Abstract: The use of lofexidine and its pharmaceutically acceptable salts in alleviating the adverse symptoms of drug withdrawal, pre-menstrual tension and peri-menopausal flushing is disclosed.
Abstract: This invention relates to a new class of compounds having important biochemical and pharmacological properties. More particularly, this invention relates to N-aralkyl piperidinemethanol derivatives which are potent and selective inhibitors of the binding of serotonin at the 5HT.sub.2 receptor site, and to the processes for their preparation and use.
Abstract: The present invention concerns a new antibiotic substance denominated antibiotic A 40926 mannosyl aglycon and the addition salts thereof, a process for preparing it from antibiotic A 40926 complex or a factor thereof, and its use in the treatment of infectious disease involving microorganisms susceptible to it.
Type:
Grant
Filed:
December 23, 1986
Date of Patent:
November 1, 1988
Assignee:
Gruppo Lepetit S.p.A.
Inventors:
Enrico Selva, Beth P. Goldstein, Pietro Ferrari, Giovanni Cassani, Francesco Parenti
Abstract: This invention relates to aryloxycycloalkanolaminoalkylene aryl ketones to the processes for their preparation and to their use as antihypertensive agents.
Type:
Grant
Filed:
April 17, 1984
Date of Patent:
May 17, 1988
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Michael E. LeTourneau, James R. McCarthy, Donald L. Trepanier
Abstract: This invention relates to novel .beta.-methylenefuranethanamines which are mechanism-based inhibitors of dopamine beta-hydroxylase useful as antihypertensive agents.
Type:
Grant
Filed:
June 6, 1986
Date of Patent:
October 27, 1987
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Thomas M. Bargar, Robert Broersma, Jr., James R. McCarthy
Abstract: Fluoroallylamine derivatives of the following Formula I are novel MAO-inhibitors and at low dose levels selectively inhibit MAO-B: ##STR1## wherein: R.sub.1 and R.sub.2 independently represent hydrogen, chlorine or fluroine;R.sub.3 represents hydrogen or (C.sub.1 -C.sub.4)alkyl; andX represents oxygen or sulfur.They are useful for the treatment of depression and, co-administered with L-dopa, in the treatment of Parkinsonism.
Abstract: The use of lofexidine and its pharmaceutically acceptable salts in alleviating the adverse symptoms of drug withdrawal, pre-menstrual tension and peri-menopausal flushing is disclosed.
Abstract: This application relates to a stereospecific process for preparing specific enantiomers of 4-amino-4,5-dihydro-2-furancarboxylic acid and C.sub.1-6 lower alkyl esters thereof. These compounds are .gamma.-aminobutyric acid transaminase inhibitors useful in the treatment of epilepsy.
Abstract: Migraine is treated with a tropyl benzoate derivative of the following general formula: ##STR1## wherein: R.sub.1 represents C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy or halogen;R.sub.2 represents hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy or halogen; andR.sub.3 represents hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy or halogen, provided that R.sub.3 is hydrogen when R.sub.2 is hydrogen, or a pharmaceutically acceptable salt thereof.Additionally, some novel tropyl benzoate derivatives are disclosed.
Abstract: Novel 5-acyl-2-(1H)pyridinones and their use as cardiotonic agents. Typical of the compounds is 5-acetyl-1,2-dihydro-6-methyl-2-oxo-3-pyridinecarbonitrile which is prepared by condensing anionic cyano acetamide with 3-[(dimethylamino)methylenyl]-2,4-pentanedione in an inert organic solvent.
Type:
Grant
Filed:
April 29, 1983
Date of Patent:
February 4, 1986
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Winton D. Jones, Richard C. Dage, Richard A. Schnettler
Abstract: Migraine is treated with a tropyl benzoate derivative of the following general formula: ##STR1## wherein: R.sub.1 represents C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy or halogen;R.sub.2 represents hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy or halogen; andR.sub.3 represents hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy or halogen, provided that R.sub.3 is hydrogen when R.sub.2 is hydrogen, or a pharmaceutically acceptable salt thereof.Additionally, some novel tropyl benzoate derivatives are disclosed.
Abstract: Novel halomethyl derivatives of .alpha.-amino acids of the following general structure: ##STR1## wherein Y is F.sub.2 CH--, F.sub.3 C--, Cl.sub.2 CH--; Z is .beta.-methylthioethyl, .beta.-thioethyl, .beta.-benzylthioethyl; S-(5'-desoxyadenosin-5'-yl)-S-methylthioethyl, .gamma.-guanidinopropyl, R.sub.a HN(CH.sub.2).sub.n -- wherein n is the integer 3 or 4 or ##STR2## wherein Y.sub.2 is F.sub.2 CH--, or F.sub.3 C--; each of R.sub.a and R.sub.b can be the same or different and 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 ##STR3## 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.
Abstract: This invention relates to certain substituted aroylimidazolones, their acid and base addition salts thereof, and to their use as cardiotonic agents.
Abstract: 1. A compound of the formula:H.sub.2 C.dbd.C.dbd.CHCH.sub.2 NHCH.sub.2 --Z--CH.sub.2 NHRwherein:Z is --CH.sub.2 CH.sub.2 -- or trans-CH.dbd.CH--,R is H, CH.sub.3 --, CH.sub.3 CH.sub.2, CH.sub.3 (CH.sub.2).sub.2 --, --(CH.sub.2).sub.3 NH.sub.2, --(CH.sub.2).sub.3 NHCOCH.sub.3, --CH.sub.2 CH.dbd.CH.sub.2, or --CH.sub.2 CH.dbd.C.dbd.CH.sub.2,or a pharmaceutically acceptable acid addition salt thereof are inhibitors of polyamine oxidase.