Abstract: A process for removing osmium from an aqueous solution of nucleosides comprising adding hydrogen sulfide, an aromatic pi base such as pyridine, and a mineral acid. The osmium is precipitated out of solution.
Type:
Grant
Filed:
May 14, 1993
Date of Patent:
August 1, 1995
Assignee:
Glaxo Group Limited
Inventors:
Brian L. Bray, Maynard E. Lichty, John J. Partridge, John P. Turnbull
Abstract: A bottle having an inserted tube in its neck to effectively reduce its interior volume and allow a large surface area for the bottle exterior, e.g. for supporting a large label or to allow oversized print, with a relatively small interior volume, e.g. to prevent abrasions caused by the interior contents moving excessively against each other.
Abstract: Compounds of the following formula (I): ##STR1## where R.sup.1 and R.sup.2 are alkyl or cycloalkyl, which may be substituted, R.sup.4 is aryl such as phenyl which may be substituted, L is a direct bond or an oxygen containing linking group, R is a hydrogen, alkyloxy, alkyl, halogen or haloalkyl and Het is a pyridinyl or pyridazinyl group. The compounds can be used antihypertensives or myocardial relaxants. Also part of the invention are pharmaceutical compositions, intermediates and methods of synthesis.
Abstract: Compounds are described of the formula ##STR1## wherein: R.sup.1 is C.sub.3-6 alkyl or C.sub.1-3 alkylthioC.sub.1-3 alkyl;R.sup.2 is an optionally substituted C.sub.1-6 alkyl or C.sub.1-6 alkoxy group, aryl, heteroaryl, arylC.sub.1-4 alkyl, heteroarylC.sub.1-4 alkyl or a side-chain of a natural .alpha.-amino acid;R.sup.3 is hydrogen, C.sub.1-6 alkyl, CHR.sup.4 COR.sup.5 (where R.sup.4 is a side-chain of a natural .alpha.-amino acid and R.sup.5 is hydroxyl, C.sub.1-6 alkoxy or NHR.sup.6 where R.sup.6 represents a hydrogen atom or a C.sub.1-6 alkyl group) or a group (CH.sub.2).sub.n X (where n is 1 to 6 and X is hydroxyl, C.sub.1-4 alkoxy, heteroaryl or a group NR.sup.7 R.sup.8 where R.sup.7 and R.sup.8 are each hydrogen or C.sub.1-6 alkyl or the group NR.sup.7 R.sup.
Type:
Grant
Filed:
June 29, 1992
Date of Patent:
October 12, 1993
Assignee:
Glaxo Inc.
Inventors:
Peter L. Myers, Andrew B. McElroy, Michael Gregson, Peter J. Brown, Howard G. Davies, David H. Drewry, Michael A. Foley
Abstract: Synthesis of the triol of formula (I) or its amine-protected derivative from a cyclopentene of the formula (II) or its amine-protected derivative: ##STR1## via steps including oxidation to the aldehyde, migration of the double bond, reduction of the aldehyde moiety back to the alcohol grouping and 1,2-cis-dihydroxylation of the double bond.
Type:
Grant
Filed:
October 7, 1991
Date of Patent:
August 3, 1993
Assignee:
Glaxo Group Limited
Inventors:
Brian L. Bray, Maynard E. Lichty, John J. Partridge, John P. Turnbull
Abstract: Pyridazinones of the following formula (I): ##STR1## where R.sup.1 -R.sup.4 are a variety of substituents and L is a linking group, a pharmaceutical composition for treating congestive heart failure, novel intermediates, methods for such treatment and processes for preparing compounds of formula (I).
Type:
Grant
Filed:
September 4, 1991
Date of Patent:
April 20, 1993
Assignee:
Glaxo Inc.
Inventors:
Thomas N. Wheeler, Terrence P. Kenakin, Joel E. Shaffer
Abstract: Cobalt prophyrins of the following formula (l): ##STR1## or a salt or ligand complex thereof and their synthesis, pharmaceutical compositions and use in controlling obesity.
Abstract: A method for detecting the presence or absence of microorganisms in a liquid test sample is provided without need for withdrawing an aliquot or destroying the sample. The method comprises taking near-infrared spectra of the sample and comparing it visually or mathematically to the spectra of a standard, which may be the values of the spectra known to the operator or may be a standard sample that is provided and run side-by-side.
Abstract: A sequential dosing medicament for topical treatment of fungal infections comprising a first pharmaceutical composition having an antifungal agent and an antiinflammatory agent, e.g. a steroid, a second separate pharmaceutical composition having only an antifungal agent as the active ingtredient. Also a method for such sequential dosing, particularly using oxiconazole as the antifungal agent and fluticasone as the steroid.
Type:
Grant
Filed:
March 26, 1991
Date of Patent:
December 29, 1992
Assignee:
Glaxo Inc.
