Abstract: Antibacterial 9-deoxo-9a-ethyl and propyl-9a-aza-9a-homoerythromycin A compounds, pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising antibacterially effective amounts thereof and a pharmaceutically acceptable carrier, the treatment of bacterial infections with antibacterially effective amounts thereof, and intermediates and processes for their preparation.
Abstract: Crystalline sodium cefoperazone and a process for the preparation thereof comprising the combining of an aqueous acetone solution of sodium cefoperazone with a solution of acetone-methylene chloride.
Abstract: Antibacterial macrolides derived from 9-dihydro-11,12-O-isopropylidene-erythromycin A and 9-dihydro-11,12-O-isopropylidene-4"-epi-erythromycin A.
Abstract: A process for the preparation of chloromethyl esters of penicillanic acids, using iodochloromethane or bromochloromethane and a tetraalkylammonium salt of the penicillanic acid, and their use in processes for the synthesis of penicillanic acid esters, using a halomethyl ester and the tetraalkylammonium salt of the penicillanic acid, which readily hydrolyze in vivo to antibacterial penicillins and the beta-lactamase inhibitor penicillanic acid sulfone.
Abstract: Processes for the preparation of the antiinflammatory agent piroxicam and intermediates leading thereto, the first of which comprises reacting N-methylsaccharin with (N-2-pyridyl)haloacetamides and alkyl haloacetates in the presence of a metal hydride to give, respectively, piroxicam and alkyl 4-hydroxy-2-methyl-2H-1,2-benzothiazine-3-carboxylate 1,1-dioxides, intermediates which can be converted into piroxicam; and the second of which comprises reacting a novel alkyl 2-(2-methyl-3-hydroxy2,3-dihydro-1,2-benzisosulfonazol-3-yl)-2-haloacetate with a metal hydride to give alkyl 4-hydroxy-2-methyl-2H-1,2-benzothiazine-3-carboxylate 1,1-dioxides, intermediates leading to piroxicam.
Abstract: The reaction product of dimethyl diazomethylphosphonate with 4"-deoxy-4"-oxo-oleandomycin and erythyromycin A derivatives as antibacterial agents.
Abstract: A process for preparing halomethyl esters of penicillanic acid sulfone, intermediates to beta-lactamase inhibitors, from the corresponding substituted thiomethyl and sulfinylmethyl esters and a halogenating agent. The thiomethyl and sulfinylmethyl esters of penicillanic acid sulfone are useful intermediates.
Abstract: Process for preparing L-carnosine by reacting L-histidine and tetrahydro-1,3-thiazin-2,4-dione in an aqueous medium at a selected pH and temperature range followed by removal of carbon oxysulfide at acid pH, removal of water and crystallization of product wherein pH adjustments are made with substituted ammonium hydroxides and organic acids having pKa .ltoreq.3.75.
Abstract: A series of 2-substituted-4-(4-imidazolyl)pyridines and the pharmaceutically acceptable acid addition salts thereof as histamine H.sub.2 -receptor inhibitors for controlling gastric acidity.
Type:
Grant
Filed:
October 16, 1980
Date of Patent:
November 24, 1981
Assignee:
Pfizer Inc.
Inventors:
John L. LaMattina, Christopher A. Lipinski
Abstract: 6.beta.-Hydroxyalkylpenicillanic acids and derivatives thereof as useful enhancers of the effectiveness of several .beta.-lactam antibiotics against many .beta.-lactamase producing bacteria, and 6.beta.-substituted penicillanic acid benzyl ester derivatives as useful intermediates leading to said agents which enhance the effectiveness of .beta.-lactam antibiotics.