FIELD: medicine, pharmaceutics.
SUBSTANCE: invention relates to novel compounds of formula I:
, where: U, V and W independently represent CR5 where R5 stands for H, C1-C6alkyl; Q stands for NR5, NNR5, NO, CR5, where R5 stands for H, C1-C6alkyl; L1 stands for -NR5C(O)-, -NR5C(O)NR5-, -C(O)NR5-, -NR5- and C5heteroaryl, containing 2 N atoms and 1 O atom, where R5 stands for H, C1-C6alkyl; L2 represents bond, -O-, -NR5C(O)-, -NR5C(O)NR5-, -C(O)NR5- ,-NR5-, where R5 stands for H, C1-C6alkyl; n = 0 or 1; m = 0, 1, 2, 3 or 4; R1 stands for C6-C10aryl and C5heteroaryl, containing 1 N atom, condensed with benzene; where any aryl, heteroaryl, contained in R1, can be optionally substituted with 1-3 radicals, which represent halogen, NH2, NO2, CN, C1-C6alkyl, C1-C6alkoxygroup, halogen-substituted C1-C6alkyl, halogen-substituted C1-C6alkoxygroup, C6-C10aryl-C0-C4alkyl, C5-C6heteroaryl-C0-C4alkyl, containing 1 or 2 N, C5-C6heterocycloalkyl-C0-C4alkyl, containing 1 or 2 N and/or O atoms; where methylene fragment of any alkyl group can be optionally substituted with O; where any aryl, heteroaryl or heterocycloalkyl substituent, contained in R1, can be optionally substituted with 1-3 radicals, which independently represent C1-C6alkyl, C1-C6alkoxygroup, halogen-substituted C1-C6alkyl, halogen-substituted C1-C6alkoxygroup and hydroxy-substituted C1-C6alkyl; R2 represents halogen, NH2, NO2, CN, C1-C6alkyl, C1-C6alkoxygroup, halogen-substituted C1-C6alkyl, halogen-substituted C1-C6alkoxygroup, C6-C10aryl-C0-C4alkyl, C5heteroaryl-C0-C4alkyl, containing 1 or 2 N, C6heterocycloalkyl-C0-C4alkyl, containing 1 or 2 N atoms and/or O; where any aryl, heteroaryl or heterocycloalkyl, contained in R2, is optionally substituted with 1-3 radicals, which independently represent halogen, NH2, NO2, CN, C1-C6alkyl, C1-C6alkoxygroup, halogen-substituted C1-C6alkyl and halogen-substituted C1-C6alkoxygroup; R3 represents H, C1-C6alkyl; R4 represents H, -XR6, -XNR5XR6, -XOXR6 and -XNR5XNR5R6; where each X independently represents bond and C1-C4alkylene; where any alkylene, contained in X can be optionally substituted with OH; R5 represents H, C1-C6alkyl; R6 represents C6-C10aryl and C5heteroaryl, containing 1 or 2 N and/or O, optionally condensed with benzene; where any aryl, heteroaryl, contained in R6, can be optionally substituted with 1-3 radicals, which independently represent C1-C6alkyl, OH, CN, -NR5S(O)0-2R5, -S(O)0-2NR5R5, - NR5S(O)0-2NR5R5, -C(O)NR5XNR5R5, -XNR5XNR5R5, -C(O)R7, -C(O)NR5XOR5, -C(O)NR5R5, -C(O)NR5R7, -C(O)NR5XR7 and -XC(O)OR5; where each X independently represent bond and C1-C4alkylene; where any alkylene, contained in X, is optionally substituted with OH; where each; R5 represents H, C1-C6alkyl; R7 represents C5-C6heterocycloalkyl-C0-C4alkyl, containing 1 or 2 N and/or O, where any heterocycloalkyl, contained in R7, is optionally substituted with radical, which represents diethylaminoethyl, dimethylaminogroup, aminogroup, C1-C6alkyl, pyrimidinyl, pyrazinyl, halogen-substituted C1-C6alkyl and -C(O)OR5; and its pharmaceutically acceptable salts, hydrates, solvates.
EFFECT: compounds possess inhibiting activity with respect to series of kinases, which allows to use them in pharmaceutical composition.
10 cl, 1 tbl, 6 ex
| Title | Year | Author | Number |
|---|---|---|---|
| COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS | 2006 |
|
RU2368602C2 |
| HETEROCYCLIC NITROGEN PYRROLE DERIVATIVES, PRODUCING THEM AND PHARMACEUTICAL APPLICATION | 2008 |
|
RU2473543C2 |
| DERIVATIVES OF PYRROLO[3,2-c]PYRIDIN-4-ONE 2-INDOLINONE AS PROTEINKINASE INHIBITORS | 2007 |
|
RU2410387C2 |
| 2-(2-OXOINDOLIN-3-YLIDENE)METHYL-5-(2-HYDROXY-3-MORPHOLIN-4-YLPROPYL)-6,7-DIHYDRO-1-H-PYRROLE[3,2-C]PYRIDIN-4(5H)-ONE COMPOUNDS AND USE THEREOF AS PROTEIN KINASE INHIBITORS | 2008 |
|
RU2472792C2 |
| COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS | 2005 |
|
RU2401265C2 |
| HETEROCYCLIC INHIBITORS OF Hh-SYGNAL CASCADE, BASED ON THEM MEDICINAL COMPOSITIONS AND METHOD OF TREATING DISEASES INDUCED BY ABBARANT ACTIVITY OF Hh-SIGNAL SYSTEM | 2007 |
|
RU2364597C1 |
| DERIVATIVES OF INDOLINE USED AS PROTEIN KINASE INHIBITORS | 2002 |
|
RU2316554C2 |
| PYRROLOPYRAZINE KINASE INHIBITORS | 2009 |
|
RU2503676C2 |
| BICYCLIC HETEROCYCLE COMPOUNDS AND THEIR USES IN THERAPY | 2012 |
|
RU2662827C2 |
| SELECTIVE HISTAMINE H4 RECEPTOR ANTAGONISTS FOR TREATING VESTIBULAR DISORDERS | 2009 |
|
RU2589846C2 |
