Patent RU-2401265-C2 (RU)
Inventor: REHN PINDA
IPC: A61K31/506
Filed: 2005-06-09
Granted: 2010-10-10
Abstract: FIELD: chemistry. 
     SUBSTANCE: invention relates to novel compounds of formula (I), specifically compounds of formula (Ia) which have inhibiting activity during activity of kinase selected from Abl, BCR-AbI, PDGF-R, trkB, c-SRC, BMX, FGFR3, b-RAF, SGK, Tie2, Lck, JNK2a2, MKK4, c-RAF, MKK6, SAPK2a and SAPK2P and pharmaceutical compositions containing such compounds. In the compound of formula   I,   Ia, m and n are equal to 0; R 1  denotes XNR 5 R 6 , where X denotes a bond; R 5  is selected from hydrogen, C 1-6 alkyl, phenyl, C 5-10 heteroaryl-C 0-4 alkyl, C 3-6 cycloalkyl and C 3-10 heterocycloalkyl-C 0-4 alkyl, where the heteroaryl and heterocycloalkyl contain 1-2 heteroatoms selected from nitrogen and oxygen; and R 6  is selected from hydrogen and C 1-6 alkyl; or R 5  and R 6  together with the nitrogen atom with which both are bonded form a heteroaryl or heterocycloalkyl; where any of phenyl, heteroaryl, cycloalkyl and heterocycloalkyl, R 5  or a combination of R 5  and R 6  can be optionally substituted with 1-3 radicals independently selected from a halogen group, C 1-6 alkyl, C 1-6 alkoxy group, halogen-substituted alkyl, -XNR 7 R 8 , -XOR 7 , -XR 8 , -XC(O)NR 7 R 8 , -XC(O)NR 7 XNR 7 R 8 , -XNR 7 C(O)R 8 , -XR 9 ; where X denotes a bond or C 1-4 alkylene; R 7  and R 8  are independently selected from a group consisting of hydrogen and C 1-4 alkyl;and R 8  is selected form C 5-6 heterocycloalkyl and C 5-6 heteroaryl; where said heterocycloalkyl or heteroaryl contain 1-2 heteroatoms selected from nitrogen and oxygen, and said heterocycloalkyl or heteroaryl in R 8  is optionally substituted with a radical selected from a group consisting of C 1-4 alkyl and XOR 7 ; R 3  denotes -NR 10 R 11 ; where R 10  denotes hydrogen; R 11  denotes phenyl; where phenyl in R 11  is optionally substituted with 1-3 radicals selected from a halogen group, C 1-6 alkyl, C 1-6 alkoxy group, halogen-substituted alkyl, halogen-substituted alkoxy group, -NR 12 C(O)R 13 , -NR 12 C(O)NR 12 R 13  and -NR 12 S(O) 0-2 R 13 ; where R 12  denotes hydrogen; R 13  is selected from phenyl, C 5-6 heteroaryl and C 5-6 heterocycloalkyl; where any of phenyl, heteroaryl, cycloalkyl or heterocycloalkyl contains 1-2 heteroatoms selected from nitrogen and oxygen, and said heterocycloalkyl or heteroaryl in R 13  is substituted with 1-3 radicals independently selected from a halogen group, C 1-6 alkyl, halogen-substituted C 1-6 alkyl, C 1-6 alkoxy group, halogen-substituted C 1-6 alkoxy group, -XNR 7 R 8 , phenyl-C 0-4 alkyl, C 5-6 heteroaryl-C 0-4 alkyl, C 5-6 heterocycloalkyl-C 0-4 alkoxy group and C 5-6 heterocycloalkyl-C 0-4 alkyl; where X, R 7  and R 8  are described above, and where any of the phenyl, heteroaryl or heterocycloalkyl fragments contain 1-2 heteroatoms selected from nitrogen and oxygen, and said heterocycloalkyl or heteroaryl in R 13  optionally further substituted with 1-3 radicals independently selected from a halogen group, C 1-6 alkyl, halogen-substituted C 1-6 alkyl, hydroxy-substituted C 1-6 alkyl, C 1-6 alkoxy group; R 15  and R 16  are selected from phenyl substitutes given in values of R 11  and R 12  for formula I compounds. 
     EFFECT: compounds can be used to treat or prevent such diseases as proliferative disorders, and diseases resulting from anomalous activation of the immune and nervous systems. 
     8 cl, 1 tbl, 1 dwg, 1 ex