US3941774A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Aminoalkyl esters of penicillins
Assignee: Beecham Group PLC
•
Filing: 1973-05-21
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Granted: 1976-03-02
•
Expires: 1993-05-21
Abstract
Abstract Novel substituted amino methyl esters of penicillins and cephalosporins for oral administration which are much better absorbed than the parent compounds.
Inventors
- 👤 John Peter Clayton
- 👤 Kenneth David Hardy
- 👤 Angela Wendy Capel Guest
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-28 09:38
CPC Classifications
C; C07; C07D; C07D499/00; Y; Y02; Y02P; Y02P20/00; Y02P20/50; Y02P20/55
Claims Analysis
Total Claims: 12
Claim 1
Independent Claim
123 words
A compound of formula (I) or a pharmaceutically acceptable acid-addition salt thereof which contains a basic nitrogen atom: ##SPC13## wherein Y is alkyl of one to six carbon atoms, phenyl, benzyl, alkoxy of one to six carbon atoms, or benzyloxy; Z is alkyl of one to six carbon atoms, phenylbenzyl, alkoxy of one to six carbon atoms, cyclopentyl, cyclohexyl and phenyl, or Y+Z taken together are a 3-benzoxazolidine ring; R is phenylacetamido, 2- or 3-thienylacetamido, phenoxyacetamido, α-amino-phenylacetamido, α-amino-2- or 3-thienylacetamido, α-carboxyphenylacetamido, α-sulphophenyl-acetamido, α-azidophenylacetamido, α-guanidino-phenylacetamido, or N-tetrazolylacetamido, provided that: when Z is hydrogen, Y is alkoxy of one to six carbon atoms then R is not a group of formula (IV): ##EQU11## in which R 1 is C 2 -7 alkyl, phenyl, or furyl.
Claim 2
Dependent Claim
123 words
A compound of formula (I) or a pharmaceutically acceptable acid-addition salt thereof which contains a basic nitrogen atom: ##SPC13## wherein Y is alkyl of one to six carbon atoms, phenyl, benzyl, alkoxy of one to six carbon atoms, or benzyloxy; Z is alkyl of one to six carbon atoms, phenylbenzyl, alkoxy of one to six carbon atoms, cyclopentyl, cyclohexyl and phenyl, or Y+Z taken together are a 3-benzoxazolidine ring; R is phenylacetamido, 2- or 3-thienylacetamido, phenoxyacetamido, α-amino-phenylacetamido, α-amino-2- or 3-thienylacetamido, α-carboxyphenylacetamido, α-sulphophenyl-acetamido, α-azidophenylacetamido, α-guanidino-phenylacetamido, or N-tetrazolylacetamido, provided that: when Z is hydrogen, Y is alkoxy of one to six carbon atoms then R is not a group of formula (IV): ##EQU11## in which R 1 is C 2 -7 alkyl, phenyl, or furyl.
Claim 3
Dependent Claim
17 words
A compound as claimed in claim 1 wherein R is phenylacetamido, 2- or 3-thienylacetamido, α-aminophenylacetamido or N-tetrazolylacetamido.
Claim 4
Dependent Claim
18 words
A compound as claimed in claim 1 wherein Y is a C 1 -6 alkoxy or benzyloxy group.
Claim 5
Dependent Claim
17 words
A compound as claimed in claim 1 wherein Z is C 1 -6 alkyl, cyclopentyl or cyclohexyl.
Claim 6
Dependent Claim
11 words
A compound as claimed in claim 5 wherein Z is methyl.
Claim 7
Dependent Claim
36 words
A compound selected from the group consisting of: N-benzoylaminomethyl ester of penicillin G 3-benzoxazolidinone methyl ester of penicillin G N-acetylaminomethyl ester of penicillin G N propionylaminomethyl ester of penicillin G Benzoxazolidinone -3-methyl ester of ampicillin hydrochloride.
Claim 8
Dependent Claim
36 words
A compound selected from the group consisting of: N-benzoylaminomethyl ester of penicillin G 3-benzoxazolidinone methyl ester of penicillin G N-acetylaminomethyl ester of penicillin G N propionylaminomethyl ester of penicillin G Benzoxazolidinone -3-methyl ester of ampicillin hydrochloride.
Claim 9
Dependent Claim
5 words
(N-Ethoxycarbonyl-N-methyl)amino-methyl ester of penicillin G.
Claim 10
Dependent Claim
5 words
(N-Ethoxycarbonyl-N-methyl)amino-methyl ester of penicillin G.
Claim 11
Dependent Claim
5 words
(N-Acetyl-N-methyl)aminomethyl ester of penicillin G.
Claim 12
Dependent Claim
5 words
(N-Acetyl-N-methyl)aminomethyl ester of penicillin G.
References Cited (Backward Citations)
US3697507A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1979-03-02 | 1979-09-01 | 1980-03-02 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1983-03-02 | 1983-09-01 | 1984-03-02 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1987-03-02 | 1987-09-01 | 1988-03-02 | $7700.00 | Window Closed / Lapsed |