁XNR₁₁C(O)R₁₂ -XNR₁₁XNR₁₁R₁₂, -XNR₁₁C(O)R₁₂, where each X is independently selected from a group comprising a chemical bond and C₁-C₄alkylene, each R₁₁ is selected from a group comprising hydrogen and C₁-C₆alkyl, and R₁₂ is selected from a group comprising hydrogen, C₁-C₆alkyl and phenyl, or R₁₁ and R₁₂ together with a nitrogen atom to which R₁₁ and R₁₂ are bonded form C₆heterocycloalkyl. Said heteroaryl or heterocycloalkyl in R₁, R₂, R₃, R₄ or R₅ optionally contains one substitute selected from a group comprising hydroxyl, cyano, C₁-C₆alkyl, hydroxyl(C₁-C₆)alkyl and carboxy, R₆ and R₇ independently denote hydrogen, R₈ is selected from a group comprising C₁-C₆alkyl, halogen(C₁-C₃)alkyl, -CH₂OR_8a and -COOR_8a or two R₈ groups bonded to different carbon atoms, together form a (C₁-C₂)alkyl bridge, or two R_8a groups bonded to one carbon atom form a (C₃-C₈)cycloalkyl group, where R_8a is selected from a group comprising hydrogen and C₁-C₆alkyl, R₉ is selected from a group comprising phenyl and C₆heteroaryl, where the said heteroaryl contains 1-2 heteroatoms selected from nitrogen atoms, and C₉heteroaryl, where the said heteroaryl contains 1-2 heteroatoms selected from nitrogen and oxygen atoms, where the said phenyl or heteroaryl in R₉ is optionally substituted with 1-2 substitutes independently selected from a group comprising halogen, cyano, hydroxy, C₁-C₃alkyl, halogen(C₁-C₃)alkyl, hydroxy(C₁-C₃)alkyl, -C(O)R₁₃, -C(O)NR₁₃R₁₄, where each of R₁₃ and R₁₄ is independently selected from a group comprising hydrogen and C₁-C₆alkyl, R₁₀ denotes hydrogen, Y and Z are independently selected from a group comprising CR₂₀ and N, where R₂₀ denotes hydrogen, provided that compounds of formula I do not include compounds of formula II, which are described in claim 1, and provided that compounds of formula I do not include compounds which are: 1-(4-fluorophenyl)-4-((3-phenyl-1H-pyrazol-4-yl)methyl)piperazine, 1- ((3-(4-fluorophenyl)-1H-pyrazol-4-yl)methyl)-4-(4-(trifluoromethyl)-(pyridin-2- yl)piperazine, 1-((3-(4-fluorophenyl)-1H-pyrazol-4-yl)methyl)-4-(5-(trifluoromethyl)-(pyridin-2-yl)piperazine and 1-((3-(4-fluorophenyl)-1H-pyrazol-4-yl)methyl)-4-(5-fluoropyridin-2-yl)piperazine. The invention also relates to specific compounds obtained.

EFFECT: novel pyrazole derivatives which can be used in treating diseases or disorders which are mediated by disrupted activation of the said compound are obtained.

8 cl, 1 tbl, 4 ex