US4281002A
Expired / Lapsed
US
⏱️ 0.0 years remaining
3-(2-Aminoethylthio)-6-amido-7-oxo-1-azabicyclo(3.2.0)-hept-2-ene-2-carboxylic acid
Assignee: Merck and Co Inc
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Filing: 1979-10-03
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Granted: 1981-07-28
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Expires: 1999-10-03
Abstract
Abstract Disclosed are 3-(2-aminoethylthio)-6-amido-7-oxo-1-azabicyclo [3.2.0]hept-2-ene-2-carboxylic acids having the structure: <IMAGE> wherein R1 is hydrogen or acyl. Such compounds as well as their pharmaceutically acceptable salt, ester and amide derivatives are useful as antibiotics. Also disclosed are processes for the preparation of such compounds, pharmaceutical compositions comprising such compounds and methods of treatment comprising administering such compounds and compositions when an antibiotic effect is indicated.
Inventors
- 👤 Burton G. Christensen
- 👤 Ravindra N. Guthikonda
- 👤 David B. R. Johnston
- 👤 Susan M. Schmitt
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-03 05:46
CPC Classifications
C; C07; C07D; C07D205/00; C07D205/02; C07D205/06; C07D205/08; C07D205/085; C07C; C07C205/00; C07C205/39; C07C205/42; C07D477/00; C07D477/10; C07D477/24; C07F; C07F7/00; C07F7/02; C07F7/08; C07F7/10
Claims Analysis
Total Claims: 4
Claim 1
Independent Claim
17 words
An antibiotic pharmaceutical composition comprising a therapeutically effective amount of a compound and a pharmaceutical carrier therefor.
Claim 2
Dependent Claim
17 words
An antibiotic pharmaceutical composition comprising a therapeutically effective amount of a compound and a pharmaceutical carrier therefor.
Claim 3
Dependent Claim
67 words
A compound having the structure: ##STR74## wherein R is hydrogen, the pharmaceutically acceptable salts or cations or lower alkyl having 1-4 carbon atoms; lower alkenyl having 1-4 carbon atoms; benzyl, p-nitrobenzyl, pivaloyloxymethyl, 3-phthalidyl or phenacyl; and R 1 is 2-furylacetyl, 5-nitrofurylacetyl, 3-furylacetyl, 2-thienylacetyl, 5-chlorothienylacetyl, 5-methoxythienylacetyl, α-guanidino-2-thienylacetyl, 3-thienylacetyl, 4-methylthienylacetyl, 3-isothiazolylacetyl, 4-methoxyisothiazolylacetyl, 4-isothiazolylacetyl, 3-methylisothiazolylacetyl, 5-isothiazolylacetyl, 3-chloroisothiazolylacetyl, 3-methyl-1,2,5-oxadiazolylacetyl, 1,2,5-thiadiazolyl-4-acetyl, 3-methyl-1,2,5-thiadiazolyl-4-acetyl, 3-chloro-1,2,5-thiadiazolyl-4-acetyl, 3-methoxy-1,2,5-thiadiazolyl-4-acetyl, 4-pyridylthioacetyl, cyanoacetyl, tetrazolylacetyl, 2-thienylglycyl, 3-thienylglycyl, 2-thienylmalonyl and 3-thienylmalonyl.
Claim 4
Dependent Claim
67 words
A compound having the structure: ##STR74## wherein R is hydrogen, the pharmaceutically acceptable salts or cations or lower alkyl having 1-4 carbon atoms; lower alkenyl having 1-4 carbon atoms; benzyl, p-nitrobenzyl, pivaloyloxymethyl, 3-phthalidyl or phenacyl; and R 1 is 2-furylacetyl, 5-nitrofurylacetyl, 3-furylacetyl, 2-thienylacetyl, 5-chlorothienylacetyl, 5-methoxythienylacetyl, α-guanidino-2-thienylacetyl, 3-thienylacetyl, 4-methylthienylacetyl, 3-isothiazolylacetyl, 4-methoxyisothiazolylacetyl, 4-isothiazolylacetyl, 3-methylisothiazolylacetyl, 5-isothiazolylacetyl, 3-chloroisothiazolylacetyl, 3-methyl-1,2,5-oxadiazolylacetyl, 1,2,5-thiadiazolyl-4-acetyl, 3-methyl-1,2,5-thiadiazolyl-4-acetyl, 3-chloro-1,2,5-thiadiazolyl-4-acetyl, 3-methoxy-1,2,5-thiadiazolyl-4-acetyl, 4-pyridylthioacetyl, cyanoacetyl, tetrazolylacetyl, 2-thienylglycyl, 3-thienylglycyl, 2-thienylmalonyl and 3-thienylmalonyl.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1984-07-27 | 1985-01-26 | 1985-07-28 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1988-07-27 | 1989-01-26 | 1989-07-28 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1992-07-27 | 1993-01-26 | 1993-07-28 | $7700.00 | Window Closed / Lapsed |