Monosulfactams

Information

  • Patent Grant
  • 4684722
  • Patent Number
    4,684,722
  • Date Filed
    Monday, January 6, 1986
    38 years ago
  • Date Issued
    Tuesday, August 4, 1987
    37 years ago
Abstract
Antibacterial activity is exhibited by monocyclic .beta.-lactam antibiotics having in the 1-position an --O--SO.sub.3 H activating group and in the 3-position an acylamino group of the formula ##STR1## wherein R.sub.3 and R.sub.4 are each independently hydrogen or alkyl.
Description
Claims
  • 1. A compound having the formula ##STR38## or a pharmaceutically acceptable salt thereof, wherein R.sub.1 and R.sub.2 are the same or different and each is hydrogen or alkyl, or R.sub.1 and R.sub.2 together are --(CH.sub.2).sub.n --wherein n is 2, 3, 4, 5 or 6; and
  • R.sub.3 and R.sub.4 are the same or different and each is hydrogen or alkyl of 1 to 3 carbon atoms.
  • 2. A compound in accordance with claim 1 wherein R.sub.1 and R.sub.2 are the same or different and each is hydrogen or alkyl.
  • 3. A compound in accordance with claim 1 wherein R.sub.1 and R.sub.2 are the same or different and each is hydrogen or methyl.
  • 4. A compound in accordance with claim 1 wherein one of R.sub.1 and R.sub.2 is hydrogen and the other is methyl or ethyl.
  • 5. A compound in accordance with claim 1 wherein R.sub.1 and R.sub.2 are each methyl.
  • 6. A compound in accordance with claim 1 wherein R.sub.1 and R.sub.2 are each hydrogen.
  • 7. A compound in accordance with claim 1 wherein R.sub.1 and R.sub.2 together are --(CH.sub.2).sub.n --.
  • 8. A compound in accordance with claim 1 wherein R.sub.3 and R.sub.4 are each hydrogen.
  • 9. A compound in accordance with claim 1 wherein R.sub.3 is alkyl of 1 to 3 carbon atoms and R.sub.4 is hydrogen.
  • 10. A compound in accordance with claim 1 wherein R.sub.3 and R.sub.4 are each alkyl of 1 to 3 carbon atoms.
  • 11. The compound in accordance with claim 1, [3S(Z)]-2-[[[1-(2-amino-4-thiazolyl)-2-[[4,4-dimethyl-2-oxo-1-(sulfooxy)-3-azetidinyl]amino]-2-oxoethylidene]amino]oxy]-2-propenoic acid.
  • 12. The compound in accordance with claim 1, (.+-.)-(Z)-2-[[[1-(2-amino-4-thiazolyl)-2-oxo-2-[[2-oxo-1-(sulfooxy)-1-azaspiro[3.3]hept-3-yl]amino]ethylidene]amino]oxy]-2-propenoic acid.
US Referenced Citations (3)
Number Name Date Kind
4399131 Durckheimer et al. Aug 1983
4423213 Takaya et al. Dec 1983
4533660 Gordon et al. Aug 1985
Foreign Referenced Citations (4)
Number Date Country
127992 Dec 1984 EPX
58-113174 Jul 1983 JPX
58-206589 Dec 1983 JPX
1602725 Nov 1981 GBX