6-Aminoalkylpenicillanic acid 1,1-dioxides as beta-lactamase inh

Details 6-Aminoalkylpenicillanic acid 1,1-dioxides as beta-lactamase inh 6-Aminoalkylpenicillanic acid 1,1-dioxides as beta-lactamase inh

1982-10-21

1984-06-05

Trousof, Natalie

Drug, bio-affecting and body treating compositions

Antigen, epitope, or other immunospecific immunoeffector

Bacterium or component thereof or substance produced by said...

2602391, 2602452R, 424269, 424271, A61K 31545, A61K 3143, C07D49900, C07D49946

Patent

active

044527969

ABSTRACT:
Beta-lactamase inhibitors which are 6-alpha- and 6-beta-(aminomethyl) and (1-aminoethyl)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, used 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 aminoalkyl penicillanic acid 1,1-dioxides and ampicillin or amoxicillin, also used in the treatment of bacterial infections; and intermediates therefor.

REFERENCES:
patent: 3487079 (1969-12-01), Sheehan
patent: 4207323 (1980-06-01), Beattie et al.
patent: 4234579 (1979-03-01), Barth
patent: 4237051 (1980-02-01), McCombie
patent: 4244951 (1981-01-01), Bigham
patent: 4260598 (1981-04-01), Barth
patent: 4287181 (1981-09-01), Kellogg
patent: 4309347 (1982-01-01), Bigham
patent: 4342768 (1982-08-01), Kellogg
patent: 4342772 (1982-08-01), Godtfredsen et al.
Sheehan et al., J. Org. Chem., 42, pp. 4045-4048, (1977).

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