Abstract: Disclosed are 4,5.alpha.-epoxy-3-hydroxy or methoxy-7-(1-hydroxyalkyl or 1-oxoalkyl)morphinan-6-one compounds characterized by the structural formulae: ##STR1## In the foregoing formulae R is methyl, cyclopropylmethyl, cyclobutylmethyl, propargyl, allyl, dimethylallyl, cis-chloroallyl or furfuryl; R.sub.1 is H or methyl; R.sub.2 is straight or branched chain alkyl of from 1 to 10 carbon atoms, aryl, substituted aryl or arylalkyl, in which the alkyl group contains from 1 to 6 carbon atoms, and R.sub.3 is a straight chain alkyl of 1 to 4 carbon atoms.
Type:
Grant
Filed:
December 10, 1980
Date of Patent:
August 31, 1982
Assignee:
SISA, Incorporated
Inventors:
James E. Quick, Raj K. Razdan, Haldean C. Dalzell
Abstract: Disclosed are 14-methoxy substituted 3-hydroxy or 3-methoxy -6-one morphinans characterized by the structural formula: ##STR1## wherein R is H or methyl; R.sub.1 is H, .alpha. methyl or .beta. methyl; and R.sub.2 is cyclobutylmethyl, cyclopropylmethyl, tetrahydrofurfuryl or dimethylallyl. The compounds of the present invention are variously useful as analgesics, narcotic antagonists and mixed analgesics/narcotic antagonists.
Abstract: Disclosed is 17-cyclopropylmethyl-14-hydroxy-3-methoxymorphinan-6-one. This compound is a mixed agonist (analgesic)/narcotic antagonist and therefore useful for the treatment of moderate to severe pain without the liability of inducing physical dependence.
Abstract: Disclosed is 17-cyclobutylmethyl-4,5.alpha.-epoxy-3-hydroxy-14-methoxy-8.alpha.-methylm orphinan-6-one characterized by the formula: ##STR1## This compound is useful as a mixed analgesic/narcotic antagonist.
Abstract: Tetrahydrodibenzopyrans having the structure ##STR1## in which R, R.sub.1, and R.sub.2 are alkyl having from 1 to 4 carbon atoms and ophthalmologically acceptable acid addition salts thereof are effective anti-glaucoma agents, free from all but a very small amount of CNS activity, when applied topically.
Type:
Grant
Filed:
January 27, 1977
Date of Patent:
November 21, 1978
Assignee:
SISA Incorporated
Inventors:
Raj K. Razdan, Haldean C. Dalzell, Harry G. Pars
Abstract: Tetrahydrodibenzopyrans having the structure ##STR1## in which R.sub.1 is hydrogen or acetyl and R.sub.2 is alkyl having from 1 to 4 carbon atoms are effective anti-glaucoma agents, free from all but a very small amount of CNS activity, when applied topically.
Type:
Grant
Filed:
January 27, 1977
Date of Patent:
November 21, 1978
Assignee:
SISA Incorporated
Inventors:
Raj K. Razdan, Haldean C. Dalzell, Barbara Z. Terris, Harry G. Pars