Abstract: The invention is directed to a pharmaceutical composition comprising a cream base which comprises mupiricin dihydrate, a mineral oil, one or more fatty alcohols or fatty esters, a polyoxyethylene ether or ester surfactant, xanthan gum, water and a method for treating a bacterial infection using said composition.
Abstract: A method of treating topical anti-bacterial infections which comprises the separate, simultaneous or sequential administration to a patient in need thereof an effective amount of mupirocin or a salt thereof and chlorhexidine or a salt thereof.
Abstract: A pharmaceutical granular composition and method are provided for masking the taste of unpleasant tasting drugs, wherein drug cores are coated with separate layers of aqueous dispersions of methacrylate ester copolymers, preferably, poly(ethylacrylate, methyl methacrylate) to which quaternary ammonium groups have been introduced to modify the permeability of the ester. Additionally, the coating composition may contain plasticizers and conventional excipients. The coating system releases drug by diffusion and is influenced by drug solubility and media pH. The coated pharmaceutical granules of the invention can be used to prepare chewable tablets with good palatability and bioavailability.
Abstract: A process for solubilising an alpha-glucan containing foodstuff which comprises processing a carbohydrate-containing material having a moisture content of less than 40% by weight in an extruder under severe conditions of mechanical disruption and shear at high screw speed. The solubility of the extrudate after milling is greater than 55% by weight in water. Novel soluble alpha-glucan components of the extrudate are provided having a ratio of greater than 1 for the amount of alpha-glucan having a degree of polymerisation greater than 50 to the amount of alpha-glucan with a degree of polymerisation less than 50. Food drinks comprising ingredients produced using the process are described.
Abstract: Novel compounds of Formula (I) ##STR1## where X.sub.4 is a substituted cyclohexane or cyclohexane group and the other radicals are defined 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. The compounds of the present invention are also useful in the mediation or inhibition of enzymatic or catalytic activity of phosphodiesterase IV and are therefore useful in the treatment of disease states in need of mediation or inhibition thereof.
Abstract: The present invention provides a process for the asymmetric synthesis of camptothecin analogues as well as novel chemical intermediates of Formula I, II, and III. In general, the present process comprises conversion of a cis dioxolanone, having the same desired absolute configuration as the desired camptothecin analogue, to a compound of Formula I, II, or III, which compound is then converted to the desired camptothecin analogue.
Abstract: A process for preparing a compound of structure (I) or a hydrate or solvate thereof in which R.sup.1 is C.sub.1-6 alkyl, optionally substituted phenyl or optionally substituted phenylC.sub.1-6 alkyl, which comprises reacting an azide of the structure (II): M.sup..sym. N.sub.3.sup..crclbar. with a cyanoformate of the structure (III): NC.CO.sub.2 R.sup.1 in which M is an alkali metal atom, and R.sup.1 is as described for structure (I), to form an intermediate salt of structure (IV), in which R.sup.1 is as described for structure (I) and M is as described for structure (II) followed by conversion of the salt (IV) to the free tetrazole (I) or to a hydrate or solvate thereof.
Type:
Grant
Filed:
August 1, 1995
Date of Patent:
June 11, 1996
Assignee:
SmithKline Beecham PLC
Inventors:
Vance Novack, Neal Ward, John C. Hanson
Abstract: Compounds of formula (I), ##STR1## wherein R.sup.1 represents C.sub.1-4 alkyl; and R.sup.2, R.sup.3, R.sup.4 and R.sup.5 each independently represent hydrogen, halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkoxyC.sub.1-4 alkyl, C.sub.1-4 alkylsulphonyl, trifluoromethylsulphonyl; optionally substituted arylsulphonyl, optionally substituted heteroarylsulphonyl, optionally substituted aralkylsulphonyl, optionally substituted heteroaralkylsulphonyl, nitro, cyano, amino, mono- or di-alkylamino, trifluoromethyl, trifluoromethoxy, hydroxyl, hydroxyalkyl, C.sub.1-4 alkylthio, C.sub.1-4 alkanoyl, C.sub.1-4 alkoxycarbonyl, aminosulphonyl, alkylaminosulphonyl or dialkylaminosulphonyl; or R.sup.1 and R.sup.2 together form a linking chain-(CH.sub.2).sub.m Op (wherein m is 2 to 4 and p is zero or 1) which chain may be optionally substituted by one or two C.sub.1-4 alkyl groups; and Y represents a group selected from (a) or (b) wherein R.sup.6 and R.sup.7 independently represent hydrogen, C.sub.
