Abstract: The compounds of formula (I) ##STR1## wherein R.sub.1 is hydrogen or an alkyl radical containing one to six carbon atoms and R.sub.2 is an alkyl radical containing one to six carbon atoms possess markedly increased activity against malaria-causing parasites. Pharmaceutical compositions and method of treatment of subjects with malaria are also disclosed.
Abstract: The invention relates to a class of tetrahydroisoquinolinylalkanoic acids containing an aryl sulphonamide group which have activity as thromboxane A.sub.2 antagonists.
Type:
Grant
Filed:
June 27, 1988
Date of Patent:
March 14, 1989
Assignee:
SmithKline & French Laboratories, Ltd.
Inventors:
Graham J. Durant, Andrew D. Gribble, Robert A. Slater
Abstract: New compounds which have potent V.sub.2 -vasopressin antagonistic activity are prepared by a 1,6-cyclization using peptide bond formation. The structures of the compounds are characterized by the Pas.sup.1,6 or Tas.sup.1,6 cyclized unit. Also a chiral synthesis of the optically pure Pas intermediates is described.
Type:
Grant
Filed:
May 9, 1988
Date of Patent:
March 7, 1989
Assignee:
SmithKline Beckman Corporation
Inventors:
James F. Callahan, William F. Huffman, Kenneth A. Newlander, Nelson C. F. Yim
Abstract: This invention provides 5-substituted-4-pyrimidones having in the 2-position a heterocyclic (or substituted phenyl) alkyl group. These compounds have histamine H.sub.2 -antagonist activity.
Type:
Grant
Filed:
February 9, 1983
Date of Patent:
February 28, 1989
Assignee:
Smith Kline & French Laboratories Limited
Abstract: This invention relates to novel substituted 4-aminoquinoline derivatives which are inhibitors of gastric acid secretion in mammals. A compound of the invention is 3-butyryl-4-(2-methylphenylamino)-8-methoxyquinoline.
Type:
Grant
Filed:
September 3, 1987
Date of Patent:
February 21, 1989
Assignee:
Smith Kline & French Laboratories Limited
Inventors:
Robert J. Ife, Thomas H. Brown, Colin A. Leach
Abstract: This invention relates to novel substituted 4-aminoquinoline derivatives which are inhibitors of gastric acid secretion in mammals. A compound of the invention is 3-butyryl-4-(2-methylphenylamino)-8-methoxyquinoline.
Type:
Grant
Filed:
May 12, 1988
Date of Patent:
February 21, 1989
Assignee:
SmithKline & French Laboratories Limited
Inventors:
Robert J. Ife, Thomas H. Brown, Colin A. Leach
Abstract: An immunomodulating pharmaceutical composition comprising an effective, leukocyte interferon production inducing amount of NS1 and a pharmaceutically acceptable carrier or diluent; and a method of modulating the immune response in a human or other animal in need thereof by inducing the production of leukocyte IFN which comprises administering an effective amount of NS1 to such human or animal.
Abstract: Potent dopamine-.beta.-hydroxylase inhibitors having the Formula ##STR1## that are useful to inhibit dopamine-.beta.-hydroxylase activity, pharmaceutial compositions including these inhibitors, and methods of using these inhibitors to inhibit dopamine-.beta.-hydroxylase activity in mammals. Also disclosed are novel intermediates useful in preparing the presently invented inhibitors.
Abstract: A novel antibiotic complex of "vancomycin-like" antibiotics, AAD 216 complex, is produced by the cultivation of a fermentation broth containing Kibdelosporangium aridum Shearer gen. nov., sp. nov. ATCC 39323 microorganisms in an aqueous nutrient medium under submerged aerobic conditions. The AAD 216 complex and its major bioactive components; AAD 216A, AAD 216B, and AAD 216C exhibit antibiotic activity and growth promotant activity.
