Decahydro-8h-isoquino[2,1-g][1,6]naphthyridine and...

C - Chemistry – Metallurgy – 07 – D

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C07D 471/14 (2006.01) A61K 31/47 (2006.01) C07D 491/22 (2006.01)

Patent

CA 2074038

ABSTRACT OF THE DISCLOSURE Compounds of the formula Image (1) wherein: X and Y are independently hydrogen; hydroxy; lower alkyl of 1-6 carbon atoms; lower alkoxy of 1-6 carbon atoms; or halo; or X and Y when adjacent and taken together are methylenedioxy or ethylene-1,2-dioxy; R is lower alkyl of 1-6 carbon atoms; cycloalkyl of 3-8 carbon atoms; phenyl or phenyl lower alkyl in which any phenyl group may be optionally substituted by one or two substituents chosen from the group consisting of halo, lower alkyl of 1-4 carbon atoms and lower alkoxy of 1-4 carbon atoms; or -ANHSO2R1; wherein A is lower alkylene of 1-6 carbon atoms; and R1 is lower alkyl of 1-6 carbon atoms or -NR2R3; wherein R2 and R3 are independently hydrogen or lower alkyl of 1-6 carbon atoms, or R2 and R3 taken together are cycloalkyl of 3-8 carbon atoms; and n is 1 or 2; and the pharmaceutically acceptable salts thereof, are useful as .alpha.2-adrenoceptor antagonists, in particular as peripherally selective .alpha.2-adrenoceptor antagonists.

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