Abstract: Aryloxyalkanol derivatives having the formulaAr--O(CH.sub.2).sub.n OHwherein n is an integer from 3 to 8 and Ar is (1) 1- or 2-naphthylenyl, (2) phenyl optionally substituted by from 1 to 3 C.sub.1-4 lower alkyl groups, or (3) a diphenyl moiety of structure ##STR1## wherein Y is a bond, CH.sub.2 or CH.sub.2 O, and esters thereof have antiretrovirus activity and are effective in a method for treating a retrovirus infection.
Abstract: This invention relates to derivatives of 3-aryl-5-alkylthio-4H-1,2,4-triazoles, to their pharmacological properties and to their use as muscle relaxants, spasmolytics, anticonvulsants and anxiolytics.
Abstract: This invention relates to an improvement in a process for making 2,6-di-tertiarybutyl-4-mercaptophenol and 4,4'-isopropylidenedithio-bis-(2,6-di-tertiarybutylphenol), which is effected by carrying out an electrocatalytic reduction of bis(3,5-di-tertiarybutyl-4-hydroxyphenol)polysulfide at a lead cathode in an acidic electrolyte medium.
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.
Abstract: The present invention is directed to new 16-methoxy-16-methyl prostaglandin E.sub.1 derivatives of the following general formula ##STR1## wherein R stands for a (C.sub.1-4) alkyl group or a non-toxic pharmaceutically acceptable cation, to a process for preparing them and to their use as gastroprotective agents.
Abstract: Improved cellulose semipermeable hollow fibers useful in detoxifying blood during hemodialysis or hemofiltration treatments. The cellulose fibers are fine, capillary fibers that are made by melt extrusion of certain cellulose ester polyol melt spin compositions into self-supporting gelled fibers. The cellulose ester gelled fibers are subsequently chemically converted into cellulose fibers by deacetylation, in aqueous alkali solution. The product fibers exhibit improved wet intrinsic tensile strength and higher water permeability characteristics than heretofore known cellulose fibers made from cellulose ester spin compositions.The invention includes the method of making the improved fibers and separatory cells such as hemodialyzers or hemofilters which contain the improved fibers in a gamma ray sterilized condition.
Abstract: The invention refers to an individual antibiotic substance selected from the group consisting of Teichomycin A.sub.2 factor 1, Teichomycin A.sub.2 factor 2, Teichomycin A.sub.2 factor 3, Teichomycin A.sub.2 factor 4 and Teichomycin A.sub.2 factor 5 in substantially pure form, and to the method of producing them by recovery from Teichomycin A.sub.2, a known antibiotic substance, by means of high-efficiency chromatographic methods. The single pure Teichomycin A.sub.2 factor 1, Teichomycin A.sub.2 factor 2, Teichomycin A.sub.2 factor 3, Teichomycin A.sub.2 factor 4 and Teichomycin A.sub.2 factor 5 are biologically distinguishable from Teichomycin A.sub.2 in that they have a higher degree of antibiotic activity against susceptible microorganisms.
Type:
Grant
Filed:
June 7, 1983
Date of Patent:
September 17, 1985
Assignee:
Gruppo Lepetit S.p.A.
Inventors:
Angelo Borghi, Rosa Pallanza, Carolina Coronelli, Giovanni Cassani
Abstract: Glycine, sarcosine, or N,N-dimethylglycine exerts a synergistic effect upon gamma-vinyl GABA for the treatment of seizure disorders, in particular epilepsy.
Abstract: N-(3-Dialkylamino-2-propenylidene)-N-alkylalkanaminium salts substituted in the 2-position with an ether or thioether and having the formula ##STR1## are active as hypoglycemic agents.
Type:
Grant
Filed:
May 16, 1983
Date of Patent:
August 6, 1985
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Eugene R. Wagner, Charlotte L. Barney, Donald P. Matthews
Abstract: Improved procedures and intermediates for synthesizing 11-deoxyprostaglandins wherein trans-2,3-dicarbomethoxycyclopentanone is subjected to a novel alcoholysis with .beta.,.beta.,.beta.-trichloroethanol to substitute a .beta.,.beta.,62 -trichlorocarboethoxy group at the 2-position followed by alkylation to allow for a wide range of upper side chains to be introduced at the 2-position of the cyclopentanone ring. The unwanted .beta.,.beta.,.beta.-trichlorocarboethoxy group at the 2-position can then be removed easily by a zinc induced elimination-decarboxylation sequence. Base catalyzed epimerization of the 2-position side chain to the desired trans-configuration, relative to the carbomethoxy group in the 3-position, is followed by partial reduction of the 2-hexynyl moiety of the side chain to the desired cis-olefinic group of the E.sub.2 -type 11-dioxyprostaglandins, or through total reduction to the alkane upper side chain of E.sub.1 -type-prostaglandin analogs.
Abstract: Novel 1,4-dihydropyridine derivatives have the following general Formula: ##STR1## and are calcium antagonists, useful for treating cardiovascular diseases.
Abstract: 3,6,7,8-Substituted-s-triazolo-pyridazine compounds such as 7,8-dimethyl-6-morpholino-3-methyl-s-triazolo[4,3-b]pyridazine or 7,8-dimethyl-6-(1-pyrrolidinyl)-3-(isopropyl)-s-triazolo-[4,3-b]pyridazine are prepared by the reaction of a carboxylic acid with a substituted 3-hydrazino-6-halo-pyridazine followed by the reaction of the resulting 6-halotriazolopyridazine with a corresponding base. The compounds have pharmacological activity as bronchodilators.
Abstract: 1,3-Dihydro-2H-imidazol-2-ones having 5-acyl and 4-oxymethyl substituents, are useful as cardiotonics, antihypertensives and antithrombotic agents. The compounds are obtained by the reaction of an appropriate alcohol or a silver salt with a substituted 4-bromomethyl-1,3-dihydro-2H-imidazol-2-one.
Type:
Grant
Filed:
April 29, 1983
Date of Patent:
July 2, 1985
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
J. Martin Grisar, Richard A. Schnettler, Richard C. Dage
Abstract: Alkoxycarbonyl and oxalyl derivatives of amino-N-(1H-tetrazol-5-yl)benzamides are described herein. The compounds involved are useful as antiallergic agents. These compounds can be prepared by the reaction of an amino-N-(1H-tetrazol-5-yl)benzamide with an appropriate acid chloride.
Abstract: This application relates to 4-amino-4,5-dihydro-2-furancarboxylic acid, and esters thereof, useful as .gamma.-aminobutyric acid transaminase inhibitors.
Abstract: Novel compounds of the following general formula are useful pharmacologic agents: ##STR1## R is .[.selected from.]. hydrogen.[., alkylcarbonyl wherein the alkyl moiety contains from 1 to 4 carbon atoms, alkoxycarbonyl wherein the alkoxy moiety contains from 1 to 4 carbon atoms and may be straight or branched, and ##STR2## wherein R.sub.10 is selected from hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl and p-hydroxybenzyl.].; R.sub.2 is .[.selected from.]. hydroxy.[., a straight or branched alkoxy group of from 1 to 8 carbon atoms, a lower alkylamino group wherein the alkyl moiety contains from 1 to 4 carbon atoms, and ##STR3## wherein R.sub.4 is selected from hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl, and p-hydroxybenzyl.].; R.sub.3 is .[.selected from.]. hydrogen.[., chlorine, bromine, and iodine.].; [A] is .[.selected from.]. ##STR4## .[.and --CH.dbd.CH--.]. wherein R.sub.1 is .[.selected from.]. hydrogen.[.