Abstract: A genus of tripeptide amides and fifteen species thereof of Examples 4-18, which are useful as analgesics and/or opiate antagonists, three processes for preparation thereof, pharmaceutical compositions thereof, and the three tripeptide amide species of Examples 1-3, which are not within the genus and are useful as analgesics and/or opiate antagonists, are disclosed.
Abstract: 3-Z-5-(Q-CO)-6-methyl-2(1H)-pyridinones (I) or salts thereof, where Q is 2(or 3)-furanyl or 2(or 3)-thienyl when Z is hydrogen or cyano, or where Q is 4(or 3)-pyridinyl or 4(or 3)-pyridinyl having one or two methyl substituents only when Z is cyano, are useful as cardiotonic agents. Processes for preparing said compounds (I) are shown.
Abstract: Water insoluble, photodynamic insecticidal compositions comprising the free acids of erythrosin B, phloxin B, rose bengal, octabromofluorescein or fluorescein or the aluminum lakes thereof, optionally including a dispersant, aqueous dispersions of the same and a method of combatting adult insects and insect larvae by use of the same.
Abstract: The invention relates to a syringe for extrusion of a semi-plastic, particulate mass comprising a barrel of flexible material having one or more longitudinal slits therein and provided at its upper end with a piston with means for making positive engagement with a plunger rod, the barrel being optionally fitted with a closure plug.
November 30, 1983
Date of Patent:
February 24, 1987
Board of Trustees of the University of Alabama
Abstract: 3-[(Substituted-amino)(aryl or heteroaryl)methyl]-1H-indoles which are useful as color-formers in pressure-sensitive carbonless duplicating systems and thermal marking systems are prepared by reacting 3-[(arylsulfonyl)(aryl or heteroaryl)methyl]-1H-indoles with amines or precursors thereof in the presence of a base.
Abstract: 3-Arylcarbonyl- and 3-cycloalkylcarbonyl-1-aminoalkyl-1H-indoles, useful as analgesic, anti-rheumatic and anti-inflammatory agents, are prepared by reacting a 3-arylcarbonyl- or 3-cycloalkylcarbonylindole with an aminoalkyl halide in the presence of an acid-acceptor; by reacting a 1-aminoalkyl-1H-indole with an arylcarboxylic acid halide or a cycloalkanecarboxylic acid halide in the presence of a Lewis acid; or by reacting a 3-arylcarbonyl- or 3-cycloalkanecarbonyl-1-tosyloxyalkyl- or haloalkyl-1H-indole with an amine.
Abstract: Novel lower-alkyl 2-(hydroxyphenylamino)benzoates, useful as inhibitors of lipoxygenase, are of the formula ##STR1## wherein R is hydrogen, lower-alkyl or lower-alkoxy; R' is hydrogen or lower-alkyl; R" is hydrogen, lower-alkyl or halo; and Alk is lower-alkyl. The compounds are prepared by de-etherification of the corresponding alkyl or benzyl ethers.
Abstract: 3-[(Alkoxy)(aryl or heteroaryl)methyl]-1H-indoles which are useful as color formers in pressure-sensitive carbonless duplicating systems and thermal marking systems are prepared by reacting 3-[(arylsulfonyl)(aryl or heteroaryl)methyl]-1H-indoles with alcohols in the presence of a base.
Abstract: An improvement in the process for esterification of 3,4-dihydroxyphenyl N-alkylaminoalkyl ketones with arylcarboxylic acid chlorides which comprises carrying out the esterification in the presence of a catalytic amount of a 4-di-lower-alkylaminopyridine or 4-(1-pyrrolidinyl)pyridine and an acid-acceptor comprising a tertiary amine or sterically-hindered secondary amine.
Abstract: Antiplaque dentifrices containing as the antiplaque ingredient the saccharin salt of an amino or quaternary ammonium antimicrobial agent, particularly chlorhexidine saccharin salt or octenidine saccharin salt, and the method of inhibiting, reducing and preventing dental plaque therewith are disclosed.
December 9, 1983
Date of Patent:
September 30, 1986
Sterling Drug Inc.
