Abstract: Derivatives of 5-[2-[(2,3-dihydro-1,4-benzodioxan-2-ylmethyl)amino]-1-hydroxyethyl]-2-hyd roxybenzoic acid are prepared which are useful for their blocking action on .alpha. and .beta.-adrenergic receptors. In addition, these compounds are useful as antihypertensive agents.
Abstract: Derivatives of 2-hydroxy-5-[1-hydroxy-2-[4-(2-oxo-1-benzimidazolinyl)piperidino]ethyl]ben zoic acid are prepared which are useful for their blocking action on .alpha. and .beta.-adrenergic receptors. In addition, these compounds are useful for their spasmolytic and anti-hypertensive activity.
Abstract: Compounds of the following general structure are useful as antirhinovirus agents: ##STR1## wherein Y is a bond, oxygen or divalent sulfur; R is a straight or branched hydrocarbon chain having from 6 to 20 carbon atoms and is saturated or unsaturated having from 1 to 4 double bonds when R has from 10 to 20 carbon atoms and 1 or 2 double bonds when R has from 6 to 9 carbon atoms; and R.sub.1 is hydrogen or a straight or branched alkyl group of from 1 to 4 carbon atoms.
Abstract: 2-(2,2-Dicyclohexylethyl)piperidine is prepared via the catalytic hydrogenation of 2-(2,2-diphenylethenyl)pyridine in a single step. High yields are obtained using a rhodium supported catalyst.
Type:
Grant
Filed:
April 14, 1976
Date of Patent:
March 4, 1980
Assignee:
Richardson-Merrell Inc.
Inventors:
Stephen W. Horgan, Frank P. Palopoli, David L. Wenstrup
Abstract: Novel acetylenic derivatives of .alpha.-amino acids of the following general structure: ##STR1## wherein n is an integer of from 1 to 3; R is hydrogen, alkylcarbonyl wherein the alkyl moiety has from 1 to 4 carbon atoms and is straight or branched, alkoxycarbonyl wherein the alkoxy moiety has from 1 to 4 carbon atoms and is straight or branched, or ##STR2## wherein R.sub.2 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or .rho.-hydroxybenzyl; each R.sub.1 is the same and is hydroxy, a straight or branched alkoxy group of from 1 to 8 carbon atoms, --NR.sub.3 R.sub.4 wherein each of R.sub.3 and R.sub.4 is hydrogen or a lower alkyl group of from 1 to 4 carbon atoms and can be the same or different, or ##STR3## wherein R.sub.5 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or .rho.-hydroxybenzyl; and the lactams thereof when n is 2 or 3; and pharmaceutically acceptable salts and individual optical isomers thereof.
Abstract: Therapeutic antihypertensive compositions containing 2-[1-(2,6-dichlorophenoxy)ethyl]-4,5-dihydro-1H-imidazole and N-(2-chloroethyl)-N-(1-methyl-2-phenoxyethyl)benzenemethanamine or their non-toxic, pharmaceutically acceptable salts are described as well as a method of reducing blood pressure in mammals.
Abstract: Compounds of the following general formula and salts thereof are irreversible inhibitors of .gamma.-aminobutyric acid transaminase: ##STR1## wherein R.sub.1 is hydrogen, alkylcarbonyl wherein the alkyl moiety has from 1 to 4 carbon atoms and is straight or branched, alkoxycarbonyl wherein the alkoxy moiety has from 1 to 4 carbon atoms and is straight or branched, the radical ##STR2## wherein R.sub.4 is hydrogen, a straight or branched alkyl group having from 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; R.sub.2 is hydroxy, a straight or branched alkoxy group of from 1 to 8 carbon atoms, the group-NR.sub.5 R.sub.6wherein each of R.sub.5 and R.sub.6 is hydrogen or a straight or branched alkyl group having from 1 to 4 carbon atoms, or ##STR3## wherein R.sub.7 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; and R.sub.3 is hydrogen or bromine.
Abstract: Substituted benzaldehydes of the following general structure are useful as hypolipidemic agents: ##STR1## wherein Y is selected from oxygen and divalent sulfur; R is selected from a straight or branched saturated hydrocarbon chain having from 10 to 20 carbon atoms and a straight or branched unsaturated hydrocarbon chain having from 10 to 20 carbon atoms and from 1 to 4 double bonds.
Type:
Grant
Filed:
June 2, 1977
Date of Patent:
February 5, 1980
Assignee:
Richardson-Merrell Inc.
Inventors:
Thomas R. Blohm, J. Martin Grisar, Roger A. Parker
Abstract: Novel compounds of the following general formula ##STR1## and pharmaceutically acceptable salts and individual optical isomers thereof. The compounds are useful as aromatic amine decarboxylase inhibitors.
Abstract: Novel acetylenic derivatives of .alpha.-amino acids of the following general structure: ##STR1## wherein Z is .beta.-methylthioethyl, .beta.-benzylthioethyl, S-(5'-desoxyadenosin-5' -yl)-S-methylthioethyl, .gamma.-guanidinopropyl, or RHN(CH.sub.2).sub.n --; n is the integer 3 or 4; each R is hydrogen, alkylcarbonyl wherein the alkyl moiety has from 1 to 4 carbon atoms and is straight or branched, alkoxycarbonyl wherein the alkoxy moiety has from 1 to 4 carbon atoms and is straight or branched, or ##STR2## wherein R.sub.2 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; R.sub.1 is hydroxy, a straight or branched alkoxy group of from 1 to 8 carbon atoms, --NR.sub.4 R.sub.5 wherein each of R.sub.4 and R.sub.5 is hydrogen or a lower alkyl group of from 1 to 4 carbon atoms, or ##STR3## wherein R.sub.3 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; and the lactams thereof when Z is RHN(CH.sub.
Abstract: Novel compounds useful as antihistamine agents, antiallergy agents, and bronchodilators are represented by the following formula ##STR1## wherein R and R.sup.1 each represent hydrogen; or R and R.sup.1 taken together form a second bond between the carbon atoms bearing R and R.sup.1 ; n is a positive whole integer of from 1 to 3; Y represents --CH.dbd.CH--, or ##STR2## with the proviso that when each of R and R.sup.1 represents hydrogen, Y represents --CH.dbd.CH, and when Y represents --CH.dbd.CH, n is equal to 1 or 2; and Z represents thienyl, phenyl, or substituted phenyl wherein the substituents on the substituted phenyl may be attached at the ortho, meta, or para positions of the phenyl ring and are selected from halogen, a straight or branched lower alkyl chain of from 1 to 4 carbon atoms, a lower alkoxy group of from 1 to 4 carbon atoms, di(lower)-alkylamino, or a saturated monocyclic heterocyclic group such as pyrrolidino, piperidino, morpholino, or N-(lower)-alkylpiperazino.
Abstract: Novel compounds of the following general formula ##STR1## and pharmaceutically acceptable salts and individual optical isomers thereof. The compounds are useful as aromatic amine decarboxylase inhibitors.
Abstract: Novel compounds of the following general formula are useful in the preparation of 4-aminohex-5-enoic acid and 4-aminohex-5-ynoic acid which are useful pharmacological agents: ##STR1## wherein R.sub.1 is hydroxy, amino, or tert-butoxy.