Abstract: The stereospecific cycloaddition of nitrogen containing acetic acid halides or anhydrides with Schiff bases having a carbalkoxy group substituted on the methine carbon atom offers new intermediates and methods for preparing synthetic cephalosporin congeners having antibacterial activity.
Type:
Grant
Filed:
March 14, 1979
Date of Patent:
March 24, 1981
Assignee:
SmithKline Corporation
Inventors:
John G. Gleason, Kenneth G. Holden, William F. Huffman
Abstract: New anthelmintic compounds, compositions and methods of use are described utilizing 5-cycloalkylthio and oxy-2-carbalkoxyaminobenzimidazole. Methods of preparation involve the reaction of 4-cycloalkylthio- or oxy-o-phenylenediamine with methyl cyanocarbamate in aqueous miscible organic solvents.
Abstract: A gelatin capsule unit dosage form containing triamterene, 2,4,7-triamino-6-phenylpteridine, which results in rapid dissolution of the active ingredient. The dosage form comprises the addition of a combination of a surfactant and a carbonate or bicarbonate salt as diluents.
Abstract: 8-Hydroxy-6,7-(2,3-dihydrofuro)-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepin es are prepared by a reaction sequence whose key is a dual cyclization forming the 3-benzazepine ring and fused thereto a dihydrofuran.
Abstract: 7,8-Dihydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines having a halo substituent at the 6-position have potent dopaminergic activity. The 6-chloro congeners are most active.
Abstract: 4-(2-Aminoethyl)-7-hydroxy-2-methyl-2,3-dihydrobenzofuran derivatives having dopaminergic activity are prepared by cyclizing a 2-allyl-3,4-dimethoxyphenethylamine such as by reacting the phenethylamine with hydrogen bromide.
Abstract: A method for preparing 1,2,3,4-tetrahydroisoquinolines comprising heating N-halo or hydroxyethyl-N-benzylamines in an aluminum chloride melt at 160.degree.-210.degree..
Type:
Grant
Filed:
August 10, 1978
Date of Patent:
February 17, 1981
Assignee:
SmithKline Corporation
Inventors:
Bing L. Lam, Wilford L. Mendelson, Charles B. Spainhour, Jr.
Abstract: 3-Allyl-7,8-dihydroxy-6-halo-1-(4-hydroxyphenyl)-2,3,4,5-tetrahydro-1H-3-be nzazepine derivatives are prepared by N-allylation of 7,8-dimethoxy-6-halo-1-(4-methoxyphenyl)-2,3,4,5-tetrahydro-1H-3-benzazepi ne using an allyl halide in acetonitrile in the presence of base followed by O-demethylation. These compounds have a unique cardiovascular effect in that they are potent renal vasodilators and also induce bradycardia.
Abstract: The compounds of this invention are cephalosporine having a 7.beta.-acyloxy group and 7.beta.-hydroxy intermediates for the preparation thereof. The compounds have antibacterial activity.
Abstract: A device for separating a microscope slide into two separate sections has a arm mounted on a horizontal pivot carrying a downwardly extending glass cutter. A releasable member maintains the arm in an elevated position. A slider advances a microscope slide under the cutter releasing the releasable member to lower the cutter onto the microscope slide. A striker on the arm strikes one section of the cut slide to separate it from the other section as the cutter drops off the trailing edge of the slide. The slide then raises the arm for the restoration of the releasable means preferably by a cam attached to the arm. Advantageously, the releasable member is spring biased to its position to maintain the arm in an elevated position and is released by a cam attached to the slide. Advantageously, the slide is supported on a bed having an opening for the downward passage of the section of the slide struck by the striker with the opening having a edge underlying the cut made in the slide by the cutter.
Abstract: The compounds of this invention are cephalosporins having various acyl substituents at the 7-position and a substituted tetrazolyl thiomethyl group at the 3-position of the cephem nucleus and intermediates for the preparation thereof. The 7-acylated compounds have antibacterial activity.
Abstract: 2,3-Dichloro-4-(2-thenoyl)phenoxyacetic acid (tienilic acid) is prepared by reacting (2,3-dichloro-4-carboxy)phenoxyacetic acid with thiophene in the presence of a dehydration agent. The (2,3-dichloro-4-carboxy)phenoxyacetic acid is a novel compound.
Abstract: The compounds of this invention are 7.beta.-hydroxy-3-heterocyclicthiomethyl cephalosporins useful as intermediates for the preparation of 7.beta.-acyloxy cephalosporins.
Abstract: Pharmaceutical compositions and methods of inhibiting phenylethanolamine N-methyltransferase using novel 2,3-dihydro-1H-isoindole compounds having 4- and 5-substituents.
Type:
Grant
Filed:
March 2, 1979
Date of Patent:
August 19, 1980
Assignee:
SmithKline Corporation
Inventors:
William E. Bondinell, Robert G. Pendleton
Abstract: The compounds of this invention are phosphonoalkyl and esterified phosphonoalkyl substituted tetrazole thiols useful for preparing antibacterially active 7-acylamino-3-(phosphonoalkyl and esterified phosphonoalkyl substituted tetrazolylthiomethyl)cephalosporins.
Abstract: Novel cephalosporins having various acyl substituents at the 7-position and a carboxymethylaminoethyl substituted tetrazolylthiomethyl group at the 3-position of the cephem nucleus are prepared. These compounds have antibacterial activity.
Abstract: The invention is for a method for analyzing a stream of liquid such as blood and apparatus for carrying out the method. While it is known to present a moving column of liquid in a viewing cell, control of the circumference of the column to control its field size and lighting the column from the end opposite the viewing end has not been accomplished. The invention involves the method of passing a first liquid in a column in a confined space to a transparent panel, introducing one or more liquids of different colors to form a hollow column exterior of the first column, exhausting the liquids from adjacent the panel, directing light upwardly at the lower ends and through the columns and varying the pressure of one or more of the liquids to vary the circumference and speed of the first column. Apparatus is provided to carry out the method.
Abstract: Pharmaceutical compositions and methods of inhibiting phenylethanolamine N-methyltransferase using substituted carbamimidothioic acid phenylalkyl esters.
Type:
Grant
Filed:
March 15, 1979
Date of Patent:
June 17, 1980
Assignee:
SmithKline Corporation
Inventors:
William E. Bondinell, Robert G. Pendleton