Abstract: This invention relates to certain salts of leukotriene antagonists and the use of a particular amine to form these salts as a means for selectively crystallizing optical isomers of the leukotriene antagonists disclosed herein.
Abstract: Imidazole derivatives are described which are useful in restoring learning and treating memory difficulties. A compound of the invention is 2,5-dioxohexahydro-1H-pyrrolo[1,2-a]imidazole.
Type:
Grant
Filed:
April 3, 1992
Date of Patent:
April 6, 1993
Assignee:
I.S.F. Societa per Azioni
Inventors:
Mario Pinza, Alberto Cerri, Carlo Farina, Maria T. Riccaboni
Abstract: Isoquinoline compounds, compositions containing them and their use in the inhibition of gastric acid secretion in mammals. A compound of the invention is 1-[(2-Methoxyphenylmethyl)amino]isoquinoline hydrochloride.
Type:
Grant
Filed:
April 4, 1990
Date of Patent:
April 6, 1993
Assignee:
Smithkline Beecham Intercredit B.V.
Inventors:
Thomas H. Brown, Robert J. Ife, Colin A. Leach
Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein L is NH;X and Y are independently selected from hydrogen or C.sub.1-4 alkyl, or together are a bond;R.sub.1 and R.sub.2 are independently selected from hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl-C.sub.1-4 alkyl, or together are C.sub.2-4 polymethylene;R.sub.3 and R.sub.4 are independently selected from hydrogen, halogen, CF.sub.3, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, C.sub.1-7 acyl, C.sub.1-7 acylamino, C.sub.1-6 alkylsulphonylamino, N-(C.sub.1-6 alkylsulphonyl)-N-C.sub.1-4 alkylamino, C.sub.1-6 alkylsulphinyl, hydroxy, nitro or amino, aminocarbonyl, aminosulphonyl, aminosulphonylamino or N-(aminosulphonyl)-C.sub.1-4 alkylamino optionally N-substituted by one or two groups selected from C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkyl C.sub.1-4 alkyl, phenyl or phenyl C.sub.1-4 alkyl groups or optionally N-disubstituted by C.sub.
Abstract: The invention provides a pharmaceutical granule comprising cimetidine and 2-20% (w/w) relative to the cimetidine of a co-polymer of dimethylaminoethylmethacrylate and neutral methacrylic acid esters. Compositions of this invention have good palatability and dissolution characteristics.
Abstract: This invention relates to certain 2-substituted benzaldehydes which are useful intermediates for preparing certain diacids which are useful as leukotriene antagonists.
Type:
Grant
Filed:
March 20, 1990
Date of Patent:
February 23, 1993
Assignee:
SmithKline Beecham Corporation
Inventors:
Ralph F. Hall, John F. Newton, Kathleen A. Phipps, Joanne Smallheer
Abstract: A method for making 8-methyl-7-(1-oxopropyl)indolizino[1,2-b]quinolin-9(11H)-ones from 4-ethyl-4-hydroxy-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinolin-3,14(4H,12 H)-diones, said method being graphically illustrated as follows: ##STR1##
Type:
Grant
Filed:
September 28, 1990
Date of Patent:
October 13, 1992
Assignee:
SmithKline Beecham Corporation
Inventors:
Joseph M. Fortunak, Mark Mellinger, Jeffery L. Wood
Abstract: Compounds comprising pyridyl and phenyl substituted pyrrolo[1,2-a]imidazole derivatives and pyridyl and phenyl substituted imidazo[1,2-a]pyridine derivatives, pharmaceutical compositions containing said compounds, and their use as 5-lipoxygenase pathway inhibitors.
Type:
Grant
Filed:
December 26, 1991
Date of Patent:
September 8, 1992
Assignee:
SmithKline Beecham Corp.
Inventors:
Jerry L. Adams, Paul E. Bender, John G. Gleason, Nabil Hanna, John F. Newton, Jr., Carl D. Perchonock
Abstract: This invention relates to alkanoic acid compounds having phenyl and heteroarylthio 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:
December 21, 1990
Date of Patent:
September 1, 1992
Assignee:
SmithKline Beecham Corporation
Inventors:
John G. Gleason, Ralph F. Hall, Irene Uzinskas
Abstract: Substituted 4-aminoquinazoline derivatives of the formula: ##STR1## wherein R.sup.1 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkoxy C.sub.1-6 alkyl,C.sub.3-6 cycloalkyl, C.sub.3-6 cycloalkyl C.sub.1-6 alkyl, phenyl C.sub.1-6 alkyl, the phenyl group being optionally substituted;R.sup.2 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, amino, C.sub.1-6 alkylthio, halogen, cyano, hydroxy, C.sub.1-6 alkanoyl or trifuromethyl;m is 1 to 3;R.sup.3 is hydrogen, C.sub.1-6 alkyl, phenyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, C.sub.1-6 alkanoyl, amino, C.sub.1-6 alkylamino, ci-C.sub.1-6 alkylamino, halogen, trifluoromethyl or cyano;n is 1 or 2; andR.sup.4 is hydrogen; or a salt thereof are useful as inhibitors of gastric acid secretion.
