Piperazine derivatives as .alpha.1a-adrenergic receptor...

Details Piperazine derivatives as .alpha.1a-adrenergic receptor... Piperazine derivatives as .alpha.1a-adrenergic receptor...

C - Chemistry, Metallurgy

07

D

C07D 295/04 (2006.01) A61K 31/495 (2006.01) A61K 31/675 (2006.01) C07D 295/088 (2006.01) C07D 295/13 (2006.01) C07F 9/6509 (2006.01)

Patent

CA 2168443

There are disclosed compounds of general formula (I). Y is a linking group, chosen from a wide range, but including -COO-, - CH2COO-, -CONH-, -CON(CH3)-, -CH2CONH-, -SO2NH-, -SO2N(CH3)- and -PO(OC2H5)NH-. W is an alkylene chain A is a substituted phenyl group or a benzofuran or benzodioxan group. R and R1 may have many values, but R is L preferably a bulky group. These compounds and their prodrugs, enantiomers, diastereoisomers, N-oxides and pharmaceutically acceptable salts block .alpha.1A-adrebergic receptors and are thus useful for the prevention of contractions of the prostate, urethra and lower urinary tract, without affecting blood pressure.

Composés répondant à la formule générale (I), dans laquelle Y représente un groupe de liaison, choisi dans une large gamme, mais comprenant -COO-, -CH2COO-, -CONH-, -CON(CH3)-, -CH2CONH-, SO2NH-, -SO2N(CH3)- et -PO(OC2H5)NH-; W représente une chaîne alkylène; A représente un groupe phénylique substitué ou un groupe benzofurane ou benzodioxane; et R et R1 peuvent avoir plusieurs valeurs, mais R est de préférence un groupe volumineux. Ces composés et leurs promédicaments, énantiomères, diastéréoisomères, N-oxydes et leurs sels pharmaceutiquement acceptables bloquent les récepteurs alpha 1a-adrénergiques et sont de ce fait utilisables dans la prophylaxie des contractions de la prostate, de l'urètre et de la partie inférieure du tractus urinaire, et ce sans intervenir sur la tension artérielle.

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