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Claims for Patent: 5,317,016

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Claims for Patent: 5,317,016

Title: Pyrrolidylthiocarbapenem derivative
Abstract:A pyrrolidylthiocarbapenem derivative represented by Formula I is provided: ##STR1## wherein R.sup.1 is hydrogen or lower alkyl; R.sup.2, R.sup.3 and R.sup.4 are hydrogen, lower alkyl which can be substituted or an amino protecting group independently, or R.sup.2 and R.sup.3 together with a nitrogen atom to which R.sup.2 and R.sup.3 are bonded form a saturated or unsaturated cyclic group, or R.sup.2 and R.sup.4, or R.sup.3 and R.sup.4 together with two nitrogen atoms and one sulfur atom in the sufamide group form a saturated or unsaturated cyclic group; each cyclic group can further include at least one atom selected from the group consisting of oxygen, sulfur and nitrogen, and each cyclic group can be substituted; X.sup.1 is hydrogen or a hydroxy protecting group; X.sup.2 is hydrogen, a carboxy protecting group, an ammonio group, an alkali metal or an alkaline-earth metal; and Y.sup.2 is hydrogen or an amino protecting group.
Inventor(s): Nishitani; Yasuhiro (Osaka, JP), Irie; Tadashi (Osaka, JP)
Assignee: Shionogi Seiyaku Kabushiki Kaisha (Osaka, JP)
Application Number:07/929,961
Patent Claims: 1. A pyrrolidylthiocarbapenem derivative represented by Formula I: ##STR45## wherein R.sup.1 is hydrogen or lower alkyl; R.sup.2, R.sup.3 and R.sup.4 are hydrogen, lower alkyl which can be substituted, or an amino protecting group independently, or R.sup.2 and R.sup.3 together with a nitrogen atom to which R.sup.2 and R.sup.3 are bonded form a saturated or unsaturated cyclic group, or R.sup.2 and R.sup.4, or R.sup.3 and R.sup.4 together with two nitrogen atoms and one sulfur atom in the sulfamide group form a saturated or unsaturated cyclic group; each cyclic group can further include at least one atom selected from the group consisting of oxygen, sulfur and nitrogen, and each cyclic group can be substituted; X.sup.1 is hydrogen or a hydroxy protecting group; X.sup.2 is hydrogen, a carboxy protecting group, an ammonio group, an alkali metal or an alkaline-earth metal; and Y.sup.2 is hydrogen or an amino protecting group.

2. A pyrrolidylthiocarbapenem derivative according to claim 1, wherein R.sup.1 is methyl.

3. A pyrrolidylthiocarbapenem derivative according to claim 2, wherein R.sup.4 is hydrogen.

4. A pyrrolidylthiocarbapenem derivative according to claim 3, wherein X.sup.1 and Y.sup.2 are hydrogens and X.sup.2 is hydrogen or alkali metal.

5. A pyrrolidylthiocarbapenem derivative according to claim 4, wherein R.sup.2 and R.sup.3 are hydrogens; R.sup.2 is methyl and R.sup.3 are hydrogen; both R.sup.2 and R.sup.3 are methyl; or R.sup.2 is 2-hydroxyethyl, and R.sup.3 are hydrogen.

6. A pyrrolidylthiocarbapenem derivative according to claim 2, wherein R.sup.3 is hydrogen, and R.sup.2 and R.sup.4 are bonded to each other to form --CH.sub.2 --CH.sub.2 --.

7. A pyrrolidylthiocarbapenem derivative according to claim 2, wherein R.sup.3 is hydrogen, and R.sup.2 and R.sup.4 are bonded to each other to form --CH.sub.2 --CH.sub.2 --CH.sub.2 --.

8. A pyrrolidylthiocarbapenem derivative according to claim 1, wherein at least one group selected from the group consisting of R.sup.2, R.sup.3, R.sup.4 and Y.sup.2 is selected from the group consisting of t-butyloxy carbonyl, allyloxycarbonyl, p-nitrobenzyloxycarbonyl, p-methoxybenzyloxycarbonyl and diazo.

9. A pyrrolidylthiocarbapenem derivative according to claim 1, wherein X.sup.1 is selected from the group consisting of hydrogen, trimethylsilyl, triethylsilyl and t-butoxydimethylsilyl.

10. A pyrrolidylthiocarbapenem derivative according to claim 1, wherein X.sup.2 is selected from the group consisting of hydrogen, sodium potassium, t-butyl, allyl, p-nitrobenzyl, p-methoxybenzyl and diphenylmethyl.

11. A pyrrolidylthiocarbapenem derivative according to claim 1, wherein the pyrrolidine ring in Formula I has a configulation of (3S,5S).

12. An antibacterial agent comprising an effective amount of the pyrrolidylthiocarbapenem derivative of claim 1 as an active ingredient.

13. An antibacterial agent comprising an effective amount of the pyrrolidylthiocarbapenem derivative of claim 4 as an active ingredient.

14. An antibacterial agent comprising an effective amount of the pyrrolidylthiocarbapenem derivative of claim 5 as an active ingredient.

15. An antibacterial agent comprising an effective amount of the pyrrolidylthiocarbapenem derivative of claim 11 as an active ingredient.

16. A method for inhibiting growth of bacteria sensitive to the pyrrolidylthiocarbapenem derivative of claim 1 by allowing the sensitive bacterium to be in contact with an effective amount of the pyrrolidylthiocarbapenem derivative.
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