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Claims for Patent: 4,634,697

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Claims for Patent: 4,634,697

Title: Carboxyalkenamidocephalosporins
Abstract:An antibacterial 7beta-(carboxyalkenoyl)amino-3-cephem-4-carboxylic acid represented by the following formula: ##STR1## (wherein R is aryl or a heterocyclic group; R.sup.1 is hydrogen or halogen; R.sup.2 is a single bond, alkylene, or thiaalkylene; R.sup.3 is a hydrogen atom or carboxy modifying group; R.sup.4 is hydrogen or methoxy; R.sup.5 is hydrogen or a 3-substituent of cephalosporins; R.sup.6 is a hydrogen atom or carboxy modifying group; and X is oxygen, sulfur, or sulfinyl) a pharmaceutical composition containing the same, and a method for treating a bacterial infection with the same.
Inventor(s): Hamashima; Yoshio (Kyoto, JP)
Assignee: Shionogi & Co., Ltd. (Osaka, JP)
Application Number:06/711,017
Patent Claims: 1. A compound of the formula ##STR100## wherein R is 2-aminothiazol-4-yl the amino group of which is unprotected or protected with a protecting group,

R.sup.3 is (1) hydrogen, (2) a pharmacologically acceptable salt forming group, (3) phthalidyl, (4) phenacyl, (5) C.sub.2-7 alkenyl, (6) diphenylmethyl, (7) trityl, (8) phenylalkyl of 7 to 15 carbon atoms said group being unsubstituted or substituted by alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 2 carbon atoms, nitro, amino or hydroxy or (9) a lower alkyl group,

R.sup.5 is hydrogen, methyl, vinyl, cyanovinyl, trifluoropropenyl, methoxymethyl, carbamoyloxymethyl, methylthiomethyl, cyanomethylthiomethyl, thiadiazolylthiomethyl, triazolylthiomethyl, aminomethylthiadiazolylthiomethyl, aminothiadiazolylthiomethyl, methoxy, fluoroethylthio, trifluoroethylthio, or halogen, and

R.sup.6 is (1) hydrogen, (2) a pharmacologically acceptable salt forming atom or group, (3) a lower alkyl group, (4) a lower alkenyl group (5) phthalidyl, (6) phenacyl, (7) diphenylmethyl, (8) trityl or (9) phenylalkyl of 7 to 15 carbon atoms said group being unsubstituted or substituted by alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 2 carbon atoms, nitro, amino or hydroxy.

2. A compound according to claim 1 wherein

R.sup.3 is hydrogen or a pharmacologically acceptable salt forming group,

R.sup.5 is hydrogen, methyl, vinyl, trifluoropropenyl, methoxymethyl, carbamoyloxymethyl, methylthiomethyl, cyanomethylthiomethyl, thiadiazolylthiomethyl, methoxy, fluoroethylthio, trifluoroethylthio, or halogen, and

R.sup.6 is hydrogen or a pharmacologically acceptable salt forming atom or group.

3. A compound according to claim 1, said compound being 7beta-[2-(2-aminothiazol-4-yl)-4-carboxy-2-butenoylamino]-3-cephem-4-carbo xylic acid.

4. A compound according to claim 1, said compound being 7beta-[2-(2-aminothiazol-4-yl)-4-carboxy-2-butenoylamino]-3-methyl-3-cephe m-4-carboxylic acid.

5. A compound according to claim 1, said compound being 7beta-[2-(2-aminothiazol-4-yl)-4-carboxy-2-butenoylamino]-3-vinyl-3-cephem -4-carboxylic acid.

6. A compound according to claim 1, said compound being 7beta-[2-(2-aminothiazol-4-yl)-4-carboxy-2-butenoylamino]-3-trifluoroprope nyl-3-cephem-4-carboxylic acid.

7. A compound according to claim 1, said compound being 7beta-[2-(2-aminothiazol-4-yl)-4-carboxy-2-butenoylamino]-3-carbamoyloxyme thyl-3-cephem-4-carboxylic acid.

8. A compound according to claim 1, said compound being 7beta-[2-(2-aminothiazol-4-yl)-4-carboxy-2-butenoylamino]-3-methoxymethyl- 3-cephem-4-carboxylic acid.

9. A compound according to claim 1, said compound being 7beta-[2-(2-aminothiazol-4-yl)-4-carboxy-2-butenoylamino]-3-methylthiometh yl-3-cephem-4-carboxylic acid.

10. A compound according to claim 1, said compound being 7beta-[2-(2-aminothiazol-4-yl)-4-carboxy-2-butenoylamino]-3-cyanomethylthi omethyl-3-cephem-4-carboxylic acid.

11. A compound according to claim 1, said compound being 7beta-[2-(2-aminothiazol-4-yl)-4-carboxy-2-butenoylamino]-3-1,2,3-triazol- 5-yl thiomethyl-3-cephem-4-carboxylic acid.

12. A compound according to claim 1, said compound being 7beta-[2-(2-aminothiazol-4-yl)-4-carboxy-2-butenoylamino]-3-1,2,3-thiadiaz ol-5-yl thiomethyl-3-cephem-4-carboxylic acid or 7beta-[2-(2-aminothiazol-4-yl)-4-carboxy-2-butenoylamino]-3-1,3,4-thiadiaz ol-5-yl thiomethyl-3-cephem-4-carboxylic acid.

13. A compound according to claim 1, said compound being 7beta-[2-(2-aminothiazol-4-yl)-4-carboxy-2-butenoylamino]-3-methoxy-3-ceph em-4-carboxylic acid.

14. A compound according to claim 1, said compound being 7beta-[2-(2-aminothiazol-4-yl)-4-carboxy-2-butenoylamino]-3-chloro-3-cephe m-4-carboxylic acid.

15. A compound according to claim 1, said compound being 7beta-[2-(2-aminothiazol-4-yl)-4-carboxy-2-butenoylamino]-3-2-fluoroethylt hio-3-cephem-4-carboxylic acid.

16. A compound according to claim 1, said compound being 7beta[2-(2-aminothiazol-4-yl)-4-carboxy-2-butenoylamino]-3-2,2,2-trifluoro ethylthio-3-cephem-4-carboxylic acid.

17. An antibacterial composition which comprises an antibacterially effective amount of a compound of claim 1 and a pharmaceutically acceptable carrier therefor.

18. A method for combatting bacteria which comprises bringing an antibacterially effective amount of a compound of claim 1 into contact with the bacteria.
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