Abstract: A novel cytosolic 58 kd phosphoprotein induced during bone marrow stem cell (BM) differentiation into dendritic cells (DC) during in vitro cultivation with the cytokine GM-CSF by addition of antisera to an 82 kd BM cell surface protein generating cultivatable dendritic progenitor cells (DP). Genes, methods for preparing them as well as early DP have been provided. Potential uses/advantages lie in the study of BM differentiation and innate immunity due to stimulatory/inhibitory DC, contribution of BM and DP to inflammation during infection and carcinogenesis, tumor promotion/regression, identification of BM-derived blood cells, T-cell activation/regulation/tolerance and inflammation.
Abstract: Solid phase combinatorial synthesis is carried out in a multi-reactor synthesizer comprising an array of separate reactor cells (1-9) containing a solid reaction support medium (26). Subsets of the reactor cells (1-9) are interconnected with one another in a desired pattern, and, in a first reaction step, reagents (A, B, C) are circulated through the subsets. After the first reaction step is completed, the reactor cells (1-9) are rearranged into a new configuration of the subsets, and the same, or other, reagents (A, B, C) are circulated through the new subsets. The process can be repeated to produce large numbers of compounds differing from one another.
Type:
Grant
Filed:
November 20, 1998
Date of Patent:
May 1, 2001
Assignee:
SmithKline Beecham Corporation
Inventors:
Michael Lee Moore, Dennis Shinji Yamashita
Abstract: Novel pyridines, pyrimidines, pyrazines, pyridazines and triazines, pharmaceutical compositions containing these compounds and their use as endothelin receptor antagonists are described.
Type:
Grant
Filed:
September 27, 1996
Date of Patent:
August 24, 1999
Inventors:
John Duncan Elliott, Deborah Lynne Bryan
Abstract: "Paroxetine hydrochloride (I) anhydrate ##STR1## free of bound propan-2-ol, and various forms thereof, are useful in the treatment of depression and other disorders for which administration of selective serotonin reuptake inhibitors are indicated.
Abstract: Novel indole, indoline and quinoline derivatives of formula (I) processes for their preparation, pharmaceutical compositions containing them, and their use in medicine is disclosed. A structurally distinct class of compounds have now been discovered and have been found to exhibit 5HT.sub.1-D antagonist activity. In a first aspect, the present invention therefore provides a compound of formula (I) or a salt thereof, in which P is a 5-7-membered heterocyclic ring containing 1 to 3 heteroatoms selected from oxygen, nitrogen or sulphur, A, B, m, R.sup.1 -R.sup.8 are defined in the application.
Abstract: "Paroxetine hydrochloride (I) anhydrate ##STR1## free of bound propan-2-ol, and various forms thereof, are useful in the treatment of depression and other disorders for which administration of selective serotonin reuptake inhibitors are indicated.
Abstract: A process for preparing clavulanic acid and other clavam derivatives using an enzyme system from Streptomyces, particularly S. Clavuligerus.
Type:
Grant
Filed:
August 25, 1995
Date of Patent:
February 9, 1999
Assignee:
SmithKline Beecham p.l.c.
Inventors:
Keith Howard Baggaley, Neville Hubert Nicholson, Stephen William Elson, Jeffrey Edwards, Alison Jane Earl, William Henry Holms, David Michael Mousdale, Jack Edward Baldwin, Christopher Schofield
Abstract: The invention provides alaS polypeptides and DNA (RNA) encoding alaS polypetides and methods for producing such polypeptides by recombinant techniques. Also provided are methods for utilizing alaS polypeptides to screen for antibacterial compounds.
