Drug – bio-affecting and body treating compositions – Plural fermentates of different origin
Patent
1982-05-24
1984-01-31
Rizzo, Nicholas S.
Drug, bio-affecting and body treating compositions
Plural fermentates of different origin
2602452R, 424270, C07D49900, C07D49932, A61K 31425
Patent
active
044289359
ABSTRACT:
A compound of the formula ##STR1## is a prodrug of 4,4-dioxopenicillanic acid, wherein R is hydrogen or methyl; R.sub.1, R.sub.2 and R.sub.3 (a) when taken individually are each alkyl containing one to four carbon atoms, or (b) when taken together with the nitrogen to which they are attached form a five- or six-membered saturated monocyclic moiety, an eight-membered saturated bicyclic moiety or a five- or six-membered aromatic cyclic moiety annulated with zero, one or two fused benzene rings, with the proviso that any R.sub.1, R.sub.2 or R.sub.3 not part of a cyclic moiety is alkyl containing one to four carbon atoms; and X.sup.- is a pharmaceutically-acceptable anion. The prodrug can be included with a beta-lactam antibiotic in a pharmaceutical composition which can be employed in the treatment of infection in mammals. The above-described compounds hydrolyze in vivo to 4,4-dioxopenicillanic acid.
REFERENCES:
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patent: 4323499 (1982-04-01), Myers
C. Kaiser and J. Winstock, "Alkenes via Hofmann Elimination; Use of Ion-Exchange Resin for Preparation of Quaternary Amines . . . " Organic Synthesis, vol. 55, pp. 3-7, (1976).
H. Ferres, "Prodrugs of B-Lactam Antibiotics," Chemistry and Industry, 1980, pp. 435-440.
N. Bodor, et al., "Soft Drugs. I. Labile Quaternary Ammonium Salts as Soft Antimicrobials," J. Medicinal Chem., vol. 23, pp. 469-480, (1980).
N. Bodor, et al., "Soft Drugs. II. Soft Alkylating Agents as Potential Antitumor Agents," J. Medicinal Chem., vol. 23, pp. 566-569, (1980).
Bloom Allen
Knuth Charles J.
Pfizer Inc.
Richardson Peter C.
Rizzo Nicholas S.
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