N-[1,2,3,4,6,7,12,12 .alpha.-octahydro-2H-indolo(2,3.alpha.)-quinolizinyl-2.beta.-yl]alkane and benzyl sulfonamides and anti-hypertensive use thereof
AssigneeJohn Wyeth & Brother Limited
InventorAlbert Opalko
Life of this patent
Estimating the term…
Abstract
Indoloquinolizines of the formula (I) ##STR1## and their pharmaceutically acceptable acid addition salts [wherein R.sup.1 represents hydrogen, lower alkyl or lower aralkyl, R.sup.2 and R.sup.3 each represent hydrogen, halogen, lower alkoxy or lower alkyl, R.sup.4 represents hydrogen, halogen or lower alkyl and R.sup.5 represents lower alkyl or aryl] possess antihypertensive activity.
Claims5
A compound of the formula:
- ##STR7## in which R.sup.1 is hydrogen, alkyl of 1 to 6 carbon atoms or aralkyl of 7 to 10 carbon atoms;
- R.sup.2 and R.sup.3, independently, are hydrogen, halogen, alkoxy of 1 to 6 carbon atoms or alkyl of 1 to 6 carbon atoms with the proviso that when R.sup.2 and R.sup.3 are tertiary alkyl groups they are on nonadjacent carbon atoms;
- R.sup.4 is hydrogen, halogen or alkyl of 1 to 6 carbon atoms;
- R.sup.5 is alkyl of 1 to 6 carbon atoms, phenyl or substituted phenyl in which the substituent is halogen, alkoxy of 1 to 6 carbon atoms, alkyl of 1 to 6 carbon atoms, alkylenedioxy of 1 to 6 carbon atoms, amino, alkylamino of 1 to 6 carbon atoms, dialkylamino of 2 to 12 carbon atoms or trifluoromethyl;
- or a pharmaceutically acceptable acid addition salt thereof.
A pharmaceutical composition having antihypertensive activity comprising a compound selected from the group consisting of an indoloquinolizine of the formula:
- ##STR8## or a pharmaceutically acceptable acid addition salt thereof, wherein R.sup.1 is hydrogen, alkyl of 1 to 6 carbon atoms or aralkyl of 7 to 10 carbon atoms;
- R.sup.2 and R.sup.3, independently, are hydrogen, halogen, alkoxy of 1 to 6 carbon atoms or alkyl of 1 to 6 carbon atoms with the proviso that when R.sup.2 and R.sup.3 are tertiary alkyl groups they are on nonadjacent carbon atoms;
- R.sup.4 is hydrogen, halogen or alkyl of 1 to 6 carbon atoms;
- R.sup.5 is alkyl of 1 to 6 carbon atoms, phenyl or substituted phenyl in which the substituent is halogen, alkoxy of 1 to 6 carbon atoms, alkyl of 1 to 6 carbon atoms, alkylenedioxy of 1 to 6 carbon atoms, amino, alkylamino of 1 to 6 carbon atoms, dialkylamino of 2 to 12 carbon atoms or trifluoromethyl;
- and a pharmaceutically acceptable carrier.
A method of treating hypertension in a mammal which comprises administering to said mammal an antihypertensively effective amount of a compound selected from the group consisting of an indoloquinolizine of the formula ##STR9## or a pharmaceutically acceptable acid addition salt thereof, wherein R.sup.1 is hydrogen, alkyl of 1 to 6 carbon atoms or aralkyl of 7 to 10 carbon atoms;
- R.sup.2 and R.sup.3, independently, are hydrogen, halogen, alkoxy of 1 to 6 carbon atoms or alkyl of 1 to 6 carbon atoms with the proviso that when R.sup.2 and R.sup.3 are tertiary alkyl groups they are on nonadjacent carbon atoms;
- R.sup.4 is hydrogen, halogen or alkyl of 1 to 6 carbon atoms;
- R.sup.5 is alkyl of 1 to 6 carbon atoms, phenyl or substituted phenyl in which the substituent is halogen, alkoxy of 1 to 6 carbon atoms, alkyl of 1 to 6 carbon atoms, alkylenedioxy of 1 to 6 carbon atoms, amino, alkylamino of 1 to 6 carbon atoms, dialkylamino of 2 to 12 carbon atoms or trifluoromethyl.
Dependencies are inferred from the claim text.