Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof, and the use of a compound of formula (I) or a pharmaceutically acceptable salt thereof:X--CO--CH.sub.2 --Z (I)whereinX is a monocyclic or polycyclic aromatic group,Z is of a linear, cyclic or bicyclic, aromatic or aliphatic moiety containing a nitrogen atom;and their use as pharmaceuticals in the treatment of gastrointestinal disorders, cardiovascular disorders and CNS disorders.
Type:
Grant
Filed:
January 26, 1998
Date of Patent:
September 5, 2000
Assignee:
SmithKline Beecham plc
Inventors:
Francis David King, Laramie Mary Gaster, Keith Raymond Mulholland
Abstract: A process for the preparation of SB 207266 or a pharmaceutically acceptable salt thereof, which process comprises the reaction of N-(1-.sup.n butyl-4-piperidyl)methylamine with a compound of formula (A), ##STR1## wherein R is alkyl.
Type:
Grant
Filed:
February 16, 1999
Date of Patent:
August 8, 2000
Assignee:
Smithkline Beecham plc
Inventors:
Michael Fedouloff, Gillian Elizabeth Smith, David William Guest, John Bryce Strachan
Abstract: The invention relates to sulphonamide compounds of formula (I) or a salt thereof having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of CNS disorders, wherein: Ar is an optionally substituted mono- or bicyclic aromatic or heteroaromatic ring; Ar' is an optionally substituted mono- or bicyclic aromatic or heteroaromatic ring; R.sup.1 is C.sub.1-6 alkyl or together with the group R.sup.3 form a 5-8 membered ring containing one or two heteroatoms optionally substituted by C.sub.1-6 alkyl; R.sup.2 is hydrogen or C.sub.1-6 alkyl; R.sup.3 is hydrogen, C.sub.1-6 alkyl or together with the group R.sup.1 form a 5-8 membered ring containing one or two heteroatoms optionally substituted by C.sub.1-6 alkyl; R.sup.4 is hydrogen or C.sub.1-6 alkyl; R.sup.5 and R.sup.6 are independently hydrogen or C.sub.1-6 alkyl; p is 1, 2 or 3; q is 1 to 3; and r is 1 or 2.
Type:
Grant
Filed:
June 23, 1999
Date of Patent:
February 15, 2000
Assignee:
SmithKline Beecham plc
Inventors:
Ian Thomson Forbes, Shirley Katherine Rahman
Abstract: A compound of formula (I) or a salt thereof, or a solvate thereof, ##STR1## wherein: R.sub.1 represents an alkyl group or a substituted or unsubstituted aryl group; R.sub.2, R.sub.3 and R.sub.4 each independently represent hydrogen, alkyl, aryl or substituted aryl; R.sub.5 and R.sub.6 each independently represent hydrogen, hydroxy, amino, alkoxy, optionally substituted aryloxy, optionally substituted benzyloxy, alkylamino, dialkylamino, halo, trifluoromethyl, trifluoromethoxy, nitro, alkyl, carboxy, carbalkoxy, carbamoyl, alkylcarbamoyl, or R.sub.5 and R.sub.6 together represent methylenedioxy, carbonyldioxy or carbonyldiamino; X represents a hydroxy or an alkoxy group wherein the alkyl group may be substituted or unsubstituted or X represents a group NR.sub.S R.sub.t wherein R.sub.S and R.sub.
Abstract: This invention relates to novel compounds of Formula (II), and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).
Type:
Grant
Filed:
April 16, 1999
Date of Patent:
January 18, 2000
Assignee:
SmithKline Beecham Corporation
Inventors:
Katherine L. Widdowson, Hong Nie, Melvin Clarence Rutledge, Jr.
Abstract: The present invention relates to libraries of compounds based upon a N-(4-alkoxyphenyl)-N-acyl-benzylamine, N-(4-alkoxyphenylmethyl)-N-acyl-benzylamine and N-[2-(4-alkoxyphenyl)ethyl]-N-acyl-benzylamine template, to processes for the preparation of such libraries and their use as a screening tool in biological assays for identifying new chemical leads.
Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## and their use as pharmaceuticals in the treatment of gastrointestinal disorders, cardiovascular disorders and CNS disorders.
