Discovery of GlyT1 inhibitors with improved pharmacokinetic properties
摘要:
Glycine transporter 1 (GlyT1) represents a novel target for the treatment of schizophrenia via the potentiation of glutamatergic NMDA receptors. The discovery of 4,4-disubstituted piperidine inhibitors of GlyT1 which exhibit improved pharmacokinetic properties, including oral bioavailability, is discussed. (C) 2009 Elsevier Ltd. All rights reserved.
The invention provides compounds of formula I
and pharmaceutically acceptable salts thereof.
The formula I thiazolyl compounds inhibit tyrosine kinase activity thereby making them useful as anticancer agents and for the treatment of Alzheimer's disease.
[EN] THIAZOLYL COMPOUNDS USEFUL AS KINASE INHIBITORS<br/>[FR] COMPOSÉS DE THIAZOLYLE EN TANT QU'INHIBITEURS DE KINASE
申请人:BRISTOL MYERS SQUIBB CO
公开号:WO2008124757A1
公开(公告)日:2008-10-16
[EN] The invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof. The formula I thiazolyl compounds inhibit tyrosine kinase activity thereby making them useful as anticancer agents and for the treatment of Alzheimer's disease. [FR] La présente invention concerne des composes de formule (I) et leurs sels pharmaceutiquement acceptables. Les composés de thiazolyle de formule I sont inhibiteurs de l'activité tyrosine kinase et donc utiles en tant qu'agents anticancéreux et pour le traitement de la maladie d'Alzheimer.