FIELD: pharmacology.
SUBSTANCE: invention relates to a triazolopyrazine derivative represented by chemical formula 1 , where R1-R3 each independently represents hydrogen, halogen; 6-membered heterocycloalkyl with one heteroatom representing nitrogen, unsubstituted or substituted C1-C5-alkyl, hydroxy-C1-C5-alkyl; 6-membered heterocycloalkenyl with one heteroatom representing nitrogen, unsubstituted or substituted C1-C5-alkyl, hydroxy-C1-C5-alkyl; C1-C3-alkoxy substituted by 6-membered heterocycloalkyl with two heteroatoms, each independently being nitrogen, oxygen, which is optionally substituted by C1-C5-alkyl; C1-C5-alkyl substituted by 6-membered heterocycloalkyl with two heteroatoms, each of which is independently nitrogen, oxygen, which is optionally substituted with C1-C5-alkyl; phenyl substituted with halogen; C1-C5-alkyl substituted by 6-membered heterocycloalkyl with two heteroatoms, each of which is independently nitrogen, oxygen, which is optionally substituted by C1-C5-alkyl; C1-C3alkoxy, substituted by 6-membered heterocycloalkyl with two heteroatoms, each of which is independently nitrogen, oxygen, which is optionally substituted by C1-C5-alkyl; acetylpiperazine-C1-C5-alkyl or methylpiperazinylcarbonyl; or 5-membered heteroaryl with two heteroatoms representing nitrogen, substituted by 6-membered heterocycloalkyl with one heteroatom representing nitrogen, hydroxy-C1-C5-alkyl or C1-C5-alkyl; where at least one of R1-R3 is not hydrogen; among R4 and R5 each independently represents hydrogen, 5-membered heteroaryl containing two heteroatoms representing nitrogen, unsubstituted or substituted C1-C5-alkyl, or phenyl substituted by cyano or halogen; where at least one of R4 and R5 is not hydrogen; and X is oxygen or carbon. The invention also relates to pharmaceutical compositions and to a method for prevention or treatment of hyperproliferative disorders mediated by c-Met tyrosine kinase.
EFFECT: new compounds with inhibitory activity against c-Met tyrosine kinase are obtained.
10 cl, 2 tbl, 7 ex
Title | Year | Author | Number |
---|---|---|---|
GCN2 INHIBITORS AND THEIR USE | 2019 |
|
RU2811408C2 |
FIVE-MEMBERED HETEROCYCLIC PYRIDINE COMPOUNDS AND PREPARATION METHOD AND USE THEREOF | 2014 |
|
RU2668074C2 |
GCN2 INHIBITORS AND THEIR USE | 2019 |
|
RU2811403C2 |
ANELLATED 9-HYDROXY-1,8-DIOXO-1,3,4,8-TETRAHYDRO-2H-PYRIDO[1,2-A]PYRAZINE-7-CARBOXAMIDES - INTEGRASE INHIBITORS, METHODS FOR PREPARING AND USING THEREOF | 2019 |
|
RU2717101C1 |
AZADECALINS CONDENSED WITH HETEROARYLKETONES - GLUCOCORTICOID RECEPTOR MODULATORS | 2013 |
|
RU2639867C2 |
BI-ARYL-META-PYRIMIDINE KINASE INHIBITORS | 2006 |
|
RU2597364C2 |
BI-ARYL-META-PYRIMIDINE KINASE INHIBITORS | 2006 |
|
RU2589878C2 |
{3-[(7H-PYRROLO[2,3-d]PYRIMIDIN-4-YL)AZOLYL]AZETIDIN-3-YL} ACETONITRILES AS JANUS KINASE INHIBITORS | 2015 |
|
RU2601410C1 |
CXCR7 ANTAGONISTS | 2013 |
|
RU2649004C2 |
PYRAZOL-4-YL-HETEROCYCLYL-CARBOXAMIDE COMPOUNDS AND METHODS FOR APPLICATION | 2012 |
|
RU2638552C2 |
Authors
Dates
2018-02-01—Published
2013-09-30—Filed