US3963704A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Penicillin esters
Assignee: Beecham Group PLC
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Filing: 1974-12-09
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Granted: 1976-06-15
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Expires: 1994-12-09
Abstract
Abstract This invention relates to a novel class of esters of penicillins and cephalosporins which, upon oral administration are absorbed into the bloodstream where they are split by enzymic action to release the antibacterially active parent penicillin or cephalosporin.
Inventors
- 👤 Harry Ferres
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-26 16:40
CPC Classifications
C; C07; C07D; C07D499/00; A; A61; A61P; A61P31/00; A61P31/04; C07C; C07C51/00; C07C51/16; C07C51/31; C07D307/00; C07D307/77; C07D307/87; C07D307/88; C07D317/00; C07D317/08; C07D317/44; C07D317/46; C07D317/48; C07D317/50; C07D317/58; C07D333/00; C07D333/50; C07D333/72; Y; Y02; Y02P; Y02P20/00; Y02P20/50; Y02P20/55
Claims Analysis
Total Claims: 5
Claim 1
Independent Claim
137 words
A compound of formula (I) or a pharmaceutically acceptable acid addition salt thereof: ##SPC4## wherein a. X and Y are both sulphur; or b. X is sulphur and Y is oxygen; or c. X is oxygen and y is sulphur; and wherein R is hydrogen, methyl or phenyl; Ra, Rb, Rc and Rd are selected from hydrogen, lower alkyl, lower alkoxy, halo and nitro and R 1 is an acylamino group selected from: phenylacetamido; p-hydroxyphenylacetamido; p-heptylphenylacetamido; phenoxyacetamido; α-phenoxypropionamido; α-phenoxybutyamido; 2,6-dimethoxyphenylacetamido; 3-phenyl-5-methyl-isoxazole-4-carbamido; 3-(2-chlorophenyl)-5-methyl-isoxazole-4-carbamido; 3-(2,6-dichlorophenyl)-5-methyl-isoxazole-4-carbamido; 3-(2-chloro-6-fluorophenyl)-5-methyl-isoxazole-4-carbamido; 2-ethoxy-naphthyl-1-carbamido; o, m or p-aminophenlyacetamido; 3-carboxy-quinoxalin-2-carbamido; 2-furylacetamido; 2-thienylacetamido; 3-thienylacetamido; 3-pyridylacetamido; isothiazolyacetamido; 3-hexenamido; 2-biphenylamido; n-hexanamido; n-octanamido; propionamido; α-aminophenylacetamido; α-amino-2-thienylacetamido; α-amino-3-thienylacetamido; α-methylaminoacetamido; α-amino-2- or -3-or -4-chlorophenylacetamido; α-amino-2-methoxyphenylacetamido; α-amino-2,4-dichlorophenylacetamido; α-amino-3,4-dichlorophenylacetamido; α-amino-α-methylphenylacetamido; α-amino-4-hydroxyphenylacetamido; α-amino-3-chloro-4-hydroxyphenylacetamido; α-methylphenylacetamido; α-hydroxyphenylacetamido; α-carboxyphenylacetamido; α-(5-tetrazolyl)phenylacetamido; α-guanidino-2-thienylacetamido; α-guanidino-4-hydroxyphenylacetamido; α-guanidino-4-hydroxy-2- or -3-methylphenylacetamido; α-carboxy-3-thienylacetamido; α-sulphaminophenylacetamido; α-sulphamino-3-thienylacetamido; α-(N-methylsulphamino)-phenylacetamido; α-azidophenylacetamido; 1-aminocyclohexylcarbamido; 1-aminocyclopentylcarbamido; 5-amino-5-carboxypentanamido; α-phenoxyphenylacetamido; α-phenyl-β-sulphaminopropionamido; α-sulphophenylacetamido; α-guanidinophenylacetamido; β-amino-β-cyclohexylpropionamido; α-(benzyloxycarbonyl)phenylacetamido.
Claim 2
Dependent Claim
137 words
A compound of formula (I) or a pharmaceutically acceptable acid addition salt thereof: ##SPC4## wherein a. X and Y are both sulphur; or b. X is sulphur and Y is oxygen; or c. X is oxygen and y is sulphur; and wherein R is hydrogen, methyl or phenyl; Ra, Rb, Rc and Rd are selected from hydrogen, lower alkyl, lower alkoxy, halo and nitro and R 1 is an acylamino group selected from: phenylacetamido; p-hydroxyphenylacetamido; p-heptylphenylacetamido; phenoxyacetamido; α-phenoxypropionamido; α-phenoxybutyamido; 2,6-dimethoxyphenylacetamido; 3-phenyl-5-methyl-isoxazole-4-carbamido; 3-(2-chlorophenyl)-5-methyl-isoxazole-4-carbamido; 3-(2,6-dichlorophenyl)-5-methyl-isoxazole-4-carbamido; 3-(2-chloro-6-fluorophenyl)-5-methyl-isoxazole-4-carbamido; 2-ethoxy-naphthyl-1-carbamido; o, m or p-aminophenlyacetamido; 3-carboxy-quinoxalin-2-carbamido; 2-furylacetamido; 2-thienylacetamido; 3-thienylacetamido; 3-pyridylacetamido; isothiazolyacetamido; 3-hexenamido; 2-biphenylamido; n-hexanamido; n-octanamido; propionamido; α-aminophenylacetamido; α-amino-2-thienylacetamido; α-amino-3-thienylacetamido; α-methylaminoacetamido; α-amino-2- or -3-or -4-chlorophenylacetamido; α-amino-2-methoxyphenylacetamido; α-amino-2,4-dichlorophenylacetamido; α-amino-3,4-dichlorophenylacetamido; α-amino-α-methylphenylacetamido; α-amino-4-hydroxyphenylacetamido; α-amino-3-chloro-4-hydroxyphenylacetamido; α-methylphenylacetamido; α-hydroxyphenylacetamido; α-carboxyphenylacetamido; α-(5-tetrazolyl)phenylacetamido; α-guanidino-2-thienylacetamido; α-guanidino-4-hydroxyphenylacetamido; α-guanidino-4-hydroxy-2- or -3-methylphenylacetamido; α-carboxy-3-thienylacetamido; α-sulphaminophenylacetamido; α-sulphamino-3-thienylacetamido; α-(N-methylsulphamino)-phenylacetamido; α-azidophenylacetamido; 1-aminocyclohexylcarbamido; 1-aminocyclopentylcarbamido; 5-amino-5-carboxypentanamido; α-phenoxyphenylacetamido; α-phenyl-β-sulphaminopropionamido; α-sulphophenylacetamido; α-guanidinophenylacetamido; β-amino-β-cyclohexylpropionamido; α-(benzyloxycarbonyl)phenylacetamido.
Claim 3
Dependent Claim
10 words
The compound of claim 1 which is 2-thiophthalide 6 penicillanate.
Claim 4
Dependent Claim
18 words
The compound of claim 1 which is 2-thiophthalide 6 penicillanate or a pharmaceutically acceptable acid addition salt thereof.
Claim 5
Dependent Claim
10 words
The compound of claim 1 which is 2-thiophthalide 6 penicillanate.
References Cited (Backward Citations)
US3652546A
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US3697507A
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US3719668A
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US3726861A
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GB1377661A
Cited
US3860579A
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1979-06-15 | 1979-12-15 | 1980-06-15 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1983-06-15 | 1983-12-15 | 1984-06-15 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1987-06-15 | 1987-12-15 | 1988-06-15 | $7700.00 | Window Closed / Lapsed |