Type:
Grant
Filed:
June 10, 1986
Date of Patent:
January 10, 1989
Assignee:
SmithKline Beckman Corporation
Inventors:
Betty A. Bowie, Richard D. Hedde, Thomas O. Lindsey, David J. Newman, Marcia C. Shearer, Robert D. Sitrin, Joseph R. Valenta
Abstract: Process for preparing pyrrolidinone derivatives of (1) ##STR1## in which R is hydrogen, alkyl or acyl characterized in that a compound of (2) ##STR2## wherein R.sup.1 is hydrogen and R.sup.2 is benzyl or substituted benzyl, or R.sup.1 and R.sup.2 can together form a group ##STR3## where R.sup.4 and R.sup.5 are independently hydrogen, alkyl, phenyl or optionally substituted aryl or together are 1,4-butylene or 1,5-pentylene; R.sup.3 is hydrogen or straight or branched alkyl of 1 to 4 carbon atoms; and X is alkyl subjected to N-deprotection and the deprotected intermediate is cyclized intramolecularly.The deprotected intermediates can be isolated as acid-addition salts.
Abstract: A method of inhibiting the 5-lipoxygenase pathway in an animal in need thereof which comprises administering an effective, 5-lipoxygenase pathway inhibiting amount of a diaryl-substituted imidazole fused to a thiazole pyrrolidine, thiazide or piperidine ring to such animal.
Type:
Grant
Filed:
June 17, 1987
Date of Patent:
December 27, 1988
Assignee:
SmithKline Beckman Corporation
Inventors:
Paul E. Bender, Don E. Griswold, Nabil Hanna, John C. Lee
Abstract: A plasmid naturally present in N. orientalis can be used as a vector for cloning or expression in Actinomycetales and to derive other vectors.
Type:
Grant
Filed:
June 12, 1985
Date of Patent:
December 13, 1988
Assignee:
SmithKline Beckman Corporation
Inventors:
Louis R. Fare, Yong K. Oh, Dean P. Taylor, Jenifer B. Widger
Abstract: A method and slide for collecting and testing fecal occult blood which permits multiple analyses of a single fecal sample. The slide contains a pocket-like member on a portion of the inside front cover of the slide. An absorbent insert is disposed in the pocket. When the cover is in a closed position the pocket overlies the fecal smear on the specimen viewing sheet and the insert can be removed from the pocket. This design permits an analysis to be done on the specimen receiving sheet of the slide together with a second confirmatory test on the insert.
Type:
Grant
Filed:
November 24, 1986
Date of Patent:
December 6, 1988
Assignee:
SmithKline Beckman Corporation
Inventors:
Josefina T. Baker, Joseph F. Pagano, Ronald J. Schoengold
Abstract: A process for preparing compounds (1) ##STR1## where Y is NR.sup.1 R.sup.2 or OR, R.sup.1 and R.sup.2 are hydrogen or C.sub.1-3 alkyl, and R is C.sub.1-3 alkyl, which comprises protecting the hydroxy group of a compound (2) ##STR2## cyclizing the product under basic conditions and removing the protecting group.
Abstract: A novel process for preparing cimetidine polymorph "B" comprises precipitating cimetidine from an aqueous-alcoholic solution of an acid addition salt. The precipitation is conducted at a temperature of above 15.degree. C.
Abstract: Amide derivatives of non-steroidal anti-inflammatory carboxylic acids which have anti-inflammatory activity in their own right as well as being effective as pro-drugs of the carboxylic acids.
Abstract: Methods for reproducibly labelling viable cells with cyanine dyes that do not significantly affect cell viability. Applications for labelled cells include using labelled red blood cells to distinguish post-transfusional bleeding from immunologic reaction and using dilution to measure growth rate of cultured cells.
Type:
Grant
Filed:
October 31, 1986
Date of Patent:
November 8, 1988
Assignee:
SmithKline Beckman Corporation
Inventors:
Paul K. Horan, Bruce D. Jensen, Sue E. Slezak
Abstract: New intermediates, namely 2-(2-halo-3,4-dimethoxybenzyl)-5-(4-methoxyphenyl)-oxazolidines, are prepared by a synthetic sequence which uses a Darzen's reaction in a homogeneous solvent system.