Benzocycloheptaisoquinoline derivatives
AssigneeAyerst McKenna and Harrison Ltd.
InventorsFrancois T. Bruderlein, Leslie G. Humber
Life of this patent
Estimating the term…
Abstract
Octahydrobenzo[6,7]-(or [5,6]-)cyclohepta-[1,2,3-de]pyrido-(or pyrrolo-)[2,1-a]isoquinolines, and decahydrobenzo[6,7]-(or[5,6]-)cyclohepta[1,2,3-de]-azepino[2,1-a]isoquinol ines and derivatives thereof, optionally substituted on the pyrrolidine, piperidine or azepine ring. The compounds are useful CNS depressants, anticonvulsant and antiinflammatory agents, and methods for their preparation and use are also disclosed.
Claims66
A compound selected from those of the formulae ##STR63## in which R.sup.1 is selected from the group which consists of hydrogen and lower alkyl containing from 1-6 carbon atoms in a straight chain and up to 4 carbon atoms in a branched chain, and Alk represents ##STR64## in which R.sup.12, R.sup.13, R.sup.14, R.sup.15 and R.sup.16 are each the same or different radicals selected from the group which consists of hydrogen and lower alkyl containing from 1-6 carbon atoms in a straight chain and up to 4 carbon atoms in a branched chain, with the proviso that the carbon atom to which R.sup.12 and R.sup.13 are attached is bonded to the nitrogen atom of said compound;
- L represents hydroxyl or lower alkanoyloxy containing from 2-10 carbon atoms in a straight chain or from 4-6 carbon atoms in a branched chain;
- and M is selected from the group which consists of hydrogen, lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl containing from three to six carbon atoms or cycloalkyl substituted with lower alkyl;
- phenyl or phenyl substituted with lower alkyl, lower alkoxy, halo, or trihalomethyl;
- benzyl, furyl, thienyl, or pyridyl;
- and their acid addition salts with pharmaceutically acceptable acids.
A compound of the formula lb ##STR65## in which R.sup.12, R.sup.13, R.sup.14, R.sup.15 and R.sup.16 are each the same or different radicals selected from the group which consists of hydrogen and lower alkyl;
- L represents hydroxyl or lower alkanoyloxy containing from 2-10 carbon atoms in a straight chain or from 4-6 carbon atoms in a branched chain;
- and M is selected from the group which consists of lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl containing 3-6 carbon atoms or cycloalkyl substituted with lower alkyl;
- phenyl or phenyl substituted with lower alkyl, lower alkoxy, halo, or trihalomethyl;
- benzyl, furyl, thienyl, or pyridyl;
- with the proviso that the hydroxyl or lower alkanoyloxy group is trans to the hydrogen atom in position 15b;
- and their acid addition salts with pharmaceutically acceptable acids.
Dependencies are inferred from the claim text.