Abstract: Compounds of the structure ##STR1## where A is straight or branched divalent alkylene or divalent cycloalkylene, R.sub.1 is selected from hydrogen; alkylthio; optionally substituted phenylthio; optionally substituted phenylalkylthio; optionally substituted 2-, 3-, and 4-pyridyl; optionally substituted 2-, and 3-thienylthio; and optionally substituted 2-thiazolythio, R.sub.2 is selected from --COOB; --COOalkyl; --COOalkyl(carbocyclic aryl); --CONR.sub.5 R.sub.6 ; --COR.sub.6 ; and --OH, R.sub.3 is selected from phenylalkyl and heteroarylalkyl, and R.sub.4 is selected from optionally substituted alkoxy(carbocyclic aryl); optionally substituted carbocyclic aryloxy; optionally substituted heteroarylalkoxy; and optionally substituted heteroaryloxy are potent inhibitors of lipoxygenase enzymes and thus inhibit the biosynthesis of of leukotrienes. These compounds are useful in the treatment or amelioration of allergic and inflammatory disease states.
Type:
Grant
Filed:
November 20, 1992
Date of Patent:
February 22, 1994
Assignee:
Abbott Laboratories
Inventors:
Dee W. Brooks, Keith W. Woods, Karen E. Rodriques
Abstract: The present invention relates to compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof wherein Z is selected from optionally substituted phenyl, furyl, thienyl or thiazolyl; which inhibits leukotriene biosynthesis and is useful in the treatment of inflammatory disease states; also disclosed are leukotriene biosynthesis inhibiting compositions and a method for inhibiting 5-lipoxygenase activity and leukotriene biosynthesis.
Type:
Grant
Filed:
November 6, 1992
Date of Patent:
February 22, 1994
Assignee:
Abbott Laboratories
Inventors:
Dee W. Brooks, Andrew O. Stewart, Anwer Basha, Pramila Bhatia, James D. Ratajczyk
Abstract: A coated article comprises an outer, coated metal veneer coated with at least one coating selected from primer coatings, pigmented topcoat coatings, pigmented basecoat coatings and outer clear topcoat coating, the coated metal veneer being affixed to an underlying substrate having substantially the same shape as the coated veneer.The coated articles are particularly useful as body parts such as doors, hoods, trunk and roof panels, fenders, and rocker panels of automobile and truck bodies.A method of manufacturing the coated articles is also disclosed.
Abstract: Pharmaceutical compositions for the sublingual or buccal administration of therapeutic agents (particularly polypeptides) which are normally degraded upon oral administration comprise such a therapeutic agent, a solvent, optionally a cosolvent and/or hydrogel, and an oral mucosal membrane transport enhancing agent which is selected from the group consisting of essential and volatile oils and inorganic and organic acids.
Abstract: Stable, solid cut flower preservatives having excellent shelf life and stability comprise from about 1 part by weight to about 99 parts by weight of a sugar, glycoside or mixture thereof, from about 0.05 part by weight to about 2 part by weight of an ACC synthase inhibitor selected from L-trans-2-amino-4-(2-aminoethoxy)-3-butenoic acid and carboxymethoxylamine, from about 0.5 part by weight to about 8 parts by weight of aluminum sulfate having less than about 27 percent by weight water of hydration, and from about 0.05 part by weight to about 5 parts by weight of an antimicrobial agent.
Type:
Grant
Filed:
March 8, 1993
Date of Patent:
February 8, 1994
Assignee:
Abbott Laboratories
Inventors:
Warren E. Shafer, Derek D. Woolard, Neyyan K. P. Samuel, Gregory D. Venburg, Balan N. Devisetty, Daniel F. Heiman
Abstract: Compounds of the structure ##STR1## where Ar is optionally substituted carbocyclic aryl, 5- or 6-membered heterocyclic aryl, 10-membered bicyclic heterocyclic aryl containing one or two nitrogen atoms, 9- or 10-membered heterocyclic containing one or two nitrogen atoms and optionally containing a further nitrogen or oxygen atom and one oxo or thioxo substituent, benzo[b]furyl, or benzo[b]thienyl, A.sub.1 is propynyl, methylene, or a direct link to X, X is oxy, thio, sulfonyl, or NR.sub.4, A.sub.2 is selected from ##STR2## where Y is hydrogen, halogen, or nitrile; Z is hydrogen, R.sub.1 is alkyl, and R.sub.2 is hydrogen or alkyl are potent inhibitors of lipoxygenase enzymes and thus inhibit the biosynthesis of leukotrienes. These compounds are useful in the treatment or amelioration of allergic and inflammatory disease states.
