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-carboxylic acid.
- 4. A compound according to claim 1, said compound being 7beta-[2-(2-aminothiazol-4-yl)-4-carboxy-2-butenoylamino]-3-methyl-3-cephem-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-trifluoropropenyl-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-carbamoyloxymethyl-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-methylthiomethyl-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-cyanomethylthiomethyl-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-thiadiazol-5-yl thiomethyl-3-cephem-4-carboxylic acid or 7beta-[2-(2-aminothiazol-4-yl)-4-carboxy-2-butenoylamino]-3-1,3,4-thiadiazol-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-cephem-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-cephem-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-fluoroethylthio-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-trifluoroethylthio-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.
Priority Claims (3)
Number |
Date |
Country |
Kind |
58-186601 |
Oct 1983 |
JPX |
|
59-18563 |
Feb 1984 |
JPX |
|
59-100890 |
May 1984 |
JPX |
|
Parent Case Info
This application is a continuation in part of application Ser. No. 656,731, filed Oct. 1, 1984 (now abandoned).
US Referenced Citations (4)
Foreign Referenced Citations (1)
Number |
Date |
Country |
2076801 |
Dec 1981 |
GBX |
Continuation in Parts (1)
|
Number |
Date |
Country |
Parent |
656731 |
Oct 1984 |
|