Patent RU-2425826-C2 (RU)
Inventor: PAN SHIFEHN
IPC: A61P17/00
Filed: 2007-07-20
Granted: 2011-08-10
Abstract: 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 -CR 1 =, -CR 2 =, -CR 3 =, -CR 4 = and -CR 5 =, where 0 or 1 in these groups is replaced with N, R 1 , R 2 , R 3 , R 4  and R 5  are independently selected from a group comprising hydrogen, hydroxy, halogen, cyano, cyano(C 1 -C 6 )alkyl, C 4 -C 6  heterocycloalkyl-C 0 -alkyl, where the said heterocycloalkyl contains 1-2 heteroatoms selected from nitrogen and oxygen atoms, C 5 heteroaryl-(C 0 -C 4 )alkyl, where the said heteroaryl contains 1-4 heteroatoms selected from nitrogen atoms, -XSO 2 R 11 , -XSO 2 NR 11 R 12 , -XSO 2 NR 11 C(O)R 12 , -XC(NR 11 )NR 11 OR 12 , -XCR 11 =NOR 12 , -XC(O)R 11 , -XC(O)OR 11 , -XNR 11 R 12 , -XC(O)NR 11 R 12 , -XOC(O)NR 11 R 12 , -XNR 11 C(O)NR 11 R 12 , -XNR 11 XOR 12 ; -XN(XOR 12 ) 2 , -XNR 11 XC(O)OR 12  -XNR 11 XNR 11 C(O)R 12  -XNR 11 XNR 11 R 12 , -XNR 11 C(O)R 12 , where each X is independently selected from a group comprising a chemical bond and C 1 -C 4 alkylene, each R 11  is selected from a group comprising hydrogen and C 1 -C 6 alkyl, and R 12  is selected from a group comprising hydrogen, C 1 -C 6 alkyl and phenyl, or R 11  and R 12  together with a nitrogen atom to which R 11  and R 12  are bonded form C 6 heterocycloalkyl. Said heteroaryl or heterocycloalkyl in R 1 , R 2 , R 3 , R 4  or R 5  optionally contains one substitute selected from a group comprising hydroxyl, cyano, C 1 -C 6 alkyl, hydroxyl(C 1 -C 6 )alkyl and carboxy, R 6  and R 7  independently denote hydrogen, R 8  is selected from a group comprising C 1 -C 6 alkyl, halogen(C 1 -C 3 )alkyl, -CH 2 OR 8a  and -COOR 8a  or two R 8  groups bonded to different carbon atoms, together form a (C 1 -C 2 )alkyl bridge, or two R 8a  groups bonded to one carbon atom form a (C 3 -C 8 )cycloalkyl group, where R 8a  is selected from a group comprising hydrogen and C 1 -C 6 alkyl, R 9  is selected from a group comprising phenyl and C 6 heteroaryl, where the said heteroaryl contains 1-2 heteroatoms selected from nitrogen atoms, and C 9 heteroaryl, where the said heteroaryl contains 1-2 heteroatoms selected from nitrogen and oxygen atoms, where the said phenyl or heteroaryl in R 9  is optionally substituted with 1-2 substitutes independently selected from a group comprising halogen, cyano, hydroxy, C 1 -C 3 alkyl, halogen(C 1 -C 3 )alkyl, hydroxy(C 1 -C 3 )alkyl, -C(O)R 13 , -C(O)NR 13 R 14 , where each of R 13  and R 14  is independently selected from a group comprising hydrogen and C 1 -C 6 alkyl, R 10  denotes hydrogen, Y and Z are independently selected from a group comprising CR 20  and N, where R 20  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