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US4092476A Expired / Lapsed US ⏱️ 0.0 years remaining

Phthalidyl esters of 7-[(α amino, 2 substituted acetamido)-3-(heterocyclic-thio methyl)]cephalosporins

Assignee: Beecham Group PLC
•
Filing: 1976-12-29
•
Granted: 1978-05-30
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Expires: 1996-12-29
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Abstract

Abstract Phthalidyl and substituted phthalidyl esters of certain cephalosporins are absorbed by the oral route into the serum, where they are hydrolyzed to the parent antibacterially active cephalosporin.

Inventors

  • 👤 Peter Hubert Bentley
  • 👤 John Peter Clayton

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-29 10:02
CPC Classifications
C; C07; C07D; C07D501/00; C07D501/14; C07D501/16; C07D501/20; C07D501/24; C07D501/36; C07D501/26

Claims Analysis

Total Claims: 7
Claim 1
Independent Claim 57 words
A cephalosporin ester of the formula ##STR9## or a pharmaceutically acceptable acid addition salt thereof, wherein R is phenyl, 4-hydroxyphenyl, 3-chloro-4-hydrophenyl, 2- or 3-thienyl or dihydrophenyl; X is a heterocyclic thio group selected from the group consisting of ##STR10## (2-methyl-1,3,4-thiadiazol-5-yl) thio, (1-methyl-(1H)-1,2,3,4-tetrazol-5-yl) thio and (1H-1,3,4-triazol-5yl) thio; and R 1 and R 2 are both hydrogen or methoxy.
Claim 2
Dependent Claim 57 words
A cephalosporin ester of the formula ##STR9## or a pharmaceutically acceptable acid addition salt thereof, wherein R is phenyl, 4-hydroxyphenyl, 3-chloro-4-hydrophenyl, 2- or 3-thienyl or dihydrophenyl; X is a heterocyclic thio group selected from the group consisting of ##STR10## (2-methyl-1,3,4-thiadiazol-5-yl) thio, (1-methyl-(1H)-1,2,3,4-tetrazol-5-yl) thio and (1H-1,3,4-triazol-5yl) thio; and R 1 and R 2 are both hydrogen or methoxy.
Claim 3
Dependent Claim 16 words
A compound according to claim 1 wheren X is (2-methyl-1,3,4-thiadiazol-5-yl) thio, (1-methyl-(1H)-1,2,3,4-tetrazol-5-yl) thio or (1H-1,3,4-triazol-5-yl) thio.
Claim 4
Dependent Claim 9 words
The compound according to claim 1 which is phthalidyl-7-[D-α-aminophenylacetamido)-3-(2'-methyl-1',3',4'-thiadiazol-5'-yl)-thiomethyl]-ceph-3-em-carboxylate.
Claim 5
Dependent Claim 9 words
The compound according to claim 1 which is 5',6'-dimethoxyphthalidyl-7-[D-α-aminophenylacetamide-3-(2'-methyl-1',3',4'-thiadiazol-5-yl)-thiomethyl]-ceph-3-em-4-carboxylate.
Claim 6
Dependent Claim 9 words
The compound according to claim 1 which is phthalidyl-7-[D-α-aminophenylacetamido-3-(1'-methyl'1'-H-tetrazol-5-yl)-thiomethyl]-ceph-3-em-4-carboxylate.
Claim 7
Dependent Claim 39 words
A cephalosporin ester according to claim 1 in the form of an acid addition salt selected from the group consisting of the sulphate, nitrate, phosphate, borate, hydrochloride, hydrobromide, hydroiodide, acetate, oxalate, tartrate, maleate, citrate, succinate, benzoate, ascorbate and methanesulphonate.

References Cited (Backward Citations)

US3951954A Cited
US3963704A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1981-05-29 1981-11-28 1982-05-30 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1985-05-29 1985-11-28 1986-05-30 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1989-05-29 1989-11-28 1990-05-30 $7700.00 Window Closed / Lapsed

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