Abstract: Peptide mimics, having a constrained peptide backbone conformation, are HIV protease inhibitors. A compound of this invention is, for example, 3-Benzyl-5(alaninyl-1-aminoethyl)-2,3,6,7-tetrahydro-N-azepinyl-2-propiony l-valinyl-valinyl methyl ester.
Type:
Grant
Filed:
July 26, 1993
Date of Patent:
August 1, 1995
Assignee:
SmithKline Beechman Corp.
Inventors:
James F. Callahan, William F. Huffman, Michael L. Moore, Kenneth A. Newlander
Abstract: A method of treatment of Cryptococcus neoformans infection by administering to a patient in need thereof an effective amount of a benzimidazile compound.
Abstract: The present inventions relates to the use of certain benzimidazole compounds in the treatment of diseases caused by microsporidia organisms, in particular the treatment of diarrhea in patients infected with human immunodeficiency virus.
Abstract: Substituted 4-aminoquinazoline derivatives which are inhibitors of gastric acid secretion. A compound of the invention are the salts of strong acids of 3-butyryl-4-(2-methylphenylamino)-8-(hydroxymethyl)quinoline.
Abstract: This invention relates to the application of hydrophobic interaction chromatography combination chromatography to the purification of antibody molecule proteins.
Type:
Grant
Filed:
February 22, 1994
Date of Patent:
July 4, 1995
Assignee:
Smith Kline Beecham Corporation
Inventors:
Paula J. Shadle, John C. Erickson, Robert G. Scott, Thomas M. Smith
Abstract: Derivatives of 2-pyrrolidinones are described which inhibit the production of TNF and are useful in the treatment of disease states mediated or exacerbated by TNF production.
Type:
Grant
Filed:
March 30, 1992
Date of Patent:
May 30, 1995
Assignee:
SmithKline Beecham Corp.
Inventors:
Siegfried B. Christensen, IV, Klaus M. Esser, Philip L. Simon
Abstract: Substituted quinoline derivatives are described as inhibitors bone resorption with in particular, the compound 1-(2-methylphenyl)imidazo[4,5-c]quinoline hydrochloride.
Type:
Grant
Filed:
December 10, 1990
Date of Patent:
May 30, 1995
Assignee:
Smith Kline & French Laboratories Limited
Inventors:
Thomas H. Brown, Robert J. Ife, Colin A. Leach, David J. Keeling
Abstract: Angiotensin II receptor antagonists having the formula: ##STR1## which are useful in regulating hypertension and in the treatment of congestive heart failure, renal failure, and glaucoma, pharmaceutical compositions including these antagonists, and methods of using these compounds to produce angiotensin II receptor antagonism in mammals.
Type:
Grant
Filed:
June 14, 1993
Date of Patent:
May 23, 1995
Assignee:
SmithKline Beecham Corporation
Inventors:
Joseph A. Finkelstein, Richard M. Keenan, Joseph Weinstock
Abstract: The present invention relates to N-pyridylamidine and N-pyridylguanidine derivatives of general formula (I) in which: Ar.sup.1 is an optionally substituted phenyl ring; Ar.sup.2 is an optionally substituted phenyl ring; R.sup.1 is hydrogen or C.sub.1-4 alkyl; R.sup.2 is hydrogen or C.sub.1-4 alkyl; R.sup.3 is hydrogen or C.sub.1-4 alkyl; R.sup.4 is hydrogen, halogen, C.sub.1-6 alkyl or C.sub.1-6 alkoxy; X is CH.sub.2 or NR.sup.5, and R.sup.5 is hydrogen or C.sub.1-4 alkyl, and the salts thereof, and their use in therapy as gastric acid secretion inhibitors.
Type:
Grant
Filed:
July 20, 1994
Date of Patent:
April 25, 1995
Assignee:
SmithKline Beecham Intercredit B.V.
Inventors:
Robert J. Ife, Colin A. Leach, Dashyant Dhanak
Abstract: This invention relates to a new antioxidant use of, and method of treatment using certain hydroxycarbazole compounds or a pharmaceutically acceptable salt thereof. More specifically, the compounds are useful for the prevention of oxidative tissue damage to organs, particularly the central nervous system including the brain, in mammals afflicted with disease-induced ischemic trauma, particularly stroke.
