Synthesis and evaluation of 2,7-diamino-thiazolo[4,5-d] pyrimidine analogues as anti-tumor epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors
摘要:
2,7-Diamino-thiazolo[4,5-d]pyrimidine analogues were synthesized as novel epidermal growth factor receptor ( EGFR) tyrosine kinase inhibitors. Representative compounds showed potent and selective EGFR inhibitory activities and inhibited in vitro cellular proliferation in EGFR-overexpressing human tumor cells. The synthesis and preliminary biological, physical, and pharmacokinetic evaluation of these thiazolopyrimidine compounds are reported. (C) 2009 Elsevier Ltd. All rights reserved.
The present invention is directed to novel thiazolopyrimidine compounds of Formula (I) or a form or composition thereof
and the thereof as inhibitors of ATP-protein kinase interactions.
[EN] THIAZOLOPYRIMIDINE KINASE INHIBITORS<br/>[FR] INHIBITEURS DE LA THIAZOLOPYRIMIDINE KINASE
申请人:JANSSEN PHARMACEUTICA NV
公开号:WO2007019191A2
公开(公告)日:2007-02-15
[EN] The present invention is directed to novel thiazolopyrimidine compounds of Formula (I) or a form or composition thereof, and the use thereof as inhibitors of ATP-protein kinase interactions. [FR] L'invention concerne de nouveaux composés de thiazolopyrimidine de formule (I) ou leur forme ou composition et leur utilisation comme inhibiteurs des interactions de l'ATP-protéine kinase.