FIELD: medicine, pharmaceutics.
SUBSTANCE: present invention refers to new imidazo[4,5-b]pyrazine derivatives of general formula 
or to its pharmaceutically acceptable salt wherein: R1 represents either aryl unsubstituted or substituted by one of the groups: halogen, hydoxyl, C1-6alkyl, C1-6alkoxyl, NH2, NHC1-6alkyl, N(C1-6alkyl)2, NHC1-6alkylC1-6alkoxy, C1-6alkylhydroxy, -C(O)NH2, -C(O)OC1-6alkyl, -C(O)NH C1-6alkyl, cyano, carboxy, heteroaryl and heterocycloalkyl; or heteroaryl unsubstituted or substituted by one of the groups: C1-6alkoxy, hydroxy, -C1-6alkyl, NH2 and NHC1-6alkyl; heterocycloalkyl unsubstituted or substituted by one group =O; and R2 represents H; unsubstituted C3-4alkyl; C1-4alkyl substituted by C5-6cycloalkyl unsubstituted or substituted by one group specified in amino, hydroxyl, C1-6alkoxy, or heterocycloalkyl unsubstituted or substituted by 1-2 groups specified in =O, C1-6alkyl; or C5-6cycloalkyl substituted by one group specified in hydroxyl, C1-6alkoxyl, C1-6alkylC1-6alkoxy, C1-6alkylhydroxy, CONH2; or substituted ir unsubstituted heterocycloalkyl; wherein aryl represents an aromatic structure consisting of 6-10 carbon atoms containing one ring or two condensed rings; wherein heteroaryl represents a 5-10-member aryl ring system containing 1-2 heteroatoms specified in nitrogen, oxygen and sulphur; wherein heterocycloalkyl represents a 5-9-member nonaromatic cycloalkyl wherein 1-2 heteroatoms specified in nitrogen and oxygen; provided the compound does not represent 1,3-dihydro-5-phenyl-2H-imidazo[4,5-b]pyrazin-2-one. Also, the invention refers to the specific imidazo[4,5-b]pyrazine derivatives, to a based pharmaceutical composition, to a method of treating or preventing cancer, inflammatory conditions, immunological diseases, metabolic conditions, and to a method of kinase inhibition in a cell expressing said kinase.
EFFECT: there are produced new imidazo[4,5-b]pyrazine derivatives showing effective biological properties.
17 cl, 2 tbl, 210 ex
| Title | Year | Author | Number |
|---|---|---|---|
| METHODS OF OBTAINING AND PURIFICATION OF HETEROARYL COMPOUNDS | 2010 |
|
RU2557242C2 |
| IMIDAZOPIRASOTHINES AS PDE1 INHIBITORS | 2016 |
|
RU2712219C2 |
| MTOR KINASE INHIBITORS FOR ONCOLOGIC INDICATIONS AND DISEASES ASSOCIATED WITH MTOR/PI3K/AKT BY METABOLISM | 2009 |
|
RU2692796C2 |
| mTOR KINASE INHIBITORS FOR ONCOLOGICAL INDICATIONS AND DISEASES METABOLICALLY BOUND TO mTOR/PI3K/AKT | 2009 |
|
RU2546658C2 |
| IMIDAZOTRIAZINONE COMPOUNDS | 2011 |
|
RU2603140C2 |
| HETEROARYL COMPOUNDS, THEIR COMPOSITIONS AND USE THEREOF AS PROTEIN KINASE INHIBITORS | 2007 |
|
RU2474582C2 |
| IMIDAZOPYRIDIN-2-ONE DERIVATIVES, HAVING mTOR INHIBITING ACTIVITY | 2009 |
|
RU2478636C2 |
| IDENTIFICATION OF LKB1 MUTATION AS PROGNOSTIC BIOMARKER OF SENSITIVITY TO TOR-KINASE INHIBITORS | 2011 |
|
RU2565034C2 |
| HETEROCYCLIC COMPOUNDS AS PRMT5 INHIBITORS | 2018 |
|
RU2797822C2 |
| AMINOTRIAZOLOPYRIDINES AND USING THEM AS KINASE INHIBITORS | 2009 |
|
RU2552642C2 |
