Abstract: A class of compounds identified as N-(1-methyl-1H-indol-5-yl)-(2,3 or 4-pyridyl)ureas, derivatives thereof, methods for their preparation, pharmaceutical compositions containing same and their 5-HT receptor antagonist activity are believed to be of potential use in the treatment of a variety of CNS disorders are described herein.
Abstract: An intermediate compound of Formula (V): ##STR1## wherein G is COQ.sub.1 and Q.sub.1 represents chloro, bromo, C.sub.1-4 alkoxy, PhO--, Cl.sub.5 C.sub.6 O--, Cl.sub.3 CO--, succinimidyloxy or imidazolyloxy; the remainder of the terms R.sub.1, R.sub.2, R.sub.3, R.sub.4, X and Y are defined in the specification. The intermediates of Formula V are useful for preparing 1-(2,3-dihydro-1-carboxamide final products wherein said final products possess 5-HT M-receptor antagonist activity.
Abstract: This invention relates to alkanoic acid compounds having phenyl and heteroarylthio substituents which are useful as leukotriene antagonists, processes for the preparation thereof, 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:
April 2, 1992
Date of Patent:
May 24, 1994
Assignee:
SmithKline Beecham Corporation
Inventors:
James S. Frazee, John G. Gleason, Ralph F. Hall
Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein R.sub.1 represents a 1,2,5,6-tetrahydropyridin-3-yl group N-substituted by R.sub.10 wherein R.sub.10 represents hydrogen, C.sub.1-2 alkyl, prop-2-enyl, prop-2-ynyl or cyclopropyl, R.sub.2 is a group OR.sub.4, where R.sub.4 is C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.2-4 alkynyl, a group OCOR.sub.5 where R.sub.5 is hydrogen or R.sub.4, or a group NHR.sub.6, or NR.sub.7 R.sub.8 where R.sub.6, R.sub.7 and R.sub.8 are independently C.sub.1-2 alkyl; and R.sub.3 is chloro, fluoro, bromo, methoxy, C.sub.1-3 alkyl substituted by one, two or three halogen atoms, or R.sub.3 is a group (CH.sub.2).sub.n R.sub.9 where R.sub.9 is --CN, --SH or --SCH.sub.3 and n is 0 or 1, with the proviso that when n is 0, R.sub.9 is not --SH; enhance acetylcholine function via an action at muscarinic receptors within the central nervous system and are therefore of potential use in the treatment and/or prophylaxis of dementia in mammals.
Type:
Grant
Filed:
February 23, 1993
Date of Patent:
May 24, 1994
Assignee:
Beecham Group p.l.c.
Inventors:
Steven M. Bromidge, Barry S. Orlek, Steven Dabbs
Abstract: A new use of, and method of treatment using, a compound selected from the group consisting essentially of compounds of Formula I: ##STR1## wherein: R.sub.1 is hydrogen, lower alkanoyl of up to 6 carbon atoms or aroyl selected from benzoyl and naphthoyl;R.sub.2 is hydrogen, lower alkyl of up to 6 carbon atoms or arylalkyl selected from benzyl, phenylethyl and phenylpropyl;R.sub.3 is hydrogen or lower alkyl of up to 6 carbon atoms;R.sub.4 is hydrogen or lower alkyl of up to 6 carbon atoms, or when X is oxygen, R.sub.4 together with R.sub.5 can represent --CH.sub.2 --O--;X is a valency bond, --CH.sub.2, oxygen or sulfur;Ar is selected from phenyl, naphthyl, indanyl and tetrahydronaphthyl;R.sub.5 and R.sub.6 are individually selected from hydrogen, fluorine, chlorine, bromine, hydroxyl, lower alkyl of up to 6 carbon atoms, a --CONH.sub.
Abstract: This invention relates to phenylpyrimidone derivatives which have bronchodilator activity. A compound of the invention is N-methyl 1,6-dihydro-6-oxo-2-(2-propoxyphenyl)pyrimidine-5-carboxamide.
Type:
Grant
Filed:
November 14, 1991
Date of Patent:
March 1, 1994
Assignee:
SmithKline & French Laboratories Limited
Abstract: This invention relates to certain salts of leukotriene antagonists and the use of certain amines to form these salts as a means for selectively crystallizing optical isomers of the leukotriene antagonists recited herein.
Abstract: Thienopyrimidine compounds are disclosed as inhibitors of the H.sup.+ K.sup.+ ATPase enzyme useful in the treatment of gastric acid secretion. A compound of the invention is 2-(2-methylphenylamino)-4-(N-methylphenylamino)thieno[3,2-d]pyrimidine.
Type:
Grant
Filed:
November 24, 1992
Date of Patent:
January 18, 1994
Assignee:
SmithKline Beecham Intercredit B.V.
Inventors:
Thomas H. Brown, Robert J. Ife, Colin A. Leach
Abstract: This invention relates to novel protein protease inhibitors as well as DNAs encoding same and vectors and transformed host cells useful for the recombinant production of the inhibitors.
Type:
Grant
Filed:
June 3, 1992
Date of Patent:
January 18, 1994
Assignee:
SmithKline Beecham Corporation
Inventors:
Thomas R. Berka, James A. Fornwald, Joselina G. Gorniak, Martin Rosenberg, James E. Strickler, Dean P. Taylor
Abstract: A compound of formula (I) ##STR1## or a salt thereof, wherein R.sub.1 and R.sub.2 are each independently hydrogen, acyl or phosphate, provided that when one of R.sub.1 or R.sub.2 is phosphate, the other is hydrogen; or R.sub.1 and R.sub.2 are joined together to form a cyclic acetal group, a cyclic carbonate group or a cyclic phosphate group.Processes for preparing these compounds and their use in therapy is also described.
Abstract: The present invention provides antiviral compounds of Formula (I): ##STR1## pharmaceutical compositions prepared therefrom, and methods of treatment of viral infections therewith.
Abstract: A recombinant DNA molecule comprising the Streptomyces gal operon galK gene; galE gene; galT gene; P1 promoter, P2 promoter, P2 promoter expression unit; P1 promoter regulated region; or the entire Streptomyces gal operon.
Type:
Grant
Filed:
October 27, 1992
Date of Patent:
September 7, 1993
Assignee:
SmithKline Beecham Corporation
Inventors:
Craig W. Adams, Mary E. Brawner, James A. Fornwald, Francis J. Schmidt
Abstract: Liposome-forming materials containing a long chain aliphatic or aromatic-based acid or amine, hydrating agents and discrete amounts of water form gels which are useful drug delivery systems and spontaneously form highly stable liposomes in aqueous solution having very high capture efficiency.
Abstract: A process for the preparation of 2,5-diamino-4,6-dichloropyrimidine, which process comprises the chlorination of 2,5-diamino-4,6-dihydroxypyrimidine with phosphorus oxychloride and a quaternary ammonium chloride or a weak tertiary amine base hydrochloride.