Abstract: Compounds of formula (I), are selective delta opioid agonsist and antagonists, and are useful as analgesics and in treating general neurologic disorders.
Abstract: The present invention relates to the use of halofantrine free base in the treatment of malarial infections. In particular, lipid-based formulations for oral and injectable use are disclosed.
Type:
Grant
Filed:
October 15, 1997
Date of Patent:
October 19, 1999
Assignee:
Smithkline Beecham p.l.c.
Inventors:
William Neil Charman, Christopher John Hamilton Porter
Abstract: According to the present invention, there is provided a compound, or a solvate or salt thereof of formula (I): ##STR1## Substituted hydroisoquinoline derivatives are potent and selective delta opioid agonists and antagonists and are of potential therapeutic utility as inter alia analgesics.
Abstract: A compound, or solvate or salt thereof, of formula (I) ##STR1## in which, R.sub.1 and R.sub.2, are, independently hydrogen, linear or branched C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkenyl, or C.sub.3-6 alkenyl, or together form a C.sub.3-7 alkyl;R.sub.3 and R.sub.4 are, independently, hydrogen, linear or branched C.sub.1-6 alkyl, or R.sub.4 is oxygen forming with the carbon atom to which is attached a C.dbd.O group;R.sub.5 is hydrogen, hydroxy, or C.sub.1-3 alkoxy;R.sub.6 is halogen, NH.sub.2 or a para or meta --COR-8 group, in which R.sub.8 is C.sub.1-8 -alkyl, C.sub.1-8 -alkoxy or NR.sub.9 R.sub.10, wherein R.sub.9 and R.sub.10, are, independently, hydrogen, straight or branched C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl or phenyl; or R.sub.6 is a para or meta group ##STR2## in which R.sub.11 and R .sub.12 are, independently, hydrogen or straight or branched C .sub.1-6 and,R.sub.7 is hydrogen, or straight or branched C.sub.1-8 alkyl; is provided.
Abstract: The use of a compound of formula (I) or a pharmaceutically acceptable salt thereof for the treatment of artrial arrhythmia, stroke or CNS disordersX--CO--CH.sub.2 --Z (I)whereinX is a monocyclic or polycyclic aromatic group,Z is of sub-formula (h), (j) or (k): ##STR1## and wherein the remaining variables are as defined herein.
Type:
Grant
Filed:
January 26, 1998
Date of Patent:
February 16, 1999
Assignee:
SmithKline Beecham p.l.c.
Inventors:
Francis David King, Laramie Mary Gaster, Keith Raymond Mulholland
Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## and their use as pharmaceuticals in the treatment of gastrointestinal disorders, cardiovascular disorders and CNS disorders.
Abstract: Compounds of formula (I), processes for their preparation and their use in medicine are disclosed: ##STR1## wherein: P represents phenyl, a quinoline or isoquinoline residue, or a 5-membered or 6-membered aromatic heterocyclic ring containing up to three heteroatoms selected from nitrogen, oxygen or sulphur;R.sup.1 is hydrogen, C.sub.1-6 alkyl, halogen, CF.sub.3, NR.sup.7 R.sup.8 or OR.sup.9 where R.sup.7, R.sup.8 and R.sup.9 are independently hydrogen, C.sub.1-6 alkyl or arylC.sub.1-6 alkyl;R.sup.2 is hydrogen or C.sub.1-6 alkyl;R.sup.3 is C.sub.1-6 alkyl;n is 0 to 3;m is 0 to 4; andR.sup.4 groups are independently C.sub.1-6 alkyl optionally substituted by one or more halogen atoms, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl, C.sub.3-6 cycloalkyl-C.sub.1-6 alkyl, C.sub.1-6 alkylthio, C.sub.3-6 cycloalkylthio, C.sub.3-6 cycloalkylC.sub.1 C.sub.6 alkylthio, halogen, nitro, CF.sub.3, OCF.sub.3, SCF.sub.3, SO.sub.2 CF.sub.3, SO.sub.2 F, formyl, C.sub.
Type:
Grant
Filed:
September 23, 1996
Date of Patent:
November 10, 1998
Assignee:
SmithKline Beecham p.l.c.
Inventors:
Peter Ham, Graham Elgin Jones, Ian Thomson Forbes