Berban derivatives as a -adrenergic antagonists

C - Chemistry – Metallurgy – 07 – D

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C07D 455/04 (2006.01) A61K 31/435 (2006.01) C07D 455/03 (2006.01) C07D 491/153 (2006.01)

Patent

CA 1294964

ABSTRACT The invention relates to novel racemic or optioally active berban derivatives of the general formula (I), wherein R1 and R2 represent independently from the other a hydroxyl, straight or branched chain alkoxy group having 1 to 6 carbon atorns or R1 and R2 together represent a C1-3 alkylenedioxy group; R3 and R4 represent independently from the other hydrogen, straight or branched chain alkyl group, having 1 to 4 oarbon atoms and optionally substituted by hydroxyl group, or a C2-6 alkoxycarbonyl or cyano group; and R5 represents hydrogen, straight or branched chain alkyl group having 1 to 6 carbon atoms, C1-7 aliphatic or aromatic acyl group or C1-7 alkylsulphonyl or aryl- sulphonyl group and a salt thereof, to pharmaceutical compositions oontalning them, to the use as well as to process for preparing the novel compounds. The compounds of the general formula (I) are selective .alpha.2-adrenergic receptor-blocking substances and thus, they may be used for the treatment of depressive illnesses.

509814

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