Abstract: The DNA coding for human recombinant growth hormone releasing factor (GRF) cloned into a bacterial plasmid expression vector by assembling in one step selected synthetic DNA fragments.
Type:
Grant
Filed:
January 8, 1985
Date of Patent:
August 15, 1989
Assignee:
Smith Kline-RIT, s.a.
Inventors:
Alfredo J. Morais Cravador, Paul Jacobs, Alex J. Bollen, Ary Van Elsen, Albert A. M. Herzog
Abstract: Invented are new tetracarboxylate compounds which are chelators for calcium ions. Also invented is a useful method of measuring intracellular calcium concentrations using these novel compounds as an optical indicator.
Type:
Grant
Filed:
May 19, 1988
Date of Patent:
July 18, 1989
Assignee:
SmithKline Beckman Corporation
Inventors:
Robert M. DeMarinis, Haralambos E. Katerinopoulos, Katharine A. Muirhead
Abstract: Novel compounds, pharmaceutical compositions and a method of inhibiting the 5-lipoxygenase products in an animal in need thereof which comprises administering an effective, 5-lipoxygenase pathway inhibiting amount of a 2,2'-[1,2-ethanediylbis-(thio)]-bis-1H-imidazole or 2,2'-[1,3-propan-2-onediylbis-(thio)]bis-1H-imidazole, or a pharmaceutically acceptable salt thereof, to such animal.
Abstract: Polynucleotide hybridization probes are labeled in non-probe regions but not in probe regions by selectively protecting probe regions prior to modification of the polynucleotide.
Type:
Grant
Filed:
April 15, 1985
Date of Patent:
June 20, 1989
Assignee:
Smithkline Beckman Corporation
Inventors:
Craig W. Adams, Jeffry J. Leary, Martin Rosenberg
Abstract: 2-(N-Phenylakyl-N-formyl)amino-3-hydroxy-2-propenoic acids are intermediates for mercaptoimidazolecarboxylic acids which are dopamine-.beta.-hydroxylase inhibitors.
Type:
Grant
Filed:
January 21, 1988
Date of Patent:
June 6, 1989
Assignee:
SmithKline Beckman Corporation
Inventors:
Joseph A. Finkelstein, Lawrence I. Kruse, Thomas B. Leonard
Abstract: A fusion between DNA sequences coding for hAT and hGRF via a synthetic adaptor coding for an in vitro cleavable amino acid sequence is used to express hGRF at high levels in E. coli.
Abstract: Vasopressin antagonists which have a 4'-methyl-.beta.-mercapto-.beta.,.beta.-cyclopentamethylenepropionic acid group have vasopressin antagonist activity without substantial agonist activity. A species of the invention is [1-(4'-methyl-.beta.-mercapto-.beta.,.beta.-cyclopentamethylenepropionic acid)-2-(O-ethyl)-D-tyrosine-4-valine-8-arginine]vasopressin.
Abstract: Sulfinyl and sulfonyl substituted 3-benzazepine compounds are useful in treating gastrointestinal motility disorders and emesis. A particular compound of this invention is 7-methylsulfonyl-2,3,4,5-tetrahydro-1H-3-benzazepine.
Type:
Grant
Filed:
March 14, 1988
Date of Patent:
April 25, 1989
Assignee:
SmithKline Beckman Corporation
Inventors:
William E. Bondinell, Herbert S. Ormsbee, III
Abstract: The invention relates to 4-hydroxy pyrrolidone derivatives which help restore learning and memory difficulties associated with ageing. A compound of the invention is 2-(4-hydroxy-2-oxo-1-pyrrolidineacetamido)acetamide.
Type:
Grant
Filed:
December 11, 1987
Date of Patent:
April 25, 1989
Assignee:
ISF Societa Per Azioni
Inventors:
Mario Pinza, Carlo Farina, Silvano Banfi, Ugo Pfeiffer
Abstract: This invention relates to (isopropyl and tertiary butyl-amino-2-hydroxypropoxy)phenyl-3[2H]-pyridazinones which have .beta.-adrenoceptor antagonist activity.
Type:
Grant
Filed:
March 20, 1987
Date of Patent:
April 11, 1989
Assignee:
Smith Kline & French Laboratories Limited
Inventors:
Anthony M. Roe, William J. Coates, Robert A. Slater, Stephen P. Breukelman
Abstract: This invention relates to alkanoic acid compounds having phenyl and thio substituents which are useful as leukotriene antagonists and pharmaceutical compositions containing such compounds. This invention also relates to methods of treating diseases in which leukotrienes are a factor by administration of an effective amount of the above compounds or compositions.
Type:
Grant
Filed:
May 16, 1988
Date of Patent:
April 11, 1989
Assignee:
SmithKline Beckman Corporation
Inventors:
John G. Gleason, Ralph F. Hall, Thomas Wen-Fu Ku, Carl D. Perchonock
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: 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.