Patent US4169947A successfully refreshed from Google Patents.
← Back to Patent Explorer
US4169947A Expired / Lapsed US ⏱️ 0.0 years remaining

7β-[[[2-Acylamino]-1,2-dioxoethyl]amino]acyl cephalosporins

Assignee: ER Squibb and Sons LLC
•
Filing: 1978-05-30
•
Granted: 1979-10-02
•
Expires: 1998-05-30
📄 Original PDF 🌐 Google Patents 🔄 Sync Now

Abstract

Abstract 7β-[[[2-Acylamino]-1,2-dioxoethyl]amino]acyl cephalosporins of the formula ##STR1## wherein R is hydrogen, lower alkyl, phenyl-lower alkyl, diphenyl-lower alkyl, tri(lower alkyl)silyl, trihaloethyl or a salt forming ion; R 1 is hydrogen, lower alkyl, saturated or unsaturated cycloalkyl, phenyl, phenyl-lower alkyl, substituted phenyl or certain heterocyclic groups; R 2 is hydrogen or methoxy; R 3 is hydrogen, lower alkyl or phenyl-lower alkyl; R 4 is lower alkyl, cycloalkyl, phenyl, substituted phenyl or certain heterocyclic groups; and X is hydrogen, lower alkanoyloxy, carbamoyloxy, lower alkoxy, lower alkylthio, ##STR2## or certain heterothio groups, are useful as antibacterial agents.

Inventors

  • 👤 Uwe D. Treuner
  • 👤 Hermann Breuer

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-29 22:39
CPC Classifications
C; C07; C07D; C07D307/00; C07D307/02; C07D307/34; C07D307/56; C07D307/68

Claims Analysis

Total Claims: 11
Claim 1
Independent Claim 177 words
A compound of the formula ##STR180## wherein R is hydrogen, lower alkyl, phenyl-lower alkyl, diphenyl-lower alkyl, tri(lower alkyl)silyl, trihaloethyl, aluminum, alkali metal, alkaline earth metal, phenyl-lower alkylamine, N,N-dibenzylethylenediamine, lower alkylamines, triethylamine, or N-lower alkylpiperidines; R 1 is hydrogen, lower alkyl, saturated or unsaturated cycloalkyl of up to 7 carbons, phenyl, phenyl-lower alkyl, substituted phenyl wherein said phenyl substituent is one or two members selected from the group consisting of halogen, lower alkyl, lower alkoxy, and hydroxy, or a heterocyclic selected from the group consisting of 2-thienyl, 3-thienyl, 2-furyl, 3-furyl, 2-pyridyl, 3-pyridyl, 4-pyridyl and 2-aminothiazolyl; R 2 is hydrogen or methoxy; R 3 is hydrogen, lower alkyl or phenyl-lower alkyl; R 4 is lower alkyl, cycloalkyl of up to 7 carbons, phenyl, substituted phenyl wherein the phenyl substituent is as defined above, or a heterocyclic selected from the group consisting of thienyl, furyl, pyridyl, thiazolyl and isothiazolyl; and X is hydrogen, lower alkanoyloxy, ##STR181## carbamoyloxy, lower alkoxy, lower alkylthio, or a heterothio group selected from the group consisting of ##STR182## and R 5 is hydrogen or lower alkyl.
Claim 2
Dependent Claim 177 words
A compound of the formula ##STR180## wherein R is hydrogen, lower alkyl, phenyl-lower alkyl, diphenyl-lower alkyl, tri(lower alkyl)silyl, trihaloethyl, aluminum, alkali metal, alkaline earth metal, phenyl-lower alkylamine, N,N-dibenzylethylenediamine, lower alkylamines, triethylamine, or N-lower alkylpiperidines; R 1 is hydrogen, lower alkyl, saturated or unsaturated cycloalkyl of up to 7 carbons, phenyl, phenyl-lower alkyl, substituted phenyl wherein said phenyl substituent is one or two members selected from the group consisting of halogen, lower alkyl, lower alkoxy, and hydroxy, or a heterocyclic selected from the group consisting of 2-thienyl, 3-thienyl, 2-furyl, 3-furyl, 2-pyridyl, 3-pyridyl, 4-pyridyl and 2-aminothiazolyl; R 2 is hydrogen or methoxy; R 3 is hydrogen, lower alkyl or phenyl-lower alkyl; R 4 is lower alkyl, cycloalkyl of up to 7 carbons, phenyl, substituted phenyl wherein the phenyl substituent is as defined above, or a heterocyclic selected from the group consisting of thienyl, furyl, pyridyl, thiazolyl and isothiazolyl; and X is hydrogen, lower alkanoyloxy, ##STR181## carbamoyloxy, lower alkoxy, lower alkylthio, or a heterothio group selected from the group consisting of ##STR182## and R 5 is hydrogen or lower alkyl.
Claim 3
Dependent Claim 11 words
A compound as in claim 1 wherein R 1 is thienyl.
Claim 4
Dependent Claim 11 words
A compound as in claim 1 wherein R 1 is phenyl.
Claim 5
Dependent Claim 10 words
A compound as in claim 1 wherein X is methyltetrazolyl.
Claim 6
Dependent Claim 16 words
A compound as in claim 1 wherein R, R 2 and R 3 each is hydrogen.
Claim 7
Dependent Claim 48 words
A compound as in claim 1 wherein R is hydrogen or alkali metal; R 1 is phenyl, thienyl or furyl; R 2 is hydrogen or methoxy; R 3 is hydrogen or lower alkyl; R 4 is lower alkyl or furyl; and X is as defined in claim 1.
Claim 8
Dependent Claim 38 words
A compound as in claim 1 wherein R is hydrogen, sodium or potassium; R 1 is phenyl, thienyl or furyl; R 2 and R 3 each is hydrogen; R 4 is furyl; and X is acetoxy or (1-methyl-1H-tetrazol-5-yl)thio.
Claim 9
Dependent Claim 28 words
A compound as in claim 1 wherein R, R 2 and R 3 each is hydrogen, R 1 is 2-thienyl; R 4 is 2-furyl; and X is (1-methyl-1H-tetrazol-5-yl)thio.
Claim 10
Dependent Claim 31 words
A compound as in claim 1 wherein R is alkali metal; R 2 and R 3 each is hydrogen; R 1 is 2-thienyl; R 4 is 2-furyl; and X is (1-methyl-1H-tetrazol-5-yl)thio.
Claim 11
Dependent Claim 28 words
A compound as in claim 1 wherein R, R 2 and R 3 each is hydrogen; R 1 and R 4 each is 2-furyl; and X is (1-methyl-1H-tetrazol-5-yl)thio.

References Cited (Backward Citations)

US4113943A Cited
US4096330A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1982-10-01 1983-04-02 1983-10-02 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1986-10-01 1987-04-02 1987-10-02 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1990-10-01 1991-04-02 1991-10-02 $7700.00 Window Closed / Lapsed

Assigned Categories & Tags

No categories assigned to this patent yet.

Assign Category Tag