Type:
Grant
Filed:
September 28, 1993
Date of Patent:
April 11, 1995
Assignee:
SmithKline Beecham Corporation
Inventors:
Frank C. Barone, Giora Feuerstein, Tian-Li Yue
Abstract: Angiotensin II receptor antagonists having tile formula: ##STR1## or a pharmaceutically acceptable salt thereof which are useful in regulating hypertension and in the treatment of congestive heart failure, renal failure, and glaucoma, pharmaceutical compositions including these antagonists, and methods of using these compounds to produce angiotensin II receptor antagonism in mammals. These antagonists function as prodrugs in vivo.
Type:
Grant
Filed:
June 30, 1994
Date of Patent:
March 7, 1995
Assignee:
SmithKline Beecham Corporation
Inventors:
Joseph Weinstock, Dimitri E. Gaitanopoulos
Abstract: An improved surface plasmon resonance detector, capable of recovering a desired eluted ligate allows for the collection and subsequent analysis of ligate solutions following interaction of the ligate with an immobilized ligand on a surface of a sensor chip of the surface plasmon resonance detector, permits the isolation and characterization of novel ligates and ligands.
Type:
Grant
Filed:
July 6, 1993
Date of Patent:
March 7, 1995
Assignee:
SmithKline Beecham Corporation
Inventors:
Michael Brigham-Burke, Daniel J. O'Shannessy
Abstract: The present invention provides a new medical use of the hydroxycarbazole compounds of Formula (I), preferably the hydroxylated metabolites of 1-(carbazol-4-yloxy-3-[[2-(o-methoxyphenoxy)ethyl]amino]-2-propanol)(carve dilol), for inhibiting the migration and proliferation of smooth muscle cells. In particular, the present invention provides a new use for the hydroxycarbazole compounds of Formula (I) for prevention of restenosis following percutaneous transluminal coronary angioplasty (PTCA), suppression of the progression of vascular hypertrophy associated with hypertension, and prevention of development of atherosclerosis. ##STR1## wherein: R.sub.1 -R.sub.9 are independently --H or --OH, with the proviso that a at least one of R.sub.1 -R.sub.9 is OH.
Abstract: Novel oxamide derivatives are described which inhibit the production of TNF and are useful in the treatment of disease states mediated or exacerbated by TNF production. The compounds of the present invention are also useful as inhibitors of PDE IV and are therefor useful in the treatment of disease states mediated or exacerbated thereby.
Type:
Grant
Filed:
March 2, 1993
Date of Patent:
February 28, 1995
Assignee:
SmithKline Beecham Corporation
Inventors:
Paul E. Bender, Siegfried B. Christensen, IV, Klaus M. Esser, Cornelia J. Forster, Michael D. Ryan, Philip L. Simon
Abstract: Compounds of the formula: ##STR1## or tautomeric forms and a pharmaceutically acceptable salt, and pharmaceutically acceptable solvates thereof, wherein:A.sup.1 is a substituted or unsubstituted oxazole substituted by up to 4 substituents selected from the group consisting of C.sub.1-6 -alkyl, C.sub.1-6 -alkoxy, phenyl, and halogen or any two substituents on adjacent carbon atoms, together with the carbon atoms to which they are attached, form a benzene ring, and wherein the carbon atoms of the benzene ring represented by the said two substituents are unsubstituted or substituted with up to three groups selected from halogen, C.sub.1-6 -alkyl, phenyl, C.sub.1-6 -alkoxy, halo-C.sub.1-6 -alkyl, hydroxy, amino, nitro, carboxy, C.sub.1-6 -alkoxycarbonyl, C.sub.1-6 -alkoxycarbonyl-C.sub.1-6 -alkyl, C.sub.1-6 -alkylcarbonyloxy, and C.sub.1-5 -alkylcarbonyl;R.sup.l is a hydrogen atom, a C.sub.1-6 -alkyl group, a C.sub.1-6 -alkylcarbonyloxy group, a phenyl-C.sub.
Abstract: A process is provided for the purification of pertussis toxin (PT) and/or filamentous hemagglutinin antigen (FHA) from a B. pertussis fermentation broth or cell free culture supernatant containing at least one antigen, which comprises contacting the fermenation broth or cell free culture supernatant with a hydroxyapatite adsorbent for a sufficient time to adsorb the antigen(s) at a pH which both PT and FHA are adsorbed and eluting a mixture containing the adsorbed antigen(s) from the adsorbent with eluant at a pH which both PT and FHA are eluted. The PT and FHA may be further purified by two sequential chromatographic columns, one of which involves apolar-ligand chromatography.
Abstract: The present invention relates to the use of an angiotensin II receptor antagonist in the manufacture of a medicament for the primary and secondary prevention of infarction.