Abstract: A compound of formula (I) is obtainable by the cultivation of a microorganism from the genus Streptomyces, such as Streptomyces NCIMB 40515. In the presence of rapamycin, and recovery thereof from the culture medium. The compound, and pharmaceutical compositions containing it, is useful as an immunomodulatory agent, as an anticancer agent, or in the treatment of microbial infections in animals including humans.
Abstract: A non-aqueous, chewable composition for oral delivery of unpalatable drugs is provided. The composition contains the drug intimately dispersed or dissolved in a pharmaceutically acceptable lipid that is solid at room temperatures. The composition also has a matrix that contains a granulating agent for the total composition and a rapid dispersal agent and optionally additives such as buffering agents, flavoring agents, surfactants and the like.
Type:
Grant
Filed:
July 14, 1995
Date of Patent:
January 28, 1997
Inventors:
Sushil Chauhan, Gordon France, John Buehler
Abstract: This invention comprises a process for preparing benzopyran derivatives represented by formula (I) ##STR1## in which, R.sup.1 is C.sub.1-20 alkyl, C.sub.2-20 alkenyl, C.sub.2-20 alkynyl, or a group of structure (i), (ii) or (iii).
Type:
Grant
Filed:
May 26, 1995
Date of Patent:
January 21, 1997
Assignee:
SmithKline Beecham Plc
Inventors:
Graham Johnson, Neil Smith, Graham R. Geen, Inderjit S. Mann, Vance Novack
Abstract: The invention describes a process for the preparation of the polymorph A form of a compound having the structure ##STR1## which involves triturating, crystallizing, or precipitating crude N-t-butyl-androst-3,5-diene-17.beta.-carboxamide-3-carboxylic acid from an ethyl acetate or t-butyl methyl ether solvent, followed by isolation of the polymorph A.
Type:
Grant
Filed:
December 2, 1994
Date of Patent:
January 21, 1997
Assignee:
SmithKline Beecham Corporation
Inventors:
Neil H. Baine, Neville L. Holder, Donald N. Klein, Robert L. Webb, Gary E. Zuber
Abstract: Two further crystalline polymorphic forms of the anti-infective agent mupirocin have been identified. Processes for the preparation thereof and the use thereof are described.
Type:
Grant
Filed:
April 18, 1995
Date of Patent:
January 14, 1997
Assignee:
SmithKline Beecham Group p.l.c.
Inventors:
Michael J. Greenway, Sarah D. Salt, Christopher E. Valder, Alan D. Curzons
Abstract: This invention relates to a novel, multisegmented nozzle for dispensing viscous materials, particularly for dispensing differently colored toothpaste into toothpaste tubes so as to produce toothpaste of striped appearance when dispensed from the tube. The nozzle has a tubular body defined by an outer body wall, and has within the tubular body a central channel and a plurality of longitudinal first and second side channels situated around the central channel. The first side channels have a cross section which narrows towards the central channel; the second side channels have a rectangular cross section. Because of this configuration the nozzle is able to load multicolored toothpaste tubes which dispense toothpaste in a substantially more uniform striped pattern than conventionally loaded multicolored toothpaste tubes.
Abstract: Invented are substituted azaspirane compounds, pharmaceutical compositions containing these compounds, and methods for using these compounds to induce an immunosuppressive effect in a mammal in need thereof.
Type:
Grant
Filed:
July 19, 1994
Date of Patent:
January 7, 1997
Assignee:
SmithKline Beecham Corporation
Inventors:
Alison M. Badger, Gary J. Bridger, David A. Schwartz
Abstract: A compound of the formula A.sup.1 --X--(CH.sub.2).sub.n --O--A.sup.2 --A.sup.3 --CO.R.sup.2 (I) or a tautomeric form thereof and/or a pharmaceutically acceptable salt thereof, and/or a pharmaceutically acceptable solvate thereof, wherein: A.sup.1 represents a substituted or unsubstituted aromatic heterocyclyl group; A.sup.2 represents a benzene ring having three optional substituents; A.sup.3 represents a moiety of formula --(CH.sub.2).sub.m --CHR.sup.1 -- wherein R.sup.1 represents a halogen atom or a moiety of formula S(O).sub.p A.sup.4 wherein A.sup.4 represents hydrogen, substituted or unsubstituted alkyl, aryl, aralkyl, alkylcarbonyl or an aromatic heterocyclyl group and p represents zero or an integer 1 or 2 and m represents zero or an integer in the range of from 1 to 5, or A.sup.3 represents a moiety of formula --CH.dbd.CR.sup.1 -- wherein R.sup.1 is as defined above; R.sup.2 represents OR.sup.3 wherein R.sup.3 represents hydrogen, alkyl, aryl or aralkyl, or R.sup.2 represents --NR.sup.4 R.sup.
Abstract: A process for preparing substituted benzopyran derivatives which comprises a final step cyclisation of the corresponding open-chain intermediates.
Type:
Grant
Filed:
May 26, 1995
Date of Patent:
December 24, 1996
Assignee:
SmithKline Beecham PLC
Inventors:
Graham Johnson, Neil Smith, Graham R. Geen, Inderjit S. Mann, Vance Novack
Abstract: A compound of formula (I), or a salt or solvate thereof, ##STR1## in which R.sub.1 and R.sub.2 each independently represents hydrogen, alkyl, optionally substituted aryl or optionally substituted aralkyl; R.sub.3 represents alkyl, optionally substituted aryl or optionally substituted aralkyl and R.sub.4 represents alkyl or optionally substituted aryl; a process for preparing such compounds and the use of such compounds for resolving certain racemates.
Type:
Grant
Filed:
May 8, 1995
Date of Patent:
December 10, 1996
Assignee:
Les Laboratoires Beecham S.A.
Inventors:
Eric Brown, Jo el Touet, Jean-Pierre Le Goff
Abstract: The use of a compound of formula (I) or pharmaceutically acceptable salt thereof, in which X.sub.1 --(CH.sub.2).sub.x --X.sub.2 forms a 5-7 membered ring wherein: X.sub.1 is O or S; X.sub.2 is O, S, NR or NRCO wherein R is hydrogen or C.sub.1-6 alkyl; x is 1, 2 or 3; Y is O or NH; Z is sub-formula (a), (b) or (c) in the manufacture of a medicament for use in the treatment of gastrointestinal disorders, cardiovascular disorders and CNS disorders.
Type:
Grant
Filed:
July 28, 1994
Date of Patent:
December 3, 1996
Assignee:
SmithKline Beecham p.l.c.
Inventors:
Francis D. King, Laramie M. Gaster, Keith R. Mulholland, Shirley K. Rahman, Paul A. Wyman, Gareth J. Sanger, Kay A. Wardle, Gordon S. Baxter, Guy A. Kennett, Alberto J. Kauman
Abstract: The present invention provides mammalian cells modified to stably express at least the entire human immunodeficiency virus-1 envelope protein gp160. The invention provides a vaccine comprising the cells of the invention. The invention also provides methods for screening compounds for their ability to inhibit formation of syncytia between cells that express HIV-1 gp160 and cells that express CD4 comprising mixing cells of invention, cells that express CD4 on their surfaces, and a test compound for a length of time sufficient for syncytia to form; and then determining the amount of syncytia formation.
Type:
Grant
Filed:
June 2, 1995
Date of Patent:
December 3, 1996
Assignee:
SmithKline Beecham Corporation
Inventors:
Zdenka L. Jonak, Christine Debouck, Robert Clark, Stephen Trulli
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.