Abstract: Phosphodiesterase (type III) inhibitors having the formula: ##STR1## 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:
October 14, 1986
Date of Patent:
March 6, 1990
Assignee:
Smith Kline & French Laboratories Limited
Abstract: The invention relates to pyridazinone derivatives which have inotropic, vasodilator and bronchodilator activity. The compounds of the invention are described by formula (I): ##STR1## wherein: R.sup.1 is hydrogen or methyl;R.sup.2 is hydrogen or methyl; and represent double or single bonds; and the benzene ring is para- or meta-substituted; and pharmaceutically acceptable salts thereof.
Type:
Grant
Filed:
July 1, 1986
Date of Patent:
February 27, 1990
Assignee:
Smith Kline & French Laboratories Limited
Abstract: The invention provides a class of alkanoic acids substituted with a benzenesulphonamidopyridyl group. The compounds have activity as thromboxane A.sub.2 -antagonists.
Type:
Grant
Filed:
April 7, 1988
Date of Patent:
February 20, 1990
Assignee:
Smith Kline & French Laboratories Limited
Abstract: This invention relates to 2-pyridine derivatives substituted in the 4-position with a dialkylamino- or piperidinyl- or pyrrolidinylalkyl group. The compounds have histamine H.sub.2 -antagonist activity.
Type:
Grant
Filed:
April 19, 1988
Date of Patent:
January 16, 1990
Assignee:
Smith Kline & French Laboratories Limited
Abstract: This invention relates to purinone derivatives which have bronchodilator, vasodilator and anti-allergic activities. A compound of the invention is 2-(2-propoxyphenyl)-6-purinone.
Type:
Grant
Filed:
January 27, 1988
Date of Patent:
December 5, 1989
Assignee:
Smith Kline & French Laboratories Limited
Abstract: The invention relates to thiadiazinone derivatives that have utility as cardiac stimulants. A compound of the invention is 7-(1H-imidazol-1-yl)-9,9a-dihydroindeno[1,2-e][1,3,4]-thiadiazin-2(3H)-one .
Type:
Grant
Filed:
January 29, 1988
Date of Patent:
August 29, 1989
Assignee:
Smith Kline & French Laboratories Limited
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)-pyridazinyl-methyl]-thyronine.
Type:
Grant
Filed:
December 21, 1987
Date of Patent:
May 2, 1989
Assignee:
Smith Kline & French Laboratories Limited
Inventors:
David Ellis, John C. Emmett, Anthony H. Underwood, Paul D. Leeson
Abstract: The present invention relates to the use of certain indolone derivatives in particular, 4-(2-di-n-propyl-aminoethyl)-2-(3H)-indolone in a method of treatment of Parkinsons disease.
Type:
Grant
Filed:
May 19, 1988
Date of Patent:
April 25, 1989
Assignee:
Smith Kline & French Laboratories Limited
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 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: A process for the prepartion of 3-[4-(4-oxo-1,4-dihydropyridin-1-yl)benzoyl]butanoic acid which comprises the reaction of 3-(4-fluorobenzoyl)butanoic acid with 4-hydroxypyridine under aqueous conditions in the presence of a base.
Type:
Grant
Filed:
January 29, 1988
Date of Patent:
November 1, 1988
Assignee:
Smith Kline & French Laboratories Limited
Inventors:
Michael B. Mitchell, Kiritkant D. Pancholi
Abstract: This invention relates to 2- and 4-pyrimidinylmethylsulphinyl(and thio)benzimidazoles in which the pyrimidyl group is substituted by an optionally substituted amino group. These compounds inhibit exogenously and endogenously stimulated gastric acid secretion.
Type:
Grant
Filed:
February 14, 1986
Date of Patent:
October 11, 1988
Assignee:
Smith Kline & French Laboratories Limited
Abstract: The invention relates to a class of 3,4-diamino-1,2,5-thiadiazole-1-oxides which have histamine H.sub.1 -antagonist activity. A preferred compound of the invention is 3-[3-(5-bromo-3-methylpyrid-2-ylamino)-propylamino]-4-amino-1,2,5-thiadiaz ole-1-oxide.
Type:
Grant
Filed:
June 11, 1986
Date of Patent:
September 13, 1988
Assignee:
Smith Kline & French Laboratories Limited
Abstract: The invention relates to cyanoalkanimidamido derivatives that have utility as cardiac stimulants. A compound of the invention is 6-[4-(N.sup.2 -cyanoethanimidamido)phenyl]-5-methyl-4,5-dihydro-3(2H)-pyridazinone.
Type:
Grant
Filed:
February 10, 1987
Date of Patent:
August 23, 1988
Assignee:
Smith Kline & French Laboratories Limited
Abstract: The invention relates to cyanoalkanimidamido derivatives that have utility as cardiac stimulants. A compound of the invention is 6-[4-(N.sup.2 -cyanopropanimidamido)phenyl]-5-methyl-4,5-dihydro-3(2H)-pyridazinone.
Type:
Grant
Filed:
March 26, 1986
Date of Patent:
August 23, 1988
Assignee:
Smith Kline & French Laboratories Limited