US4281116A
Expired / Lapsed
US
⏱️ 0.0 years remaining
3-Halo cephalosporins
Assignee: Eli Lilly and Co
•
Filing: 1980-07-02
•
Granted: 1981-07-28
•
Expires: 2000-07-02
Abstract
Abstract 7-Acylamido- and 7-amino-3-halo-3-cephem-4-carboxylic acids, esters and pharmaceutically-acceptable salts and esters thereof are new cephalosporin compounds provided by the reaction of a 7-acylamido-3-hydroxy-3-cephem-4-carboxylic acid ester or a 7-amino-3-hydroxy-3-cephem-4-carboxylic acid ester with an iodinating, fluorinating, chlorinating, or brominating reagent. For example, 7-amino-3-chloro-3-cephem-4-carboxylic acid and 7-phenoxyacetamido-3-chloro-3-cephem-4-carboxylic acid are provided. The 7-acylamido-3-halo cephalosporin acids and pharmaceutically acceptable salts and esters provided are valuable antibiotic compounds having desirable therapeutic properties.
Inventors
- 👤 Robert R. Chauvette
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-01 10:07
CPC Classifications
C; C07; C07D; C07D501/00; C07D501/14; C07D501/16; C07D501/59
Claims Analysis
Total Claims: 5
Claim 1
Independent Claim
67 words
A compound of the formula ##STR51## wherein a and a' independently are hydrogen, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, halogen, hydroxy, nitro, amino, or carboxy; R 1 is hydrogen, benzyl, p-methoxybenzyl, p-nitrobenzyl, diphenylmethyl, 2,2,2-trichloroethyl, t-butyl, or a pharmaceutically acceptable ester of the formula ##STR52## X is fluoro, chloro, bromo or iodo; and when R 1 is hydrogen the non-toxic pharmaceutically acceptable salts thereof.
Claim 2
Dependent Claim
67 words
A compound of the formula ##STR51## wherein a and a' independently are hydrogen, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, halogen, hydroxy, nitro, amino, or carboxy; R 1 is hydrogen, benzyl, p-methoxybenzyl, p-nitrobenzyl, diphenylmethyl, 2,2,2-trichloroethyl, t-butyl, or a pharmaceutically acceptable ester of the formula ##STR52## X is fluoro, chloro, bromo or iodo; and when R 1 is hydrogen the non-toxic pharmaceutically acceptable salts thereof.
Claim 3
Dependent Claim
9 words
The compound of claim 1 wherein X is chloro.
Claim 4
Dependent Claim
12 words
The compound of claim 2 wherein a and a' are both hydrogen.
Claim 5
Dependent Claim
10 words
The compound of claim 3 wherein R 1 is hydrogen.
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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) | 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 |