9h-pyrimido¬4,5-b|indole derivatives: crf1 specific ligands

Details 9h-pyrimido¬4,5-b|indole derivatives: crf1 specific ligands 9h-pyrimido¬4,5-b|indole derivatives: crf1 specific ligands

C - Chemistry, Metallurgy

07

D

C07D 487/04 (2006.01) A61K 31/519 (2006.01) A61P 25/00 (2006.01) C07D 209/00 (2006.01) C07D 239/00 (2006.01) G01N 33/566 (2006.01)

Patent

CA 2371271

Disclosed are compounds of formula (I), wherein Ar, R1, R2, R3, R4 and R5 are defined herein, which compounds are selective antagonists at CRF1 receptors and are therefore useful in the diagnosis and treatment of stress related disorders such as post traumatic stress disorder (PTSD) as well as depression, headache, anxiety, cardiovascular disorders, and eating disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also disclosed.

L'invention concerne des composés de formule (I), dans laquelle Ar, R?1¿, R?2¿, R?3¿, R?4¿ et R?5¿ sont définis dans le dossier. Lesdits composés sont des antagonistes sélectifs au niveau des récepteurs de la corticolibérine CRF1 et sont donc utiles dans le diagnostic et le traitement de troubles liés au stress, tels que les états de stress post-traumatique ainsi que la dépression, la migraine, l'anxiété, les troubles cardio-vasculaires et les troubles alimentaires. Des méthodes de traitement desdits troubles ainsi que des compositions pharmaceutiques conditionnées sont également décrites.

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