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 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: 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: A process for the prepartion of 3-[4-(4-oxo-1,4-dihydropyridin-1-yl)benzoyl]butanoic acid which comprises the reaction of 3-(4-fluorobenzoyl)butanoic acid with 4-hydroxypyridine under aqueous conditions in the presence of a base.
Type:
Grant
Filed:
January 29, 1988
Date of Patent:
November 1, 1988
Assignee:
Smith Kline & French Laboratories Limited
Inventors:
Michael B. Mitchell, Kiritkant D. Pancholi
Abstract: A novel process for the isolation and purification of vancomycin class antibiotics which utilized affinity chromatography by the formation of a sorption complex between the antibiotic and an immobilizing ligand selected from -D-alanyl-D-alanine or -X-D-alanyl-D-alanine, wherein X is an amino acid radical and the novel affinity chromatography sorbent employed therein are disclosed.
Type:
Grant
Filed:
February 4, 1987
Date of Patent:
October 18, 1988
Assignee:
Smithkline Beckman Corporation
Inventors:
Robert D. Sitrin, Kenneth M. Snader, Gail F. Wasserman
Abstract: This invention relates to 2- and 4-pyrimidinylmethylsulphinyl(and thio)benzimidazoles in which the pyrimidyl group is substituted by an optionally substituted amino group. These compounds inhibit exogenously and endogenously stimulated gastric acid secretion.
Type:
Grant
Filed:
February 14, 1986
Date of Patent:
October 11, 1988
Assignee:
Smith Kline & French Laboratories Limited
Abstract: The compounds represented by the formula (I) ##STR1## wherein n is 1 or 2; m is 0, 1 or 2; p is 9, 10, 11, 12 or 13; X is hydrogen or hydroxyl; R is hydroxyl or amino; R.sub.1 is hydrogen, amino or ##STR2## and R.sub.2 is hydroxyl, amino, ##STR3## with the proviso that when m is 0, R.sub.1 is hydrogen or pharmaceutically acceptable salts thereof have been found to be leukotriene antagonists and useful in the treatment of diseases in which leukotrienes are a factor, such as asthma.
Abstract: The invention relates to a class of 3,4-diamino-1,2,5-thiadiazole-1-oxides which have histamine H.sub.1 -antagonist activity. A preferred compound of the invention is 3-[3-(5-bromo-3-methylpyrid-2-ylamino)-propylamino]-4-amino-1,2,5-thiadiaz ole-1-oxide.
Type:
Grant
Filed:
June 11, 1986
Date of Patent:
September 13, 1988
Assignee:
Smith Kline & French Laboratories Limited
Abstract: The imidazolylthio substituted alkanoic acids represented by the formula (I) or (IA) as defined herein have been found to be leukotriene antagonists and useful in the treatment of diseases in which leukotrienes are a factor, such as asthma.
Type:
Grant
Filed:
October 24, 1986
Date of Patent:
September 6, 1988
Assignee:
Smithkline Beckman Corporation
Inventors:
William E. Bondinell, David T. Hill, Barry M. Weichman
Abstract: Vasopressin antagonists which have a dipeptide tail composed of a neutral and basic amino acid unit demonstrate potent V.sub.1 and V.sub.2 -antagonist activity. Two species of this invention, which are prepared by solid phase peptide synthesis, are [1-(.beta.-mercapto-.beta.,.beta.-cyclopentamethylene propionic acid)-2-(O-ethyl)-D-tyrosine-4-valine-7-tyrosine-8-arginine-9-desglycine]- vasopressin and [1-(.beta.-mercapto-.beta.,.beta.-cyclopentamethylenepropionic acid)-2-(O-ethyl)-D-tyrosine-4-valine-7-arginine-8-tyrosine-9-desglycine]- vasopressin.
Abstract: The invention relates to cyanoalkanimidamido derivatives that have utility as cardiac stimulants. A compound of the invention is 6-[4-(N.sup.2 -cyanoethanimidamido)phenyl]-5-methyl-4,5-dihydro-3(2H)-pyridazinone.
Type:
Grant
Filed:
February 10, 1987
Date of Patent:
August 23, 1988
Assignee:
Smith Kline & French Laboratories Limited
Abstract: The invention relates to cyanoalkanimidamido derivatives that have utility as cardiac stimulants. A compound of the invention is 6-[4-(N.sup.2 -cyanopropanimidamido)phenyl]-5-methyl-4,5-dihydro-3(2H)-pyridazinone.
Type:
Grant
Filed:
March 26, 1986
Date of Patent:
August 23, 1988
Assignee:
Smith Kline & French Laboratories Limited
Abstract: This invention relates to chemical compounds which have selective thyromimetic activity. A compound of this invention is 3,5-dibromo-3'-[6-oxo-3(1H)-pyridazinylmethyl]-thyronine.
Type:
Grant
Filed:
January 14, 1986
Date of Patent:
August 23, 1988
Assignee:
Smith Kline & French Laboratories Ltd.
Inventors:
David Ellis, John C. Emmett, Anthony H. Underwood, Paul D. Leeson
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 a 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:
April 28, 1987
Date of Patent:
July 26, 1988
Assignee:
Smithkline Beckman Corporation
Inventors:
James F. Callahan, William F. Huffman, Kenneth A. Newlander, Nelson C. F. Yim
Abstract: This invention relates to 2-pyridine derivatives substituted in the 4-position with a dialkylamino- or piperidinyl- or pyrrolidinylallyl group. The compounds have histamine H.sub.2 -antagonist activity.
Type:
Grant
Filed:
October 31, 1985
Date of Patent:
July 19, 1988
Assignee:
Smith Kline & French Laboratories Limited
Abstract: A novel process for preparing 6-amino-3-hydrazinopyridazine derivatives comprising reacting a 3-amino-6-chloropyridazine derivative with ethyl carbazate under aqueous conditions.
Type:
Grant
Filed:
May 13, 1986
Date of Patent:
July 12, 1988
Assignee:
ISF Societa per Azioni
Inventors:
Mario Pinza, Riccardo Monguzzi, Riccardo Colombo
Abstract: This invention relates to tricyclic pyridazinone compounds, pharmaceutical compositions containing the compounds, and a method of stimulating cardiac activity in a mammal by administering an effective amount of the compound. A compound of the invention is 7-carboxamido-4,4a-dihydro-4a-methyl-[5H]-indeno[1,2-c]-pyridazin-3[2H]-on e.
Type:
Grant
Filed:
September 22, 1987
Date of Patent:
July 5, 1988
Assignee:
Smith Kline & French Laboratories Limited
Abstract: Compounds having the formula ##STR1## wherein n is 0 or 1, R.sup.2 through R.sup.9 are H or C.sub.1-2 alkyl, and X is pyridyl or mono- or disubstituted phenyl are useful in the preparation of the compounds which inhibit the 5-lipoxygenase pathway.