Type:
Grant
Filed:
February 23, 1989
Date of Patent:
September 1, 1992
Assignee:
SmithKline Beckman Intercredit B.V.
Inventors:
Robert J. Ife, Thomas H. Brown, Colin A. Leach
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:
December 4, 1989
Date of Patent:
July 28, 1992
Assignee:
SmithKline Beecham Corporation
Inventors:
Paul E. Bender, John G. Gleason, Don E. Griswold, Nabil Hanna, Ivan Lantos, Kazys A. Razgaitis, Henry M. Sarau, Susan C. Shilcrat
Abstract: This invention relates to an animal pour-on pesticidal formulation which comprises at least one pesticide selected from the group consisting of the synthetic pyrethroids, preferably cypermethrin, the organophosphates and the amidines, and at least one vegetable oil consisting of glycerides of carboxylic acids with carbon chain lengths of more than 14 carbon atoms e.g. sunflower oil, as carrier for the pesticide which carrier constitutes at least 70% m/v of the formulation. The formulation may optionally further include a synergist, preferably piperonylbutoxide and solvents such as diacetone alcohol and dibutylphthalate.
Abstract: Compounds of structure (1); ##STR1## and pharmaceutically acceptable salts are described, whereR is hydrogen or C.sub.1-4 alkyl,R' is hydrogen, C.sub.1-4 alkyl, or a C.sub.1-4 alkyl group substituted by an alkyne or allene group provided that R' is not methyl when R and R" are both hydrogen, andR" is hydrogen or a C.sub.1-4 alkyl group substituted by an alkyne or allene group.These compounds have anti-depressant activity. Processes for the preparation of the compounds, pharmaceutical compositions and methods of use, are described.
Type:
Grant
Filed:
October 2, 1990
Date of Patent:
July 14, 1992
Assignee:
Consejo Superior de Investigaciones Cientificas
Inventors:
Eldiberto F. Alvarez, Carlos E. Recalde, Maria Angeles C. Villalobos, Antonio Diaz Diaz, Carlos B. Barrios, Maria del Carmen O. Estomba
Abstract: This invention relates to phenylpyrimidone derivatives which have bronchodilator activity. A compound of the invention is 4-cyano-6-hydroxy-2-(2-propoxyphenyl)pyrimidine.
Type:
Grant
Filed:
April 25, 1990
Date of Patent:
June 2, 1992
Assignee:
Smith Kline & French Laboratories Limited
Abstract: Polymers bearing a quaternary ammonium group are disclosed as being useful in lowering serum cholesterol levels in man. A compound of the invention is N,N-dimethyl-N-(2-(N,N-dimethylcarbamoyl)ethyl)-ammoniomethyl-substitut ed polystyrene, chloride salt.
Type:
Grant
Filed:
June 12, 1990
Date of Patent:
May 12, 1992
Assignee:
Smith Kline & French Laboratories
Inventors:
Albert A. Jaxa-Chamiec, Deirdre M. B. Hickey
Abstract: Polymers bearing a quaternary ammonium group are disclosed as being useful in lowering serum cholesterol levels in man. A compound of the invention is N-(2-N,N-dimethylamino)ethyl)-N,N-dimethylammoniomethyl-substituted polystyrene, chloride salt.
Type:
Grant
Filed:
June 12, 1990
Date of Patent:
May 5, 1992
Assignee:
Smith Kline & Franch Laboratories Limited
Inventors:
Albert A. Jaxa-Chamiec, Deirdre M. B. Hickey
Abstract: Invented are 4-aza-5-alpha-8(14)-17 substituted-androsten-3-ones having an 8(14), 7(8), or 16(17) double bond, optionally also having a 1(2) double bond, pharmaceutical compositions containing the compounds, and methods of using these compounds to inhibit steroid 5-alpha-reductase.
Type:
Grant
Filed:
October 10, 1989
Date of Patent:
May 5, 1992
Assignee:
Smithkline Beecham Corporation
Inventors:
Dennis A. Holt, Mark A. Levy, Brian W. Metcalf
Abstract: This invention relates to a process for preparing epoxy esters, and intermediates prepared by this process, in particular, to a process which produces non-racemic epoxy esters which are of use as intermediates in the preparation of pharmaceutical compounds.
Type:
Grant
Filed:
June 14, 1989
Date of Patent:
May 5, 1992
Assignee:
Smithkline Beckman Corp.
Inventors:
Joseph R. Flisak, Paul G. Gassman, Ivan Lantos, Wilford L. Mendelson