Abstract: A group of 6,9-disubstituted-7,8-dihydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepi nes have dopaminergic activity. Examples of leading species of the invention are 6,9-dichloro-7,8-dihydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine and 6,9-dichloro-7,8-dihydroxy-1-(p-hydroxy-phenyl)-2,3,4,5-tetrahydro-1H- 3-benzazepine in the form of an acid addition salt.
Abstract: The compounds of this invention are cephalosporins having various acyl substituents at the 7-position and a sulfaminoalkyl substituted tetrazolylthiomethyl group at the 3-position of the cephem nucleus and intermediates for the preparation thereof. The 7-acylated cephalosporin compounds have antibacterial activity.
Abstract: The compounds of this invention are cephalosporins having various acyl substituents at the 7-position and a sulfaminoalkyl substituted tetrazolylthiomethyl group at the 3-position of the cephem nucleus and intermediates for the preparation thereof. The 7-acylated cephalosporin compounds have antibacterial activity.
Abstract: The compounds of this invention are cephalosporins having various acyl substituents at the 7-position and a sulfaminoalkyl substituted tetrazolylthiomethyl group at the 3-position of the cephem nucleus and intermediates for the preparation thereof. The 7-acylated cephalosporin compounds have antibacterial activity.
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:
August 3, 1977
Date of Patent:
September 4, 1979
Assignee:
SmithKline Corporation
Inventors:
John G. Gleason, Kenneth G. Holden, William F. Huffman
Abstract: A new process and intermediates for preparing 2,3-dichloro-4-(2-thenoyl)phenoxyacetic acid (ticrynafen, a diuretic agent) using as a key reaction a Friedel-Crafts acylation of an esterified 3-(2,3-dichlorophenoxy)-1,2-propanediol using a thenoyl halide.
Type:
Grant
Filed:
November 2, 1977
Date of Patent:
August 28, 1979
Assignee:
SmithKline Corporation
Inventors:
Antonietta R. Mastrocola, Robert L. Webb
Abstract: Substituted 2H-pyran-2,6(3H)-dione derivatives useful in the treatment of allergic conditions are prepared by reaction of 3,5-diacetyl-4,6-dihydroxy-2H-pyran-2-one with an appropriate aniline.
Abstract: A group of 1-phenyl-3-benzazepines with structures characterized by having a carboxy derived substituent at position 6 which are dopaminergic agents or are intermediates for preparing other dopaminergic agents. Particular illustrative species include 6-carbomethoxy-7,8-dihydroxy-3-methyl-1-phenyl-2,3,4,5-tetrahydro-1H-3-ben zazepine, 6-carboxy-7,8-dihydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine and 6-carbomethoxy-7,8-dihydroxy-1-(4'-hydroxyphenyl)-2,3,4,5-tetrahydro-1H-3- benzazepine.
Abstract: New lactam intermediates and methods for preparing a new series of 7-acylamino-8-oxo-3-oxa-1-azabicyclo[4.2.0]-octane-2-carboxylic acid derivatives are described. The end product compounds have antibacterial activity especially against certain Gram negative organisms.An example of the compounds of this invention are cis-3-blocked amino-4-ketoazetidinyl-2-acetaldehydes and their acetal derivatives.
Abstract: Substituted 2H-pyran-2,6(3H)-dione derivatives useful in the treatment of allergic conditions are prepared by reaction of 3,5-diacetyl-4,6-dihydroxy-2H-pyran-2-one with an appropriate aniline.
Abstract: The compounds of this invention are cephalosporins having a 3- or 4-aminomethylphenylacetamido substituent at the 7-position and a sulfonic acid substituted tetrazolyl thiomethyl group at the 3-position of the cephem nucleus. The compounds have antibacterial activity.
Abstract: The compounds of this invention are cephalosporins having a 7.beta.-acyloxy group and 7.beta.-hydroxy intermediates for the preparation thereof. The compounds have antibacterial activity.
Abstract: 3-Acyl-5-alkyltetrahydro-2,4,6-pyrantriones are prepared by catalytic hydrogenation of their 3,5-diacyl congeners. They have been found to have anti-allergic activity useful for treating the symptoms of asthma.
Abstract: The compounds are 6-hydroxy-5,6-substituted-phenyl-2,3,5,6-tetrahydroimidazo[2,1-b]thiazoles which have antiarthritic activity and are useful as intermediates for preparing 2,3-dihydroimidazo[2,1-b]thiazole antiarthritic compounds. A particular compound of this invention is 5,6-bis-(p-fluorophenyl)-6-hydroxy-2,3,5,6-tetrahydroimidazo[2,1-b]thiazol e.
Abstract: A device for smearing on slides a drop of liquid placed on a predetermined point on each slide has slide magazines containing a plurality of slides with the uppermost slide in each magazine having its upper face exposed for the reception of a drop of liquid towards one end thereof. Spreaders are adjacent the other ends of the slides. Means advance the spreaders out of contact with the slides, lower the spreaders into contact with the slides as they approach said predetermined points on the slides and slow the advance of the spreaders as they approach said points. The spreaders are retracted and the angle between each spreader and slide decreases to thin the smear of liquid. Means advance the uppermost slide in each magazine forwardly out of the magazine a predetermined distance to facilitate the removal of the slide by hand after the desired smear is made.
Abstract: A new synthesis for the preparation of 6-(2-hydroxyphenyl)-3-pyridazinones whose key reaction is cyclizing a 1,1,1-trihalo-2-hydroxy-4-(2-hydroxyphenyl)-1-butanone with hydrazine. 6-(2-Hydroxyphenyl)-3-pyridazinones are important intermediates for preparing medicinally active compounds.
Type:
Grant
Filed:
October 19, 1977
Date of Patent:
May 1, 1979
Assignee:
SmithKline Corporation
Inventors:
Sidney H. Levinson, Wilford L. Mendelson
Abstract: New semisynthetic cephalosporins characterized by having structures with a 1-carboxymethylthioethyltetrazolyl-5-thiomethyl group at position 3. Exemplary is the antibacterially effective 7-D-mandelamido-3-(1-carboxymethylthioethyltetrazolyl-5-thiomethyl)-3-ceph em-4-carboxylic acid disodium salt.