Abstract: Peptides having vasopressin antagonist activity are prepared by a peptide synthesizer to insert a N-methylarginine at the 7-position of the structure. An example of this series of compounds is [1-(.beta.-mercapto-.beta.,.beta.-cyclopentamethylenepropionic acid)-2-(O-ethyl-D-tyrosine)-4-valine-7-desproline-8-N-methylarginine-9-de sglycine]-vasopressin.
Type:
Grant
Filed:
November 19, 1985
Date of Patent:
August 18, 1987
Assignee:
SmithKline Beckman Corporation
Inventors:
Fadia E. Ali, William F. Huffman, Garland R. Marshall, Michael L. Moore
Abstract: 2- or 3-.beta.-Indolylalanyl and .beta.-indolylglycyl vasopressins are prepared by standard peptide synthetic methods. These 2- or 3-TRP vasopressins have vasopressin antagonist activity.
Abstract: Vasopressin derivatives having V.sub.1 and oxytocin antagonist activity whose structures are characterized by a Mpa unit at position 1 and a des-Pro unit at position 7 are prepared by standard peptide synthetic methods also using an oxidative cyclization of a dimercaptan. Representative species are [1-deaminopenicillamine-2-(O-methyl)-tyrosine-7-desproline-8-arginine-9-de sglycine]vasopressin or [1-.beta.-mercaptopropionic acid-2-D-(O-ethyl)tyrosine-3-isoleucine-4-threonine-7-desproline-8-arginin e-9-desglycine]-vasopressin.
Abstract: Certain vasopressin-like peptides, which have an acyclic unit at position 1 and which have an .omega.-amino- or guanidinoalkyl substituent attached to the cysteine in the 6-position of the ring, have V.sub.1 -vasopressin and oxytocin antagonist activity. A species of this series of new compounds is [1-desaminopenicillamine-2-(O-ethyl-D-tyrosine)-8-(1,4-diaminobutane)-9-de sglycinamide]-vasopressin.
Type:
Grant
Filed:
April 16, 1986
Date of Patent:
August 4, 1987
Assignee:
SmithKline Beckman Corporation
Inventors:
James F. Callahan, William F. Huffman, Michael L. Moore, Nelson C. Yim
Abstract: The process is applicable to the supernatant of engineered yeast cells disrupted in the presence of a non-ionic detergent: it comprises the precipitation of contaminants by polyethylene glycol and the treatment cation or, after eventual ultrafiltration, with ammonium sulfate.
Type:
Grant
Filed:
April 3, 1985
Date of Patent:
July 28, 1987
Assignee:
Smith Kline RIT, S.A.
Inventors:
Frans Van Wijnendaele, Daniel Gilles, Guy Simonet
Abstract: Selected 2-(.alpha.-pyridyl)-.DELTA..sup.2 -heterocyclic compounds are used as active ingredients in animal feed compositions and in methods for increasing the growth or feed efficiency of monogastric animals. An active ingredient for use in this invention is 3,4-dihydro-4-hydroxy-5-(3-hydroxy)-2-pyridinyl)-4-methyl-2H-pyrrole-5-car boxamide.
Abstract: Tetraphosphine-coordinated gold(I) compounds, pharmaceutical compositions containing an effective, tumor cell growth-inhibiting amount of such a compound, and a method for treating tumor cells sensitive to such a compound which comprises administering a tumor cell growth-inhibiting amount of such a compound to an animal afflicted by said tumor cells.
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 26, 1985
Date of Patent:
June 9, 1987
Assignee:
SmithKline Beckman Corporation
Inventors:
Betty A. Bowie, David J. Newman, Marcia C. Shearer
Abstract: DNA sequences and recombinant DNA molecules comprising at least a portion coding for all or part of subunits A and/or B of cholera toxin are prepared by enzymatic digestion of DNA of V. cholerae strains, isolating specific fragments and inserting them in appropriate vectors and subunits A and/or B of cholera toxin are prepared by culture of microorganisms containing said modified vectors.
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:
July 13, 1983
Date of Patent:
May 19, 1987
Assignee:
SmithKline Beckman Corporation
Inventors:
Robert D. Sitrin, Kenneth M. Snader, Gail F. Wasserman
Abstract: This invention relates to 5-(phenyl)-2(1H)-pyrazinones substituted in the 4-position of the phenyl ring by an amino or acylamino group. These compounds has inotropic activity. One specific compound is 5-(4-acetamidophenyl)-2(1H)-pyrazinone.
Type:
Grant
Filed:
September 19, 1985
Date of Patent:
April 14, 1987
Assignee:
Smith Kline & French Laboratories Ltd.
Inventors:
John C. Emmett, Robert A. Slater, Brian H. Warrington
Abstract: This invention relates to cyanoguanidine derivatives that have utility in the treatment of congestive heart failure. A specific compound of this invention is 6-[4-(N.sup.3 -methyl-N.sup.2 -cyanoguanidino)phenyl]-5-methyl-4,5-dihydro-3(2H)-pyridazinone.
Abstract: The supernatant of engineered yeast cells having produced hepatitis B surface antigaen and disrupted in the presence of a polysorbate non-ionic detergent is clarified by addition of urea and adsorbed on colloidal silica from which the purified antigen is desorbed with a low ionic strength buffer supplemented with urea and a polysorbate non-ionic detergent.
Abstract: This invention relates to [.alpha.,.omega.-bis(diphenylphosphino)hydrocarbon]bis[(thiosugar)gold] and bis[(selenosugar)gold] derivatives, pharmaceutical compositions comprising an effective tumor cell growth-inhibiting amount of such a derivative, and a method of treating tumor cells sensitive to such a derivative which comprises administering a tumor cell growth-inhibiting amount of such a derivative to an animal afflicted by said tumor cells.
Abstract: A bacterial product is made by transforming a temperature sensitive lysogen with a DNA molecule which codes, directly or indirectly, for the product, culturing the transformant under permissive conditions and externalizing the product by raising the temperature to induce phage encoded functions.
Abstract: This invention relates to 5-(4-substituted)phenylpyrazinone compounds which have positive inotropic and vasodilator activity. One such compound is 5-(4-carboxamidophenyl)pyrazin-2(1H)-one.
Abstract: A live bovine viral diarrhoea (BVD) virus vaccine capable of producing immunity in bovines without causing significant side effects comprising a temperature sensitive (ts) mutant of BVD virus which is obtained by mutating a strain of BVD virus with nitrous acid. The temperature sensitive mutants show a replication ability considerably limited at the animal body temperature of 39.5.degree. C. The vaccine may be combined with other live bovine vaccines such as respiratory virus vaccines and then administered to bovines.
Abstract: Tetraphosphine-coordinated gold (I) compounds, pharmaceutical compositions containing an effective, tumor cell growth-inhibiting amount of such a compound, and a method of treating tumor cells sensitive to such a compound which comprises administering a tumor cell growth-inhibiting amount of such a compound to an animal afflicted by said tumor cells.