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Details for Patent: 6,187,804

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Details for Patent: 6,187,804

Title: Antibiotic compounds
Abstract:The present invention relates to carbapenems and provides a compound of the formula (I): ##STR1## or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof wherein: R.sup.1 is 1-hydroxyethyl, 1-fluoroethyl or hydroxymethyl; R.sup.2 is hydrogen or C.sub.1-4 alkyl; R.sup.3 is hydrogen or C.sub.1-4 alkyl; R.sup.4 and R.sup.5 are the same or different and are selected from hydrogen, halo, cyano, C.sub.1-4 alkyl, nitro, hydroxy, carboxy, C.sub.1-4 alkoxy, C.sub.1-4 alkoxycarbonyl, aminosulphonyl, C.sub.1-4 alkylaminosulphonyl, di-C.sub.1-4 -alkylaminosulphonyl, carbamoyl, C.sub.1-4 alkylcarbamoyl, di-C.sub.1-4 alkylcarbamoyl, trifluoromethyl, sulphonic acid, amino, C.sub.1-4 alkylamino, di-C 1.sub.4 alkylamino, C.sub.1-4 alkanoylamino, C.sub.1-4 alkanoyl(H-C.sub.1-4 alkyl)amino, C.sub.1-4 alkanesulphonamido and C.sub.1-4 alkylS(O).sub.n -- wherein n is zero, one or two: with the proviso that there is no hydroxy or carboxy substituent in a position ortho to the link to --NR.sup.3 --. Processes for their preparation, intermediates in their preparation, their use as therapeutic agents and pharmaceutical compositions containing them.
Inventor(s): Betts; Michael John (Wilmslow, GB), Davies; Gareth Morse (Macclesfield, GB), Swain; Michael Lingard (Stockport, GB)
Assignee: Zeneca Limited (London, GB)
Filing Date:Oct 08, 1998
Application Number:09/168,293
Claims:1. A dry-blended pharmaceutical composition comprising an alkali metal carbonate or bicarbonate and a compound of the formula (I) ##STR17##

or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof wherein:

R.sup.1 is 1-hydroxyethyl, 1-fluoroethyl or hydroxymethyl;

R.sup.2 is hydrogen or C.sub.1-4 alkyl;

R.sup.3 is hydrogen or C.sub.1-4 alkyl;

R.sup.4 and R.sup.5 are the same or different and are selected from hydrogen, halo, cyano, C.sub.1-4 alkyl, nitro, hydroxy, carboxy, C.sub.1-4 alkoxy, C.sub.1-4 alkoxycarbonyl, aminosulphonyl, C.sub.1-4 alkylaminosulphonyl, di-C.sub.1-4 -alkylaminosulphonyl, carbamoyl, C.sub.1-4 alkylcarbamoyl, di-C.sub.1-4 alkylcarbamoyl, trifluoromethyl, sulphonic acid, amino, C.sub.1-4 alkylamino, di-C.sub.1-4 alkylamino, C.sub.1-4 alkanoylamino, C.sub.1-4 alkanoyl(N--C.sub.1-4 alkyl)amino, C.sub.1-4 alkanesulphonamido and --S(O).sub.n C.sub.1-4 alkyl and wherein n is zero, one or two;

with the proviso that there is no hydroxy or carboxy substituent in a position ortho to the link to --NR.sup.3 -- and that overall the compound of formula (I) is acidic.

2. The dry-blended pharmaceutical composition according to claim 1, wherein R.sup.1 is 1-hydroxyethyl.

3. The dry-blended pharmaceutical composition according to claim 1 or claim 2, wherein R.sup.2 is hydrogen or methyl.

4. The dry-blended pharmaceutical composition according to claim 1 or claim 2, wherein R.sup.2 is methyl.

5. The dry-blended pharmaceutical composition according to claim 1 or claim 2, wherein R.sup.3 is hydrogen.

6. The dry-blended pharmaceutical composition according to claim 1 or claim 2, wherein the compound has the structure of formula (IV): ##STR18##

wherein R.sup.3, R.sup.4 and R.sup.5 are as hereinbefore defined.

7. The dry-blended pharmaceutical composition according to claim 6 wherein R.sup.4 and R.sup.5 are the same or different and selected from hydrogen, fluoro, chloro, hydroxy, carboxy, cyano, nitro, methyl, ethyl, methoxy, ethoxy, methoxycarbonyl, carbamoyl, methylcarbamoyl, dimethylcarbamoyl, trifluoromethyl, sulphonic acid, methylsulphinyl, methylsulphonyl, methanesulphonamido or acetamido.

8. The dry-blended pharmaceutical composition according to claim 6 wherein at least one of R.sup.4 and R.sup.5 in the compound of formula (IV) is hydrogen.

9. The dry-blended pharmaceutical composition according to claim 7 wherein at least one of R.sup.4 and R.sup.5 in the compound of formula (IV) is hydrogen.

10. The dry-blended pharmaceutical composition according to claim 6 wherein R.sup.4 is hydrogen, carboxy, fluoro, chloro, methyl, methoxy, cyano, sulphonic acid or methoxycarbonyl and R.sup.5 is hydrogen.

11. The dry-blended pharmaceutical composition according to claim 1, wherein the compound is (1R,5S,6S,8R,2'S,4'S)-2-(2-(3-carboxyphenylcarbamoyl)pyrrolidin-4-ylthio)- 6-(1-hydroxyethyl)-1-methylcarbapenem-3-carboxylic acid or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof.
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