Type:
Grant
Filed:
August 24, 1992
Date of Patent:
December 7, 1993
Assignee:
Abbott Laboratories
Inventors:
Joseph F. Dellaria, Jimmie L. Moore, Dee W. Brooks
Abstract: Pro-drugs of potent 5-lipoxygenase inhibiting compounds comprise compounds of the formula ##STR1## in which A is an alkylene or alkenylene group, X is oxygen, sulfur, sulfoxyl, or substituted nitrogen, and Y is a group which includes substituted or unsubstituted carbocyclic or substituted or unsubstituted heterocyclic aryl. R.sup.1 is an alkyl, alkenyl, amino, alkylamino, dialkylamino, or hydroxyamino group or an amine group bearing a metabolically cleavable leaving group. M is hydrogen, a pharmaceutically acceptable cation or a metabolically cleavable leaving group, with the proviso that either M or R.sup.1 must bear a metabolically cleavable leaving group.
Abstract: Substituted 8-alkoxy-1,2,3,3a,8,8a-hexahydroindeno[1,2-c]pyrroles; 5-alkoxy-2,3,4,4a,9,9a-hexahydro-1-H-indeno[2,1-c]pyridines; and 9-alkoxy-2,3,3a,4,5,9a-hexahydro-1H-benz[e]isoindoles are selective 5-HT receptor agents and are thus useful in the treatment of anxiety, depression, and hypertension.
Type:
Grant
Filed:
July 9, 1991
Date of Patent:
September 14, 1993
Assignee:
Abbott Laboratories
Inventors:
John F. DeBernardis, Michael D. Meyer, Kevin B. Sippy
Abstract: Oligopeptide compounds or oligopeptide analogue compounds of the formula A-B-D-E-G-J-L-M-Q-T are ligands for the anaphylatoxin receptor and are useful in the treatment of inflammatory disease states. Also disclosed are anaphylatoxin receptor ligand compositions and a method for modulating anaphylatoxin activity.
Type:
Grant
Filed:
June 19, 1991
Date of Patent:
June 29, 1993
Assignee:
Abbott Laboratories
Inventors:
Megumi Kawai, Yat S. Or, Paul E. Wiedeman, Jay R. Luly, Mikel P. Moyer
Abstract: Compounds of the formula: ##STR1## wherein R.sub.1 is selected from (1) hydrogen; (2) --NR.sub.2 R.sub.3, --OR.sub.2 or --SR.sub.2 where R.sub.2 and R.sub.3 are independently selected from hydrogen, alkyl, aryl and alkylaryl; and (3) optionally substituted C1-C8 alkyl, C2-C8 alkenyl, arylalkyl or cycloalkyl;Y is selected from sulfur and oxygen;n is an integer selected from 0 and 1;M is hydrogen, a pharmaceutically acceptable cation, or a metabolically cleavable group; andZ is a residue of a non-steroidal antiinflammatory drug of general form Z--COOH;or a pharmaceutically acceptable salt, ester or prodrug thereof,as well as pharmaceutical compositions containing the above compounds and a method for their use as lipoxygenase inhibitors.
Type:
Grant
Filed:
April 19, 1990
Date of Patent:
June 15, 1993
Assignee:
Abbott Laboratories
Inventors:
Dee W. Brooks, Joseph F. Dellaria, Jr., James B. Summers, Jr.
Abstract: The present invention provides certain (substituted carbocyclic aryl)amidoalkyl-and (substituted heterocyclic aryl)amidoalkyl-N-Hydroxy urea compounds which inhibit lipoxygenase enzyme activity and are thus useful in the treatment of allergic and inflammatory disease states.
Type:
Grant
Filed:
July 19, 1991
Date of Patent:
May 25, 1993
Assignee:
Abbott Laboratories
Inventors:
Joseph F. Dellaria, Dee W. Brooks, Jimmie L. Moore, Kevin J. Sallin
Abstract: R(+)-2-[4-[(tetrahydro-2-furanyl)carbonyl]-1-piperazinyl]-6,7-dimethoxy-4-q uinazolinamine hydrochloride or a pharmaceutically acceptable salt or hydratet hereof (terazosin), substantially free of the S(-)-enantiomer.
Abstract: Oligopeptide compounds or oligopeptide analogue compounds of the formula A-B-D-E-G-J-L are ligands for the anaphylatoxin receptor and are useful in the treatment of inflammatory disease states. Also disclosed are anaphylatoxin receptor ligand compositions and a method for modulating anaphylatoxin activity.
