Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is an N-heterocyclic group as defined herein and Y can be --NH--, --O-- or --CH.sub.2 --, are disclosed. These compounds are inhibitors of renin and therefore useful as cardiovascular agents.
Abstract: In accordance with the present invention, a controlled release formulation is provided from which a drug, selected from the group consisting of angiotensin converting enzyme inhibitors and ascorbic acid, is released at a substantially controlled rate. The controlled release formulation of the invention is comprised of a reactive matrix of from about 5 to about 80 percent by weight of the drug in combination with from about 5 to about 70 percent by weight of poly[(1.fwdarw.4)-2-amino-2-deoxy-.beta.-D-glucose] (also referred to as chitosan herein). Further in accordance with the present invention there is provided a gel-like complex formed of the drug and the chitosan in environments ranging from neutral to acidic.
Abstract: A compound of the formula ##STR1## wherein R.sub.1 is hydrogen, hydroxy, alkoxy or aryloxy; R.sub.2 is hydrogen, hydroxy, alkoxy or aryloxy; or wherein R.sub.1 and R.sub.2 taken together is an aromatic ring; R.sub.3 is hydrogen or lower alkyl; R.sub.4 is lower alkyl, substituted alkyl, alkenyl or alkynyl; X is amino, alkylamino, alkanoylamino, oxygen or a single bond; A is CH.sub.2 --CH.dbd.CH or a single bond; and n is an integer from 0 to 9, with the proviso that when A is a single bond, n is an integer from 1 to 9 including all stereoisomers thereof.These new compounds have been found to simultaneously inhibit the arachidonic acid enzymes 5-lipoxygenase and cyclooxygenase and as such are useful, for example, as antiinflammatory agents.
Abstract: 7-Oxabicyclo(2.2.1)heptane-based N-hydroxy-N-alkyl (or aryl) ureas, carbamic acids and carbamothioic acids are disclosed having the general formula ##STR1## wherein R.sub.1 is hydrogen, lower alkyl, alkenyl, aryl or aralkyl; R.sub.2 is hydrogen, lower alkyl, aralkyl, alkanoyl or aroyl; R.sub.3 is lower alkyl, alkenyl or alkynyl; A is --CH.sub.2 --CH.dbd.CH-- or a single bond; X is oxygen, sulfur or NH; n is an integer from 1 to 8; and all stereoisomers thereof.These new compounds have been found to simultaneously inhibit the enzymes arachidonic acid cyclooxygenase and arachidonic acid 5-lipoxygenase and are therefore useful as antiinflammatory, antiasthma and antipsoriatic agents.
Type:
Grant
Filed:
September 23, 1986
Date of Patent:
September 22, 1987
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Ravi K. Varma, Sam T. Chao, Eric M. Gordon