Abstract: Novel compounds of Formulas (I) and (II) ##STR1## are described herein. These compounds inhibit the production of Tumor Necrosis Factor and are useful in the treatment of disease states mediated or exacerbated by TNF production; these compounds are also useful in the mediation or inhibition of enzymatic or catalytic activity of phosphodiesterase IV.
Type:
Grant
Filed:
September 29, 1994
Date of Patent:
September 12, 1995
Assignee:
SmithKline Beecham Corporation
Inventors:
Siegfried B. Christensen, IV, Paul E. Bender, Cornelia J. Forster, John G. Gleason
Abstract: Tetrahydrobenzothienopyridines of formula (I), ##STR1## wherein, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.8 and R.sub.9 are as defined in the specification and pharmaceutical compositions containing such compounds are of use in treating anxiety, convulsion and sleep disorders.
Type:
Grant
Filed:
February 10, 1994
Date of Patent:
September 5, 1995
Assignee:
SmithKline Beecham p.l.c.
Inventors:
David T. Davies, Ian T. Forbes, Mervyn Thompson
Abstract: Substituted quinoline derivatives are described as inhibitors bone resorption with in particular, the compound 1-(2-methylphenyl)imidazo[4,5-c]quinoline hydrochloride.
Type:
Grant
Filed:
December 10, 1990
Date of Patent:
May 30, 1995
Assignee:
Smith Kline & French Laboratories Limited
Inventors:
Thomas H. Brown, Robert J. Ife, Colin A. Leach, David J. Keeling
Abstract: The present invention relates to N-pyridylamidine and N-pyridylguanidine derivatives of general formula (I) in which: Ar.sup.1 is an optionally substituted phenyl ring; Ar.sup.2 is an optionally substituted phenyl ring; R.sup.1 is hydrogen or C.sub.1-4 alkyl; R.sup.2 is hydrogen or C.sub.1-4 alkyl; R.sup.3 is hydrogen or C.sub.1-4 alkyl; R.sup.4 is hydrogen, halogen, C.sub.1-6 alkyl or C.sub.1-6 alkoxy; X is CH.sub.2 or NR.sup.5, and R.sup.5 is hydrogen or C.sub.1-4 alkyl, and the salts thereof, and their use in therapy as gastric acid secretion inhibitors.
Type:
Grant
Filed:
July 20, 1994
Date of Patent:
April 25, 1995
Assignee:
SmithKline Beecham Intercredit B.V.
Inventors:
Robert J. Ife, Colin A. Leach, Dashyant Dhanak
Abstract: This invention relates to a new antioxidant use of, and method of treatment using certain hydroxycarbazole compounds or a pharmaceutically acceptable salt thereof. More specifically, the compounds are useful for the prevention of oxidative tissue damage to organs, particularly the central nervous system including the brain, in mammals afflicted with disease-induced ischemic trauma, particularly stroke.
Type:
Grant
Filed:
September 28, 1993
Date of Patent:
April 11, 1995
Assignee:
SmithKline Beecham Corporation
Inventors:
Frank C. Barone, Giora Feuerstein, Tian-Li Yue
Abstract: An improved surface plasmon resonance detector, capable of recovering a desired eluted ligate allows for the collection and subsequent analysis of ligate solutions following interaction of the ligate with an immobilized ligand on a surface of a sensor chip of the surface plasmon resonance detector, permits the isolation and characterization of novel ligates and ligands.
Type:
Grant
Filed:
July 6, 1993
Date of Patent:
March 7, 1995
Assignee:
SmithKline Beecham Corporation
Inventors:
Michael Brigham-Burke, Daniel J. O'Shannessy
Abstract: The present invention provides a new medical use of the hydroxycarbazole compounds of Formula (I), preferably the hydroxylated metabolites of 1-(carbazol-4-yloxy-3-[[2-(o-methoxyphenoxy)ethyl]amino]-2-propanol)(carve dilol), for inhibiting the migration and proliferation of smooth muscle cells. In particular, the present invention provides a new use for the hydroxycarbazole compounds of Formula (I) for prevention of restenosis following percutaneous transluminal coronary angioplasty (PTCA), suppression of the progression of vascular hypertrophy associated with hypertension, and prevention of development of atherosclerosis. ##STR1## wherein: R.sub.1 -R.sub.9 are independently --H or --OH, with the proviso that a at least one of R.sub.1 -R.sub.9 is OH.
Abstract: Novel oxamide derivatives are described which inhibit the production of TNF and are useful in the treatment of disease states mediated or exacerbated by TNF production. The compounds of the present invention are also useful as inhibitors of PDE IV and are therefor useful in the treatment of disease states mediated or exacerbated thereby.
