Abstract: Pyridiniomethacrylate polymers are described which are of use in the treatment of elevated serum cholesterol levels. A compound of the invention is cross-linked 3-(N-methyl-3-pyridinio)propyl methacrylate chloride.
Abstract: Aminoquinoline derivatives are described as inhibitors of the H.sup.+ K.sup.+ ATPase enzyme useful in the treatment of gastric acidity. A compound of the invention is 3-butyryl-4-(2-methylphenylamino)-8-(3-dimethylaminopropoxy)quinoline.
Type:
Grant
Filed:
August 7, 1990
Date of Patent:
January 21, 1992
Assignee:
SmithKline Beecham Intercredit B.V.
Inventors:
Thomas H. Brown, Robert J. Ife, Colin A. Leach
Abstract: Pharmaceutical compositions suitable for intra-rectal administration in the form of a foam are described which comprise a therapeutically effective amount of 5-aminosalicylic acid, a pharmaceutically acceptable aqueous carrier therefor, and means for generating a foam.
Type:
Grant
Filed:
April 25, 1990
Date of Patent:
January 21, 1992
Assignee:
Smith Kline & French Laboratories Limited
Abstract: A compound of formula (I) ##STR1## or a salt or acyl derivative thereof, in which X represents chlorine, C.sub.1-6 alkoxy, phenoxy, phenyl C.sub.1-6 alkoxy, NH.sub.2, --OH or --SH, is useful in treating viral infections.
Abstract: This invention relates to fused pyrimidine derivatives which have bronchodilator activity. A compound of this invention is 2-(2-propoxyphenyl)thieno[2,3-d]pyrimidin-4(3H)-one.
Abstract: This invention relates to phenylpurinone derivatives which have bronchodilator and anti-allergic activities. A compound of the invention is 2-(2-propoxy-5-chlorophenyl)purin-6-one.
Abstract: Phosphodiesterase (type III) inhibitors having the formula: ##STR1## wherein R.sup.4 is hydrogen and A is a dihydro-1,2,4-triazin-3-one group or a dihydro-1,2,4-triazin-6-one group which are useful in stimulating cardiac activity and in treating congestive heart failure and bronchoconstriction, pharmaceutical compositions including these inhibitors, and methods of using these compounds to produce phosphodiesterase (type III) inhibition in mammals.
Type:
Grant
Filed:
December 18, 1989
Date of Patent:
November 19, 1991
Assignee:
Smith Kline & French Laboratories Limited
Abstract: 2,4-diaminoquinazoline compounds are inhibitors of the H.sup.+ K.sup.+ ATPase enzyme and useful for the treatment of diseases of the stomach based on excessive gastric acid secretion. A compound of the invention is 2-[2-methyl-4-fluorophenyl)amino]-4-(N-methylphenylamino)quinazoline.
Type:
Grant
Filed:
May 8, 1990
Date of Patent:
November 12, 1991
Assignee:
Smithkline Beecham Intercredit B.V.
Inventors:
Robert J. Ife, Thomas H. Brown, Colin A. Leach, David J. Keeling
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.
Abstract: The present invention provides a pharmaceutical granule composition comprising cimetidine and, as a granulating agent and taste-masking agent, an ester of a polyhydroxy compound, and where desired a palatable pharmaceutically acceptable emulsifier. Particular esters are glycerol esters. The granules of the present invention can be used in the preparation of chewable tablets which have good palatability and bioavailability.
Type:
Grant
Filed:
December 20, 1988
Date of Patent:
October 15, 1991
Assignee:
Smith Kline Dauelsberg GmbH
Inventors:
Eberhard F. Gottwald, Hermann P. Osterwald, Horst M. Machoczek, David Mayron
Abstract: 1,4-Substituted 2,3-dihydropyrrolo[3,2-c]quinolines which are inhibitors of H.sup.+ K.sup.+ ATPase activity and useful as inhibitors of gastric acid secretion. A compound of the invention is 1-(2-methylphenyl)-4-amino-6-methyl-2,3-dihydropyrrolo[3,2-c]quinoline.