William G. Gorman, Karl F. Popp, Kenneth M. Mavica
Abstract: A series of 4-pyridinylaminobenzamides, useful as antihypertensive agents, was prepared from the corresponding 4-pyridinylaminobenzoic acids by reacting the acid chloride of the latter with ammonia or a primary or secondary amine. Alternatively the compounds were prepared by reacting an aminobenzamide with 4-chloropyridine or equivalent reagent.
Abstract: The method of preparing a 2.alpha.-cyano-4.alpha.,5.alpha.-epoxy-3-oxo steroid or a steroid fused at the 2- and 3-positions with a heterocyclic ring of controlled particle size which comprises dissolving the steroid in an organic solvent, precipitating the steroid by mixing a non-solvent for the steroid with the resulting solution, and controlling the time of mixing and the degree of agitation during mixing.
Abstract: 4-R'-5-Q-1,6-naphthyridin-2(1H)-ones (I), where R' is hydrogen or methyl and Q is hydroxymethyl, 1-hydroxyethyl alkanoyloxymethyl or 1-alkanoyloxyethyl, are produced by first reacting 4-R'-5-acetyl(or n-propanoyl)-6-[2-(di-lower-alkylamino]-2(1H)-pyridinone [III] with hydroxylamine or salt thereof to produce 4-R'-5-Q'-1,6-naphthyridin-2(1H)-one-6-oxide (II), where R' is defined as above and Q' is methyl or ethyl; next reacting II with an alkanoic anhydride to produce I where Q is alkanoyloxymethyl or 1-alkanoyloxyethyl; and, then hydrolyzing said alkanoyloxymethyl or -ethyl compound to produce I where Q is hydroxymethyl or 1-hydroxyethyl. Also shown is the cardiotonic use of II and I where Q is hydroxymethyl, 1-hydroxyethyl or alkanoyloxymethyl.
Abstract: Disclosed and claimed is the cardiotonic use of 1-R.sub.1 -5-(3-R'-4-R"-phenyl)-6-R-2(1H)-pyridinones (II), where R.sub.1 is hydrogen, lower-alkyl or lower-hydroxyalkyl, R is lower-alkyl or hydrogen, and, R' and R" are each hydrogen, amino or hydroxy, at least one of R' or R" being other than hydrogen, or where R' is nitro when R" is hydroxy, or pharmaceutically acceptable acid-addition salts thereof where at least one of R' and R" is amino. Also disclosed and claimed are 1-R.sub.1 -5-(3-R'-4-R"-phenyl)-6-R-2(1H)-pyridinones (I), where R.sub.1, R' and R" are defined as above and R is lower-alkyl and acid-addition salts thereof where at least one of R' and R" is amino. Also shown and claimed is the process which comprises reacting 1-R.sub.1 -1,2-dihydro-2-oxo-5-(3-R'-4-R"-phenyl)-6-R-nicotinonitrile, where R.sub.
April 2, 1984
Date of Patent:
July 8, 1986
Sterling Drug Inc.
George Y. Lesher, Chester J. Opalka, Jr., Donald F. Page, Ruthann M. McGarry
Abstract: A glazing system comprising a glass pane and a wooden frame, and a beading strip comprised of two co-extruded hardness grades of a rubber or plastic material, the harder material forming a main body portion of the beading strip and the softer grade forming a weather seal.
Abstract: N-[1-(alkyl or arylmethyl)-4(1H)-pyridinylidine]-alkanamine and pharmaceutically acceptable acid addition salts thereof, for example, N-(1-octyl-4(1H)-pyridinylidine)octanamine monohydrochloride salt, which are useful as antimicrobial agents, especially on living tissues and nonliving surfaces and most especially against pathogenic dental microbes, and a process for preparation, methods of use and compositions thereof are disclosed.
Abstract: Basic amino or ammonium antimicrobial agent (especially bisbiguanide, quarternary ammonium salt and bispyridine)-polyethylene glycol ester surfactant-betaine and/or amine oxide surfactant antimicrobial skin cleansing compositions and method of use thereof are disclosed.