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Penicillanic acid dioxide prodrug

  • US 4,428,935 A
  • Filed: 05/24/1982
  • Issued: 01/31/1984
  • Est. Priority Date: 05/24/1982
  • Status: Expired due to Term
First Claim
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1. A compound of the formula ##STR5## wherein:

  • R is hydrogen;

    Q is chosen so that the compound hydrolyzes in vivo to 4.4-dioxopenicillanic and is selected from the group consisting ofN(R1) (R2) (R3) wherein R1, R2 and R3 are each alkyl having 1-4 carbon atoms, hydroxyalkyl having 1-4 carbon atoms, alkoxycarbonylalkyl wherein the alkyl has 1-4 carbon atoms and the alkoxy has 1-4 carbon atoms or aminocarbonylalkyl wherein the alkyl has 1-4 carbon atoms,N-alkyl-morpholyl wherein the alkyl has 1-4 carbon atoms, N-alkyl-piperidyl wherein the alkyl has 1-4 carbon atoms or N-alkyl-pyrrolidyl wherein the alkyl has 1-4 carbon atom, and those groups substituted at a ring position with alkyl having 1-4 carbon atoms, aminocarbonyl, hydroxyl or alkoxycarbonyl wherein the alkoxy has 1-4 carbon atoms,bicyclo [2.2.2]1-,4-diazaoctanyl and those substituted with alkyl having 1-4 carbon atoms, aminocarbonyl, hydroxyl or alkoxycarbonyl wherein the alkoxy has 1-4 carbon atoms,pyridyl, alkylpyridyl wherein the alkyl has 1-4 carbon atoms, dialkylpyridyl wherein each alkyl has 1-4 carbon atoms, trialkylpyridyl wherein each alkyl has 1-4 carbon atoms, halopyridyl, cyanopyridyl, nitropyridyl, aminocarbonylpyridyl, N-alkylaminocarbonylpyridyl wherein the alkyl has 1-4 carbon atoms, N,N-dialkylaminocarbonylpyridyl wherein each alkyl has 1-4 carbon atoms, alkoxycarbonylpyridyl wherein the alkoxy contains 1-4 carbon atoms, or N,N-dialkylaminopyridyl wherein each alkyl has 1-4 carbon atoms, andquinolyl or N-alkylimidazolyl wherein the alkyl has 1-4 carbon atoms; and

    X- is a pharmaceutically-acceptable anion.

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