Type:
Grant
Filed:
June 4, 1991
Date of Patent:
March 2, 1993
Assignee:
Abbott Laboratories
Inventors:
Jay R. Luly, Megumi Kawai, Paul E. Wiedeman
Abstract: Substituted phenyl, naphthyl, and thienyl N-hydroxy urea compounds form a class of potent inhibitors of 5- and 12-lipoxygenase and are thus useful compounds in the treatment of inflammatory disease states where leukotrienes and other products of lipoxygenase enzyme activity are implicated.
Type:
Grant
Filed:
September 30, 1991
Date of Patent:
February 9, 1993
Assignee:
Abbott Laboratories
Inventors:
Dee W. Brooks, Daniel J. Kerkman, Jonathan G. Martin, Andrew O. Stewart, James B. Summers
Abstract: Certain N-aryl, N-heteroaryl-, N-arylalkyl-, N-heteroarylalkyl-, N-arylcyclopropyl- and N-heteroaryl-cyclopropyl-N'-hydroxyurea compounds are inhibitors of lipoxygenase enzyme activity and are thus useful agents in treating disease states such as asthma, arthritis, allergy, psoriasis, inflammatory bowel disease, gout, adult respiratory distress syndrome, endotoxin shock, and other inflammatory conditions in which the products of the arachidonic acid cascade are implicated.
Type:
Grant
Filed:
July 10, 1991
Date of Patent:
December 29, 1992
Assignee:
Abbott Laboratories
Inventors:
Dee W. Brooks, James B. Summers, Karen E. Rodriques
Abstract: A process for the production in high yield of 2-acetylbenzo[.beta.]thiophene and its alkyl and alkoxy substituted derivatives by converting a 2-halobenzaldehyde to a 2,2'-dithiobis(benzaldehyde) intermediate and reacting that intermediate successively with 2,4-pentanedione and chloroacetone in the presence of base.
Type:
Grant
Filed:
November 22, 1991
Date of Patent:
December 8, 1992
Assignee:
Abbott Laboratories
Inventors:
Daniel A. Dickman, Bruce W. Horrom, Brian A. Roden, Sanjay R. Chemburkar
Abstract: Water-dilutable polyurethane/acrylic copolymers which may be either completely nonionically stabilized or partically nonionically and partically anionically stabilized comprise the reaction product of an ethylenically terminated polyurethane macromonomer containing poly(oxyalklyene) segments and one or more ethylencially unsaturated monomers selected from acrylic acid, methacruylic acid, fumaric acid, styrene, vintyltoluene, and alkyl and hydroxyalkyl esters of acrylic, methacrylic, and furamic acids. The copolymers are useful as principal resins and as pigment grind resins in water-borne automotive base coat paint formulations.
Abstract: Compounds useful in inhibiting the biosynthesis of leukotrienes have the structure ##STR1## where M is hydrogen, a pharmaceutically acceptable cation, or a metabolically cleavable group, R.sup.4 is alkyl, cycloalkyl or --NR.sup.5 R.sup.6, where R.sup.5 and R.sup.6 are hydrogen, alkyl, cycloalkyl or alkanoyl, where A is a valence bond or is a straight or branched divalent alkylene group of from one to twelve carbon atoms, R.sup.2 and R.sup.3 are independently selected from hydrogen, straight or branched alkyl of from one to twelve carbon atoms, halogen, or trifluoroalkyl, and R.sup.1 is selected from phenoxy, phenylthio, 2-, 3-, or 4-pyridyloxy, 1 or 2-naphthyloxy, or 2,4,5, or 8-quinolyloxy, all optionally substituted with alkyl, haloalkyl, alkoxy, hydroxy or halogen.
Type:
Grant
Filed:
February 26, 1992
Date of Patent:
December 8, 1992
Assignee:
Abbott Laboratories
Inventors:
Dee W. Brooks, Andrew O. Stewart, Pramila Bhatia, Richard A. Craig
Abstract: A composition and method for thinning Perlette Seedless grape clusters is disclosed. The composition contains a surfactant and a gibberellin. In a method for thinning Perlette Seedless grape clusters, the composition is applied to Perlette Seedless grape clusters during bloom, with the result that clusters are produced that have fewer grapes and in which the grapes are increased in size and weight.
Abstract: Novel tetracyclic spirobenzazepine compounds of the formula ##STR1## or a pharmaceutically-acceptable salt, amide or ester thereof, which are dopamine D-1 receptor antagonists useful for treating dopamine-related neurological and psychological disorders, cognitive impairment, attention deficit disorders and addictive behavior disorders.
Type:
Grant
Filed:
September 19, 1991
Date of Patent:
October 27, 1992
Assignee:
Abbott Laboratories
Inventors:
Robert W. Schoenleber, Paul P. Ehrlich, John W. Kebabian, James R. Campbell