NEW TRIAZOLOPYRASINE DERIVATIVES AND THEIR APPLICATION Russian patent published in 2018 - IPC C07D487/04 A61K31/4985 A61K31/5377 A61P35/00 

Abstract RU 2643361 C2

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

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RU 2 643 361 C2

Authors

Dzhun Khee Dzhun

Kha Dzhe Du

Cho Sun Yun

Kim Kheun Re

Lee Kvan Kho

Lee Chkhon Ok

Chkhoi San Un

Park Chkhi Khoon

Dates

2018-02-01Published

2013-09-30Filed