THIENO[3,2-d]PYRIMIDINE DERIVATIVES, POSSESSING INHIBITING ACTION WITH RESPECT TO PROTEINKINASE Russian patent published in 2014 - IPC C07D495/04 A61K31/519 A61K31/5377 A61K31/551 A61K31/496 A61P35/00 

Abstract RU 2524210 C2

FIELD: chemistry, pharmaceutics.

SUBSTANCE: invention relates to thieno[3,2-d]pyrimidine derivative of formula (I) or to its pharmaceutically acceptable salt: (I), where Y stands for -CH=CR1-, -C≡C- or -C(=O)NR1-; L stands for -C(=O)NR2-, -NR2C(=O)- or -NR2C(=O)NR2-; R1 and R2, each independently stands for H; R stands for H, a halogen atom, methyl or methoxy; E stands for phenyl or C3-10heteroaryl, which is non-substituted or substituted with 1-2 substituents, consisting of a group, which includes a halogen atom, -CF3, C1-6alkyl, hydroxy-C1-6alkyl, C3-8cycloalkyl, -(CH2)n-C1-6alkylamino, -(CH2)n-diC1-6alkylamino, -(CH2)nC1-6alkoxy, -(CH2)n-OS(=O)2-C1-6-alkyl, -(CH2)n-phenyl, -(CH2)n-C2-5heteroaryl and -(CH2)n-C4-6heterocycloalkyl, where C3-10heteroaryl represents pyridine, isoquinoline, indole or isoxazole, C2-5heteroaryl of radical -(CH2)n-C2-5heteroaryl represents imidazole or pyrrol, C4-6heterocycloalkyl of radical -(CH2)n-C4-6heterocycloalkyl represents piperazine, morpholine, diazepam, pyrrolidine or piperidine, and phenyl, heteroaryl and heterocycloalkyl each independently, is non-substituted or substituted with substituent selected from a group, which consists of C1-6alkyl, hydroxy-C1-6alkyl, a halogen atom and diC1-6alkylamino, n is equal to 0 or 1; and Z stands for H, -C(=O)R3, C1-6alkyl, hydroxyC1-6alkyl, C3-8cycloalkyl, piperidine, phenyl or pyridine, where piperidine, phenyl and pyridine, each independently, is non-substituted or substituted with C1-6alkyl, C1-6alkoxy or R3-piperazinyl and R3 represents C1-6alkyl or phenyl. The invention also relates to an intermediate compound for obtaining the claimed final compound of formula (I).

EFFECT: novel compound, which can be applied in medicine for the prevention or treatment of diseases, characterised by an anomalous growth of cells as a result of an excessive expression of proteinkinase, is obtained.

8 cl, 2 tbl, 128 ex

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RU 2 524 210 C2

Authors

Son Dzung Beom

Dzung Seung Khiun

Choj Va Il

Dzung Joung Khee

Choj Dzae Jul

Song Dzi Jeon

Li Kiu Khang

Li Dzae Chul

Kim Eun Joung

Akhn Jung Gil

Kim Maeng Sup

Choj Khvan Geun

Sim Tae Bo

Kham Joung Dzin

Park Dong-Sik

Kim Khvan

Kim Dong-Vook

Dates

2014-07-27Published

2011-01-31Filed