Receptor antagonist

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 487/04 (2006.01) A61K 31/519 (2006.01) A61P 25/16 (2006.01) C07D 487/14 (2006.01)

Patent

CA 2430328

[In the formula, p is an integer of 1 to 3; R1 represents a heterocyclic group, etc.; R2 represents -N(-R4)(-R5) (wherein R4 and R5 are the same or different and each represents hydrogen, aralkyl, etc. or R4 and R5 in cooperation with the adjacent nitrogen atom form a heterocyclic group), etc.; and Q represents -N=C(-R7)- (wherein R7 represents substituted amino, etc.), etc.] An adrenergic .alpha.2C receptor antagonist which contains as an active ingredient a fused-ring pyrimidine derivative represented by the general formula (I) or a pharmacologically acceptable salt of the derivative is provided. The antagonist is useful in treatments for and/or prevention of various diseases attributable to the hyperenergia of an adrenergic .alpha.2C receptor.

Selon l'invention, [dans la formule (I), p est un nombre entier compris entre 1 et 3 ; R?1¿ désigne un groupe hétérocyclique, etc. ; R?2¿ désigne N(-R?4¿)(-R?5¿) (R?4¿ et R?5¿ étant identiques ou différents et désignant dans chaque cas hydrogène, aralkyle, etc. ou R?4¿ et R?5¿ forment un groupe hétérocyclique conjointement avec l'atome d'azote adjacent), etc. ; et Q désigne N=C(-R?7¿)- (R?7¿ désignant amino substitué, etc.), etc.] L'invention concerne un antagoniste de récepteur adrénergique .alpha.¿2C?, qui contient comme principe actif, un dérivé de pyrimidine à anneaux condensés, représenté par la formule générale (I) ou un sel pharmaceutiquement acceptable dudit dérivé. L'antagoniste s'utilise pour assurer le traitement et/ou la prévention de diverses pathologies imputables à l'hyperénergie d'un récepteur adrénergique .alpha.¿2C?.

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