Abstract: A novel antibiotic, polynitroxin, is produced by the cultivation of a fermentation broth containing Nocardiopsis mutabilis Shearer sp. nov. ATCC 31520 in an aqueous nutrient medium under submerged aerobic conditions.
Abstract: Imidodisulfamide derivatives useful in the treatment of allergic conditions are prepared by reaction of an appropriately substituted tetrahydroisoquinoline and bis (chlorosulfonyl)imide in the presence of a tertiary amine. Pharmaceutical compositions and methods of inhibiting the symptoms of an allergic response are also disclosed.
Abstract: Imidodisulfamide derivatives useful in the treatment of allergic conditions are prepared by reaction of an appropriately substituted tetrahydroisoquinoline and bis(chlorosulfonyl)imide in the presence of a tertiary amine.
Abstract: A new group of 2(3H)-indolones whose structures are characterized by having an aminoalkyl substituent at position 4 and a hydroxy group at position 7 of the indolone nucleus have beneficial activity on the cardiovascular system. A typical species of the group is 4-di-n-propylaminoethyl-7-hydroxy-2(3H)-indolone and its acid addition salts.
Abstract: Novel cephalosporins with improved antibacterial and pharmacokinetic properties are disclosed. These compounds have a 2-alkoxyimino-2-(2-amino-4-thiazolyl)-acetamido group at position 7 and a sulfaminoalkyltetrazolythio group at position 3.
Abstract: Lower alkyl .beta.-(S-benzylmercapto)-.beta.,.beta.-pentamethylenepropionates are prepared in improved yields by reacting lower alkyl cyclohexylideneacetates with benzylmercaptan in the presence of an alkali metal mercaptide.
Abstract: A novel anthracycline antibiotic complex, fragilomycin complex, is produced by the cultivation of a fermentation broth containing Streptosporangium fragilis Shearer sp. nov. ATCC 31519 microorganisms in an aqueous nutrient medium under submerged aerobic conditions. The fragilomycin complex and its major bioactive component, fragilomycin A, exhibit antibiotic activity.
July 24, 1980
Date of Patent:
October 6, 1981
Claude H. Nash, III, Marcia C. Shearer, Kenneth M. Snader, Joseph R. Valenta, David Cooper
Abstract: Imidodisulfamide derivatives useful in the treatment of allergic conditions are prepared by reaction of an appropriately substituted primary amine and bis(chlorosulfonyl) imide in the presence of a tertiary amine.
February 13, 1980
Date of Patent:
September 29, 1981
Fadia E. Ali, Robert D. Krell, Kenneth M. Snader
Abstract: New 7,8-dihydroxy-1-(sulfamylphenyl)-2,3,4,5-tetrahydro-1H-3-benzazepines having pharmaceutical activity together with new intermediates and methods of synthesis for preparing them. The lead compound is 6-chloro-7,8-dihydroxy-1-(p-sulfamylphenyl)-2,3,4,5-tetrahydro-1H-3-benzaz epine which has very potent renal dopaminergic activity.
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: N-Phenyl-N'-cyano-O-phenylisoureas are prepared from N-cyanodiphenoxyimidocarbonate and an optionally substituted o-phenylenediamine or o-aminophenol. The isoureas are new chemical intermediates especially useful for preparing 2-cyanamido and 2-carbomethoxyaminobenzimidazole and benzoxazole compounds having anthelmintic activity.
Abstract: A group of 1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines whose structures have amino, hydroxy substituents at the 7,8-positions of the benzazepine nucleus is disclosed. Novel intermediates and routes of synthesis used for preparing them are also described. The end products have pharmacodynamic activity.
January 31, 1980
Date of Patent:
August 18, 1981
Kenneth G. Holden, Carl Kaiser, Joseph Weinstock
Abstract: 3,4-Dihydroxyphenyltetrahydrothieno[2,3-c] or [3,2-c] pyridines are prepared by cyclization of a N-thienylmethyl-2-(3',4'-dimethoxyphenyl)-ethanolamine. These compounds have renal vasodilating activity. A species is 4-(3,4-dihydroxyphenyl)-1,2,3,4-tetrahydrothieno[2,3-c]pyridine and its pharmaceutically acceptable acid addition salts or esters.
Abstract: New semisynthetic cephalosporins having antibacterial activity are described. The structures of the new compounds are characterized by having an .alpha.-oxyimino group in the 7-acetamidomoiety plus a carboxyalkyltetrazolylthiomethyl group at position 3.
Abstract: 5-(5'-Halo-2'-methoxyphenyl)-3,4-dihalo-2(5H)-furanones are prepared by a Friedel-Crafts reaction using a p-haloanisole and a mucohalic acid in the presence of aluminum chloride. They are used as chemical intermediates for preparing hydroxyphenylpyridazinones.
Abstract: A series of 6-lower alkyl-7,8-dihydroxyl-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines having dopaminergic activity together with intermediates and processes for their preparation are disclosed.
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.