Inventors:
Robert M. Day, Charles E. Holland, George E. Van Lear
Abstract: Pyridones of formula (I) for treating congestive heart failure: ##STR1## wherein: R.sup.1 and R.sup.2 are a variety of phenyl substituents, L is a divalent alkylene linking group. Pharmaceutical composition, methods for their use in treating cardiovascular conditions, processes used in synthesis and intermediates used in such processes.
Type:
Grant
Filed:
June 13, 1991
Date of Patent:
October 6, 1992
Assignee:
Glaxo Inc.
Inventors:
Thomas N. Wheeler, Terrence P. Kenakin, Joel E. Shaffer
Abstract: Pharmaceutical compositions containing cobalt porphyrins of the following formula (I): ##STR1## wherein R.sup.1 =--CH.sub.2 CH.sub.2 CN and R.sup.2 =--CH.sub.2 CH.sub.2 COOH or R.sup.1 and R.sup.2 =--CH.sub.2 CH.sub.2 COOH or R.sup.1 =--H and R.sup.2 =--CH.sub.2 lCH.sub.2 COOH or a salt or ligand complex thereof and their use in controlling obesity.
Abstract: Process for synthesizing 2-aminobenzophenones such as the following formula (I): ##STR1## wherein X.sup.1 and X.sup.2 are substituents and r and s are 1 or 2, by reacting an anthranilic acid amide e.g. an N-alkoxy-N-alkyl anthranilic acid amide, with a halobenzene in the presence of an alkyllithium reagent.
Abstract: Compounds of the following formula (I): ##STR1## where R.sup.1 and R.sup.2 are alkyl or cycloalkyl, which may be substituted, R.sup.4 is aryl such as phenyl which may be substituted, L is a direct bond or an oxygen containing linking group, R is a hydrogen, alkyloxy, alkyl, halogen or haloalkyl and Het is a pyridinyl or pyridazinyl group. The compounds can be used antihypertensives or myocardial relaxants. Also part of the invention are pharmaceutical compositions, intermediates and methods of synthesis.
Abstract: Pyridazinones of the following formula (I): ##STR1## where R.sup.1 -R.sup.4 are a variety of substituents and L is a linking group, a pharmaceutical composition for treating congestive heart failure, novel intermediates, methods for such treatment and processes for preparing compounds of formula (I).
Type:
Grant
Filed:
July 20, 1990
Date of Patent:
March 17, 1992
Assignee:
Glaxo Inc.
Inventors:
Thomas N. Wheeler, Terrence P. Kenakin, Joel E. Shaffer
Abstract: Process for synthesizing 2-aminobenzophenones such as the following formula (I): ##STR1## wherein X.sup.1 and X.sup.2 are substituents and r and s are 1 or 2, by reacting an anthranilic acid amide e.g. an N-alkoxy-N-alkyl anthranilic acid amide, with a halobenzene in the presence of an alkyllithium reagent.
Abstract: A kinetic resolution of pyridazinones of the following formula (A): ##STR1## where R.sup.1 is alkyl by enzymatic hydrolysis results in good optical purity of the phenolic product. This is significant considering the distance in the molecule (A) from the C-5 chiral center to the site of hydrolysis.
Abstract: Pyridones of formula (I) for treating congestive heart failure: ##STR1## wherein: R.sup.1 and R.sup.2 are a variety of phenyl substituents, L is a divalent alkylene or amide containing alkylene linking group. Pharmaceutical composition, methods for their use in treating cardiovascular conditions, processes used in synthesis and intermediates used in such processes.
Type:
Grant
Filed:
August 9, 1990
Date of Patent:
September 24, 1991
Assignee:
Glaxo Inc.
Inventors:
Thomas N. Wheeler, Terrence P. Kenakin, Joel E. Shaffer
Abstract: An efficient synthesis of quanidines, e.g. of the formula (III), by oxidizing a thiourea, e.g. of the following formula (II): ##STR1## with H.sub.2 O.sub.2 and a molybdenum catalyst to yield an aminoiminomethane sulfonic acid which can then be reacted with an amine followed by optional transamination steps.
Type:
Grant
Filed:
July 20, 1987
Date of Patent:
July 25, 1989
Assignee:
McNeilab, Inc.
Inventors:
Cynthia A. Maryanoff, James N. Plampin, Robin C. Stanzione
Abstract: A diastereoselective process for known antidepressive compounds (I) via reduction of the corresponding alcohol (VII): ##STR1## whereby the product mixture of diastereomers is surprisingly and unexpectedly rich in the content of the trans configuration (II) over the cis configuration (III) as defined in the following formulae: ##STR2## The preferred reaction conditions include use of a borane complex as the reducing agent and an acidic solvent such as trifluoroacetic acid.
Type:
Grant
Filed:
February 16, 1988
Date of Patent:
June 6, 1989
Assignee:
McNeilab, Inc.
Inventors:
Bruce E. Maryanoff, Cynthia A. Maryanoff, David F. McComsey, Kirk L. Sorgi