The invention relates to compounds of formula (1) and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R, R, R, R, R, and Rare as defined herein. The invention also relates to methods of treating abnormal cell growth, such as cancer, in mammals by administering the compounds of formula 1 and to pharmaceutical compositions for treating such disorders which contain the compounds of formula (1). The invention also relates to methods of preparing the compounds of formula (1).
Crystalline Benzenesulfonate Salts Of Sultamicillin
Wayne E. Barth - East Lyme CT Vytautas J. Jasys - New London CT
Assignee:
Pfizer Inc. - New York NY
International Classification:
A61K 3143 C07D49932
US Classification:
424271
Abstract:
Novel benzenesulfonic acid addition salts of sultamicillin of the formula ##STR1## and hydrated forms thereof, where X is hydrogen or chloro, especially the crystalline dihydrate salts, having advantages over the prior art forms of sultamicillin in pharmaceutical dosage forms, most particularly those for use in pediatric medicine, method for their use and pharmaceutical compositions thereof.
Certain novel 6-acylamino-2,2-dimethyl-3-(5-tetrazolyl)penam derivatives, and salts thereof; their use as broad-spectrum antibacterial agents; and methods for their preparation. Their preparation comprises acylation of the novel intermediate, 6-amino-2,2-dimethyl-3-(5-tetrazolyl)penam or simple derivatives thereof, followed, in some cases, by further transformations of the 6-acylamino group or by removal of a protecting group from the 5-tetrazolyl moiety. Process for the preparation of 6-amino-2,2-dimethyl-3-(5-tetrazolyl)penam, simple derivatives thereof and intermediates therefor.
Certain novel antibacterial 7-acylamino-3-substituted-4-(tetrazol-5-yl)-. DELTA. sup. 3 -cephem derivatives, and salts thereof, and intermediates useful in their preparation.
beta-Lactamase inhibitors which are aminoacid esters of 6-alpha- and 6-beta-(hydroxymethyl)pencillanic acid 1,1-dioxides; pharmaceutically-acceptable salts thereof; conventional esters thereof which are hydrolyzable in vivo; bis-methanediol esters thereof; or mixed methanediol esters with said beta-lactamase inhibitors and sulbactam. Pharmaceutical compositions comprising said beta-lactamase inhibitors and a conventional beta-lactam antibiotic, said compositions useful in the treatment of bacterial infections. Compounds useful as intermediates in the synthesis of said beta-lactamase inhibitors. Antibacterial mixed bis-methanediol esters of said aminoacyloxymethyl penicillanic acid 1,1-dioxides and ampicillin or amoxicillin, also useful in the treatment of bacterial infections; and intermediates therefor.
Process For 6-(Aminomethyl)Penicillanic Acid 1,1-Dioxide And Derivatives Thereof
A process for the preparation of beta-lactamase inhibiting 6-alpha-(aminomethyl)penicillanic acid 1,1-dioxide and derivatives. R- and S-1-(ethoxycarbonyloxy)ethyl 6-alpha-(aminomethyl)penicillanate 1,1-dioxide are specifically described.