Sulfonyl-decahydro-8H-isoquino[2,1-G][1,6]-naphthyridines and related compounds useful as .alpha..sub.2 -blockers
AssigneeSyntex (U.S.A.) Inc.
InventorRobin D. Clark
Life of this patent
Estimating the term…
Abstract
Compounds of formulas (1) and (2): ##STR1## in which: X and Y are independently hydrogen, hydroxy, lower alkyl, lower alkoxy or halo, or X and Y taken together is methylenendioxy or ethylene-1,2-dioxy, and R is lower alkyl, optionally substituted phenyl, --(CH.sub.2).sub.m OR.sup.1 or --NR.sup.1 R.sup.2 wherein m is an integer of 1 to 6 and R.sup.1 and R.sup.2 are independently hydrogen or lower alkyl, or --NR.sup.1 R.sup.2 taken together is a heterocycle of the formula: ##STR2## wherein A is --CH.sub.2 --, --NR.sup.1 -- or oxygen, or a pharmaceutically acceptable salt thereof, are useful as .alpha..sub.2 -blockers, especially as antidepressants.
Claims28
A compound of the formula (1) or (2):
- ##STR13## in which:
- X and Y are independently hydrogen, hydroxy, lower alkyl of one to six carbon atoms, lower alkoxy of one to six carbon atoms or halo, or X and Y taken together is methylenedioxy or ethylene-1,2-dioxy;
- and
- R is lower alkyl of one to six carbon atoms, phenyl optionally substituted by one or two substituents chosen from halo or nitro groups or lower alkyl or lower alkoxy groups of one to four carbon atoms, --(CH.sub.2).sub.m OR.sup.1 or --NR.sup.1 R.sup.2 wherein m is an integer of 1 to 6 and R.sup.1 and R.sup.2 are independently hydrogen or lower alkyl, or --NR.sup.1 R.sup.2 taken together is a heterocycle of the formula:
- ##STR14## wherein A is --CH.sub.2 --,--NR.sup.1 -- or oxygen;
- or a pharmaceutically acceptable salt thereof.
A composition suitable for administration to a mammal having a disease-state which is alleviated by treatment with an .alpha..sub.2 -blocker, which composition comprises a pharmaceutically acceptable non-toxic carrier and a therapeutically effective amount of a compound of the formula ##STR15## in which:
- X and Y are independently hydrogen, hydroxy, lower alkyl of one to six carbon atoms, lower alkoxy of one to six carbon atoms or halo, or X and Y taken together is methylenedioxy or ethylene-1,2-dioxy;
- and
- R is lower alkyl of one to six carbon atoms, phenyl optionally substituted by one or two substituents chosen from halo or nitro groups or lower alkyl or lower alkoxy groups of one to four carbon atoms, --(CH.sub.2).sub.m OR.sup.1 or and R.sup.1 and R.sup.2 are independently hydrogen or lower alkyl, or --NR.sup.1 R.sup.2 taken together is a heterocycle of the formula:
- ##STR16## wherein A is --CH.sub.2 --, --NR.sup.1 -- or oxygen;
- or a pharmaceutically acceptable salt thereof, in admixture with one or more pharmaceutically acceptable carriers.
A method for treating a mammal having a disease-state which is alleviated by treatment with an .alpha..sub.2 -blocker, which comprises administering a therapeutically effective amount of a compound of the formula ##STR17## in which:
- X and Y are independently hydrogen, hydroxy, lower alkyl of one to six carbon atoms, lower alkoxy of one to six carbon atoms or halo, or X and Y taken together is methylenedioxy or ethylene-1,2-dioxy;
- and
- R is lower alkyl of one to six carbon atoms, phenyl optionally substituted by one or two substituents chosen from halo or nitro groups or lower alkyl or lower alkoxy groups of one to four carbon atoms, --(CH.sub.2).sub.m OR.sup.1 or --NR.sup.1 R.sup.2 wherein m is an integer of 1 to 6 and R.sup.1 and R.sup.2 are independently hydrogen or lower alkyl, or --NR.sup.1 R.sup.2 taken together is a heterocycle of the formula:
- ##STR18## wherein A is --CH.sub.2 --, --NR.sup.1 -- or oxygen;
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.