Patent · US Expired

.beta.-Lactam-containing antibacterial agents and .beta.-lactamase inhibitors

US4558042A · kind A · utility

4Cited by
4References
6Claims
0Family size

Assignee

Inventors

Key dates

Filing dateMar 30, 1984
Grant dateDec 10, 1985
Priority date
Expiry dateMar 30, 2004

Classification

  • Technology area (CPC C)Chemistry; Metallurgy
  • CPC primaryC07D499/88
  • WIPO fieldOrganic fine chemistry
  • WIPO sectorChemistry

Abstract

There are disclosed .beta.-lactam-containing compounds of the formula: ##STR1## where R is hydrogen, lower alkyl, trichloroethyl, acetonyl, benzyl, substituted benzyl, phenyl, substituted phenyl, benzidryl or a residue that will undergo metabolic activation "in vivo" and have favorable pharmacokinetic properties; R.sup.1 is a hydrogen atom, lower alkyl, lower alkoxy, cycloalkyl, or hydroxyalkyl, with the alcoholic function of the hydroxyalkyl being free or protected; Z is hydrogen, halogen, hydroxy, amino, carbamoyloxy, mercapto, pyridinium, OR.sup.2, OCOR.sup.2, NHCOR.sup.2, or SR.sup.3 wherein each of R.sup.2 and R.sup.3 is any of lower alkyl, aryl, or a heterocyclic ring, each of which may be substituted or unsubstituted, and n is 0 or 1. The compounds have broad spectrum antibacterial activity and .beta.-lactamase inhibiting activity. Processes for the production of the .beta.-lactam-containing compounds and various intermediates in the production of those compounds are also disclosed.

Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.