Type:
Grant
Filed:
March 2, 1993
Date of Patent:
February 28, 1995
Assignee:
SmithKline Beecham Corporation
Inventors:
Paul E. Bender, Siegfried B. Christensen, IV, Klaus M. Esser, Cornelia J. Forster, Michael D. Ryan, Philip L. Simon
Abstract: A douche nozzle has an internal baffle member for regulating the flow of liquid exiting the nozzle. The nozzle may be provided with spaced apart grooves on its exterior surface extending from the distal end of the nozzle to and across an internally threaded open base.
Type:
Grant
Filed:
August 19, 1993
Date of Patent:
January 10, 1995
Assignee:
SmithKline Beecham
Inventors:
Robert W. Pritchard, Lawrence J. Stuppi
Abstract: A collapsible container for extrudable viscous fluids comprising a tube, two opposing side walls of the tube being deformable under applied compressive pressure, the tube closed at one end and open at the other, the open end having a nozzle and openable cap means.
Type:
Grant
Filed:
June 2, 1993
Date of Patent:
December 20, 1994
Inventors:
Hans Halm, Manfred Hansen, Stefan Bender
Abstract: Compounds of the formula I ##STR1## wherein R.sub.1 represents ##STR2## and the remainder of the variables are defined in the specification are useful in the treatment and/or prophylaxis of dementia in mammals.
Type:
Grant
Filed:
March 19, 1993
Date of Patent:
November 8, 1994
Assignee:
Beecham Group p.l.c.
Inventors:
Barry S. Orlek, Steven M. Bromidge, Richard E. Faulkner, deceased
Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein: R.sub.1 is --CH.sub.3 or --CH.sub.2 CH.sub.3 unsubstituted or substituted by 1 to 3 fluorines;X is O or S(O).sub.s where s=0 to 2;R.sub.2 is C.sub.4 -C.sub.6 cyclic alkyl, optionally substituted by one to three methyl groups or one ethyl group; --CH.sub.2 -cyclopentyl, --CH.sub.2 -cyclopropyl, 3-tetrahydrofuranyl, C.sub.1-7 alkyl, CH.sub.3 or CH.sub.2 CH.sub.3 substituted by one to three fluorines;--(CH.sub.2).sub.n COO(CH.sub.2).sub.g CH.sub.3, or (CH.sub.2).sub.n O(CH.sub.2).sub.g CH.sub.3, wherein n is 2 to 4 and g is 0 to 2;R.sub.3 represents a moiety of formula (a); ##STR2## wherein R.sub.4 and R.sub.5 each represent hydrogen or R.sub.4 and R.sub.5 together represent a bond;B represents >C.dbd.O, >C.dbd.S or >CH--R.sub.6 wherein R.sub.6 represents H, OH, C.sub.1-6 alkoxy or C.sub.
Abstract: Rapamycin derivatives; pharmaceutical compositions comprising such rapamycin derivatives and pharmaceutically acceptable carriers or excipients; and methods of using such derivatives to inhibit pathogenic fungi growth inhibition, inhibit immunosuppression or treat carcinogenic tumors are disclosed.
Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## 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 OH; a group hydrolysable in vivo to OH or hydrogen; C.sub.1-8 alkoxy; C.sub.2-8 alkenyloxy; C.sub.2-8 alkynyloxy; C.sub.3-8 cycloalkyloxy; or COR.sub.13 wherein R.sub.13 represents hydrogen, C.sub.1-8 alkyl, phenyl or phenyl C.sub.1-4 alkyl; in which any phenyl moiety is optionally substituted by up to 3 substituents independently selected from C.sub.1-6 alkoxy, C.sub.1-6 alkyl, halo, C.sub.1-6 alkoxycarbonyl, cyano, C.sub.1-6 alkylthio or C.sub.1-6 alkylsulphonyl; 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:
April 5, 1993
Date of Patent:
October 18, 1994
Assignee:
Beecham Group p.l.c.
Inventors:
Steven M. Bromidge, Barry S. Orlek, Steven Dabbs
Abstract: The present invention provides antiviral compounds of Formula (I), and pharmaceutically acceptable salts thereof: ##STR1## wherein X is --CH.sub.2 O or --CH.sub.2 ;R.sub.1 is hydroxy or amino;R.sub.2 is hydrogen or amino;R.sub.3 is hydrogen, hydroxymethyl or acyloxymethyl, wherein the acyl group of said acyloxymethyl is selected from the group consisting of C.sub.1-7 alkanoyl and benzoyl optionally substituted in the phenyl ring by one, two or three substituents selected from the group consisting of fluoro, chloro, bromo, C.sub.1-4 alkyl and C.sub.1-4 alkoxy, wherein the alkyl moiety of said C.sub.1-4 alkyl and C.sub.1-4 alkoxy substituents is selected from the group consisting of methyl, ethyl, n- and iso-propyl, n-, sec-, iso- and tert-butyl,R.sub.4 is a group of formula: ##STR2## wherein R.sub.5 and R.sub.6 are independent selected from hydrogen, C.sub.1-6 alkyl and phenyl optionally substituted by one, two or three substituents selected from the group consisting of fluoro, chloro, bromo, C.sub.