Type:
Grant
Filed:
February 3, 1995
Date of Patent:
June 4, 1996
Assignee:
SmithKline Beecham PLC
Inventors:
Geoffrey Stemp, Michael S. Hadley, David J. Nash, Christopher N. Johnson
Abstract: A compound of formula (I) or a salt thereof: ##STR1## Wherein: P represents a quinoline or isoquinoline residue; R.sub.1 is hydrogen or C.sub.1-6 alkyl; R.sub.2, R.sub.3, R.sub.10, R.sub.11 are independently hydrogenR.sub.1 is hydrogen or C.sub.1-6 alkyl; R.sub.2, R.sub.3, R.sub.10, R.sub.11 are independently hydrogen or C.sub.1-6 alkyl, or R.sub.10 and R.sub.11 together form a bond, or R.sub.2 and R.sub.10 or R.sub.3 and R.sub.11 together form a C.sub.2-6 alkylene chain. R.sub.4 is hydrogen, C.sub.1-6 alkyl, halogen, NR.sub.8 R.sub.9, OR.sub.12 or COOR.sub.12, where R.sub.8 R.sub.9 and R.sub.12 are independently hydrogen or C.sub.1-6 alkyl; R.sub.5 and R.sub.6 are independently hydrogen or C.sub.1-6 alkyl; and R.sub.7 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or halogen; and wherein the urea moiety is attached at the 4-, 5- or 6-position of the indoline ring, which has been found to have 5HT.sub.1c receptor antagonist activity.
Type:
Grant
Filed:
August 30, 1994
Date of Patent:
April 16, 1996
Assignee:
SmithKline Beecham, p.l.c.
Inventors:
Ian T. Forbes, Roger T. Martin, Graham E. Jones
Abstract: This invention relates to a process for producing a heterologous polypeptide in Streptomyces which involves transforming a Streptomyces organism with a recombinant DNA molecule comprising an LEP-10 of LTl sequence selected from the group consisting of a sequence encoding a gene expression unit, a promoter sequence or an export control encoding sequence each operatively linked to a heterologous coding sequence and then culturing the transformed Streptomyces such that the heterologous polypeptide is expressed.
Type:
Grant
Filed:
December 3, 1993
Date of Patent:
March 12, 1996
Assignee:
SmithKline Beckman Corporation
Inventors:
Thomas R. Berka, James A. Fornwald, Joselina G. Gorniak, Martin Rosenberg, James E. Strickler, Dean P. Taylor
Abstract: The present invention provides a process for the asymmetric synthesis of camptothecin analogs as well as novel chemical intermediates of Formula I, II, and III. In general, the present process comprises conversion of a cis dioxolanone, having the same desired absolute configuration as the desired camptothecin analog, to a compound of Formula I, II, or III, which compound is then converted to the desired camptothecin analog.
Type:
Grant
Filed:
December 23, 1994
Date of Patent:
November 21, 1995
Assignee:
SmithKline Beecham Corporation
Inventors:
Joseph Fortunak, John Kitteringham, Nicholas Sisti, Jeffery Wood
Abstract: A new use of, and method of treatment of atherosclerosis 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: Novel cyclohexanes of Formulas (I) and (II) ##STR1## are described herein. They 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 V.
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