Type:
Grant
Filed:
June 19, 1990
Date of Patent:
September 24, 1991
Assignee:
SmithKline Beckman Intercredit B.V.
Inventors:
Thomas H. Brown, Robert J. Ife, Colin A. Leach
Abstract: Vasopressin derivatives having V.sub.1 antagonist activity which alleviate the symptoms of motion sickness. More specifically, the vasopressin V.sub.1 antagonists of this invention are employed to prevent nausea and emesis associated with motion. The antagonists may also be employed for preventing nausea and emesis due to other etiologies.
Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein L is NH or O;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: This invention relates to fused pyrimidine derivatives which have bronchodilator and anti-allergic activities. A compound of the invention is 2-(2-propoxyphenyl)pyrido[2,3-d]pyrimid-4(3H)-one.
Type:
Grant
Filed:
June 13, 1989
Date of Patent:
September 10, 1991
Assignee:
Smith Kline & French Laboratories, Ltd.
Inventors:
William J. Coates, Sean T. Flynn, Derek A. Rawlings
Abstract: A pharmaceutical composition is described which comprises a pharmaceutically acceptable carrier and a compound of the formula (1): ##STR1## or a pharmaceutically acceptable salt thereof wherein X is CH.sub.2 or S, in an amount sufficient to stimulate selectively histamine H.sub.3 -receptors.
Type:
Grant
Filed:
July 20, 1990
Date of Patent:
September 10, 1991
Assignee:
Smith Kline & French Laboratories Limited
Abstract: Invented are carboxyl and carboxyl alkyl ester substituted 11-keto and hydroxy analogues of synthetic steroidal compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds to inhibit steroid 5-.alpha.-reductase.
Type:
Grant
Filed:
November 1, 1989
Date of Patent:
August 20, 1991
Assignee:
SmithKline Beecham Corporation
Inventors:
Dennis A. Holt, Brian W. Metcalf, Mark A. Levy
Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein X is CO and Y is NH or O, or X is NH and Y is CO;Z is CH.sub.2, O, S or NR.sub.3 wherein R.sub.3 is hydrogen, C.sub.1-6 alkyl, C.sub.3-7 alkenyl-methyl, phenyl or phenyl C.sub.1-4 alkyl either of which phenyl moieties may be substituted by one or two of halogen, CF.sub.3, C.sub.1-6 alkoxy or C.sub.1-6 alkyl; and R.sub.a is not present; orZ is CH or N and R.sub.a is as defined for R.sub.3 above;R.sub.b is present when X--Y--R.sub.2 is attached at the phenyl ring and is selected from hydrogen, halogen, CF.sub.3, hydroxy, C.sub.1-6 alkoxy or C.sub.1-6 alkyl;R.sub.1 is 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.
Abstract: This invention relates to (R)-.alpha.-methyl-4-halobenzenemethanamine salts of epimers of acids of the formula ##STR1## and the use of these salts to separate these epimers. These acids are leukotriene antagonists.
Abstract: Invented are carboxyl and carboxyl alkyl ester substituted 7-keto and hydroxy analogues of synthetic steroidal compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds to inhibit steroid 5-.alpha.-reductase. Also invented are methods for preparing these compounds.
Type:
Grant
Filed:
August 24, 1989
Date of Patent:
July 16, 1991
Assignee:
SmithKline Beecham Corporation
Inventors:
Brian W. Metcalf, Dennis A. Holt, Mark A. Levy
Abstract: The invention relates to 3-phosphinic acid steroidal compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds to inhibit steroid 5.alpha.-reductase.
Type:
Grant
Filed:
December 23, 1988
Date of Patent:
June 25, 1991
Assignee:
SmithKline Beecham Corporation
Inventors:
Dennis A. Holt, Mark A. Levy, Brian W. Metcalf