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US 5,143,908 AGranted
Antibacterial agents and potentiators of carbapenem antibiotics
AssigneeMerck & Co., Inc.
InventorsWilliam H. Parsons, William R. Schoen, Arthur A. Patchett, Masao Taniguchi
Life of this patent
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Abstract
New 3-(1-aminoalkylphosphinyl)-(2-substituted)propionic acids are described which display antibacterial activity and potentiate carbapenem antibiotics.
Claims10
A pharmaceutical composition useful in the treatment of antibacterial infections which comprises a pharmaceutically acceptable carrier and a pharmaceutically effective amount to treat bacterial infections of an antibacterial compound of formula I:
- ##STR53## wherein R.sub.1 is
- H, or
- CH.sub.3 ;
- R.sub.2 is
- (a) hydrogen;
- (b) C.sub.1 -C.sub.12 linear or branched alkyl;
- (c) C.sub.1 -C.sub.12 linear or branched monoalkenyl;
- (d) C.sub.7 -C.sub.20 aralkyl, wherein the alkyl chain is linear or branched C.sub.1 -C.sub.8 and wherein said above values from R.sub.2 can be substituted by one halo, hydroxy, carboxy, C.sub.1 -C.sub.4 alkoxycarbonyl, C.sub.7 -C.sub.16 arylalkoxycarbonyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.6 -C.sub.12 aryloxy, amino, mono- or di-C.sub.1 -C.sub.8 alkylamino, thio, C.sub.1 -C.sub.4 alkylthio, C.sub.6 -C.sub.12 arylthio, C.sub.7 -C.sub.16 aralkylthio, or the radical --S--(CH.sub.2).sub.n --CH--(NH.sub.2)COOH, where n=1-2;
- with the proviso that R.sub.2 is at least C.sub.2 alkyl if substituted by one of the above-defined thio groups, and wherein the aryl ring can be further substituted by one C.sub.1 -C.sub.4 linear or branched alkyl, trihalomethyl, nitro, halo, cyano or sulfonamido;
- R.sub.3 and R.sub.4 are
- hydrogen,
- C.sub.1 -C.sub.4 alkyl;
- wherein the carbon atoms attached to R.sub.1 are D(S) or DL(SR) and R.sub.2 are D(R) or DL(RS) stereoconfiguration.
10 more elements
Dependencies are inferred from the claim text.