3-(sulfonyl)pyrazolo[1,5-a]pyrimidines - antagonists of...

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 487/04 (2006.01) A61K 31/519 (2006.01) A61P 3/04 (2006.01) A61P 3/08 (2006.01) A61P 9/10 (2006.01) A61P 25/08 (2006.01) A61P 25/16 (2006.01) A61P 25/18 (2006.01) A61P 25/26 (2006.01) A61P 25/28 (2006.01)

Patent

CA 2749742

The present invention relates to novel substituted 3- (arylsulfonyl)pyrazolo[1,5-a]pyrimidines of general formula 1 pharmaceutically acceptable salts and/or hydrates, to novel serotonin 5-HT6 receptor antagonists, to novel drug substances, pharmaceutical compositions, medicaments and methods for their preparation and use for treatment and prophylaxis of pathological states and diseases of CNS, pathogenesis of which is associated with disturbance of serotonin 5-HT6 receptor activation. In compounds of general formula 1 (see formula 1) Ar represents optionally substituted aryl or heterocyclyl; R1, R2 and R3 independently of each other represent hydrogen, C1-C3 alkyl or phenyl; R4 represents hydrogen, optionally substituted C1-C5 alkyl, substituted hydroxyl group or substituted sulfanyl group.

L'invention concerne de nouvelles 3-sulfonyl-pyrazolo[1,5-a] pyrimidines ayant la formule générale (1) ou leurs sels et/ou hydrates pharmaceutiquement acceptables, de nouveaux antagonistes de récepteurs 5-HT6 de sérotonine, de nouvelles préparations médicinales, compositions pharmaceutiques, des préparations médicinales et des procédés pour leurs préparation et utilisation pour le traitement et la prévention des états pathologiques et des maladies du SNC dont la pathogenèse est due aux troubles d'activation des récepteurs 5-HT6 de sérotonine. Dans les composants ayant la formule générale (1): Ar est un aryle éventuellement substitué ou un hétérocyclyle éventuellement substitué; R(1), R(2) et R(3), représentent indépendamment un atome d'hydrogène, un alkyle C(1)-C(3) ou un phényle; R(4) représente un atome d'hydrogène, un alkyle C(1)-(5) éventuellement substitué, un groupe hydroxyle substitué ou un groupe sulfonyle substitué.

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