US4536393A
Expired / Lapsed
US
⏱️ 0.0 years remaining
6-(Aminomethyl)penicillanic acid 1,1-dioxide esters and intermediates therefor
Assignee: Pfizer Inc
•
Filing: 1984-02-06
•
Granted: 1985-08-20
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Expires: 2004-02-06
Abstract
Abstract 6-alpha- and 6-beta-(Aminomethyl)penicillanic acid, 1,1-dioxide esters which are hydrolyzable under physiological conditions, particularly those wherein the ester radical is 1H-isobenzofuran-3-on-1-yl or (5-methyl-1,3-dioxol-2-on-4-yl)methyl, and an improved process and intermediates used in their synthesis.
Inventors
- 👤 Wayne E. Barth
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-25 12:57
CPC Classifications
C; C07; C07D; C07D307/00; C07D307/77; C07D307/87; C07D307/88; C07D499/00
Claims Analysis
Total Claims: 19
Claim 1
Independent Claim
19 words
A beta-lactam ester of the formula ##STR11## wherein Y is ##STR12## or a pharmaceutically acceptable acid addition salt thereof.
Claim 2
Dependent Claim
19 words
A beta-lactam ester of the formula ##STR11## wherein Y is ##STR12## or a pharmaceutically acceptable acid addition salt thereof.
Claim 3
Dependent Claim
9 words
A compound of claim 1 of the formula (I).
Claim 4
Dependent Claim
9 words
The compound of claim 2 wherein Y is ##STR13##
Claim 5
Dependent Claim
9 words
The compound of claim 2 wherein Y is ##STR14##
Claim 6
Dependent Claim
33 words
A pharmaceutical composition fore treating bacterial infections which comprises an antibacterially effective amount of a compound of claim 1 and a conventional beta-lactam antibiotic in a weight ratio of 1:3 to 3:1 .
Claim 7
Dependent Claim
32 words
A pharmaceutical composition for treating bacterial infections which comprises an antibacterial effective amount of the compound of claim 3 and a conventional beta-lactam antibiotic in a weight ratio of 1:3 to 3:1.
Claim 8
Dependent Claim
31 words
A pharmaceutical composition for treating bacterial infections which comprises an antibacterial amount of the compound of claim 4 and a conventional beta-lactam antibiotic in a weight ratio of 1:3 to 3:1.
Claim 9
Dependent Claim
27 words
A method of treating a bacterial infection in a mammal which comprises administering to said mammal an antibacterially effective amount of a pharmaceutical composition of claim 5.
Claim 10
Dependent Claim
27 words
A method of treating a bacterial infection in a mammal which comprises administering to said mammal an antibacterially effective amount of a pharmaceutical composition of claim 6.
Claim 11
Dependent Claim
27 words
A method of treating a bacterial infection in a mammal which comprises administering to said mammal an antibacterially effective amount of a pharmaceutical composition of claim 7.
Claim 12
Dependent Claim
40 words
A compound of the formula ##STR15## wherein Y' is (C 1 -C 3 )alkyl and R 1 is hydrogen, or a conventional ester forming radical which is hydrolyzable under physiological conditions, or cationic salts therof when R 1 is hydrogen.
Claim 13
Dependent Claim
40 words
A compound of the formula ##STR15## wherein Y' is (C 1 -C 3 )alkyl and R 1 is hydrogen, or a conventional ester forming radical which is hydrolyzable under physiological conditions, or cationic salts therof when R 1 is hydrogen.
Claim 14
Dependent Claim
38 words
A compound of claim 11 wherein said ester forming radical is: ##STR16## --CHR 2 OCOR 3 or --CHR 2 OCOOR 3 , wherein R 2 is hydrogen or methyl and R 3 is (C 1 -C 6 )alkyl.
Claim 15
Dependent Claim
11 words
A compound of claim 12 wherein R 1 is hydrogen, ##STR17##
Claim 16
Dependent Claim
13 words
A compound of claim 13 having the formula (III) wherein Y' is methyl.
Claim 17
Dependent Claim
17 words
The compound of claim 14 wherein R 1 is hydrogen in the form of its tetrabutylammonium salt.
Claim 18
Dependent Claim
10 words
The compound of claim 14 wherein R 1 is ##STR18##
Claim 19
Dependent Claim
10 words
The compound of claim 14 wherein R 1 is ##STR19##
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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) | 1988-08-19 | 1989-02-18 | 1989-08-20 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1992-08-19 | 1993-02-18 | 1993-08-20 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1996-08-19 | 1997-02-18 | 1997-08-20 | $7700.00 | Window Closed / Lapsed |