3-aryl substituted pyrazolo¬4,3-d|pyrimidine derivatives;...

C - Chemistry – Metallurgy – 07 – D

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C07D 487/04 (2006.01) A61K 31/505 (2006.01)

Patent

CA 2276610

This invention encompasses compounds of formula (I), wherein Ar represents a mono-, di- or trisubstituted aryl group where at least one position on Ar ortho to the point of attachment to the pyrazole ring is substituted; and R1 represents lower alkyl; R2 is hydrogen or lower alkyl; and R3 and R4 independently represent organic and inorganic substituents, which compounds are highly selective partial agonists or antagonists at human CRF1 receptors and are useful in the diagnosis and treatment of treating stress related disorders such as post traumatic stress disorder (PTSD) as well as depression, headache and anxiety.

L'invention concerne des composés représentés par la formule (I), dans laquelle Ar représente un groupe aryle à une, deux ou trois substitutions dont au moins une position sur Ar en ortho par rapport au point de fixation du noyau pyrazole est substituée; R¿1? représente un alkyle inférieur; R¿2? représente un hydrogène ou un alkyle inférieur; R¿3? et R¿4? représentent indépendamment des substituants organiques ou inorganiques. Ces composés constituent des agonistes ou des antagonistes partiels hautement sélectifs pour des récepteurs de CRF¿1? humain, et sont utiles dans le diagnostic et le traitement de troubles associés au stress, tels des troubles de stress post-traumatique (SSPT), des dépressions, des maux de tête ou l'anxiété.

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