Abstract: Polymorph "A" a novel polymorphic form of N-t-butyl-androst-3,5-diene-17.beta.-carboxamide-3-carboxylic acid. Novel processes for preparing polymorph "A" are also disclosed.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
January 12, 1999
Assignee:
SmithKline Beecham Corporation
Inventors:
Neil Howard Baine, Neville Lewis Holder, Donald Nathaniel Klein, Robert Lee Webb, Gary Edward Zuber
Abstract: A process for preparing a compound of formula (I), wherein n is 2 or 3; which process comprises reducing a compound of formula (II), wherein R.sup.1 is hydrogen or C.sub.1-4 alkyl and n is 2 or 3; by catalytic hydrogenation in the presence of a rhodium catalyst.
Abstract: The present invention relates to paroxetine hydrochloride anhydrate substantially free of bound propan-2-ol, several forms of the above, processes for preparing the above, new intermediates useful in preparing the above and methods of treating and/or preventing certain diseases by administering the compounds of the invention to a patient in need thereof.
Abstract: Chimeric, humanized and other IL-5 mAbs, derived from high affinity neutralizing mAbs, pharmaceutical compositions containing same, methods of treatment and diagnostics are provided.
Type:
Grant
Filed:
September 30, 1997
Date of Patent:
December 22, 1998
Assignee:
SmithKline Beecham Corporation
Inventors:
Robert S. Ames, Jr., Edward Robert Appelbaum, Irwin M. Chaiken, Richard M. Cook, Mitchell Stuart Gross, Stephen Dudley Holmes, Lynette Jane McMillan, Timothy Wayne Theisen
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: This invention relates to compounds which are effective for inhibiting platelet aggregation, pharmaceutical compositions for effecting such activity, a method for inhibiting platelet aggregation and clot formation in a mammal, and a method for inhibiting reocclusion of a blood vessel following fibrinolytic therapy.
Abstract: A pharmaceutical granular composition and method for taste masking bitter, or unpleasant tasting drugs comprising a drug core of a nonsteriodal anti-inflammatory drug, and as a taste masking agents, methacrylate ester copolymers. The method comprises coating the drug cores with separate layers of aqueous dispersions of the copolymers. Additionally, the coating composition may contain plasticizers and conventional excipients. The granules of the present invention can be used in the preparation of chewable tablets which have good palatability and bioavailability. Preferable copolymers are poly(ethylacrylate, methylmethacrylate) to which quaternary ammonium groups have been introduced to modify the permeability of the ester. The coating system of this invention releases the drug by diffusion and is influenced by drug solubility and media pH.
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
Abstract: The invention provides compounds of the general formula (I):A.sup.1 --B.sup.1 --X.sup.1 --(CH.sub.2).sub.m --(CON(R.sub.1)).sub.r --(CH.sub.2).sub.s --Y.sup.1 --(CH.sub.2).sub.s --(N(R.sub.1)CO).sub.r --(CH.sub.2).sub.n --X.sup.1 --B.sup.1 --A.sup.1The compounds of this invention are also illustrated by the Formula (II):A.sup.2 --B.sup.2 --X.sup.2 --(CH.sub.2).sub.m --(N(R.sub.1)CO).sub.r --(CH.sub.2).sub.s --Y.sup.2 --(CH.sub.2).sub.s --(CON(R.sub.1)).sub.r --(CH.sub.2).sub.n --X.sup.2 --B.sup.2 --A.sup.2The compounds have hemoregulatory activities and can be used to stimulate haematopoiesis and for the prevention and treatment of viral, fungal and bacterial infectious diseases.
Type:
Grant
Filed:
January 30, 1996
Date of Patent:
November 3, 1998
Assignees:
SmithKline Beecham Corporation, Nycomed Pharma AS
Inventors:
Pradip Kumar Bhatnagar, Dirk Heerding, Peter Martin Fischer
Abstract: Invented are methods of transporting quantities of potassium clavulanate. Also invented are methods of forming a uniform continuous waxy barrier around medicament particles.
Type:
Grant
Filed:
May 25, 1995
Date of Patent:
October 27, 1998
Assignee:
SmithKline Beecham Corporation
Inventors:
Nageswara R. Palepu, Gopadi M. Venkatesh