US4263291A
Expired / Lapsed
US
⏱️ 0.0 years remaining
3,7-Disubstituted-3-cephem-4-carboxylic acid compounds and processes for the preparation thereof
Assignee: Astellas Pharma Inc
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Filing: 1979-04-03
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Granted: 1981-04-21
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Expires: 1999-04-03
Abstract
Abstract 3,7-Disubstituted-3-cephem-4-carboxylic acid compounds having bacteriostatic properties and the following formula: <IMAGE> in which R1 is thiadiazolyl or isothiazolyl, each of which may have suitable substituent(s), or thiazolyl; R2 is hydrogen or lower alkyl; R3 is carboxy or protected carboxy; R4 is hydrogen, acyloxy or a heterocyclicthio group which may have suitable substituent(s); and R5 is hydrogen or lower alkoxy, process for making same and treating infectious diseases therewith.
Inventors
- 👤 Takao Takaya
- 👤 Hisashi Takasugi
- 👤 Toshiyuki Chiba
- 👤 Zenzaburo Tozuka
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-10 00:59
CPC Classifications
C; C07; C07D; C07D275/00; C07D275/02; A; A61; A61P; A61P31/00; A61P31/04; C07D285/00; C07D285/01; C07D285/02; C07D285/04; C07D285/06; C07D285/10; C07D285/12; Y; Y02; Y02P; Y02P20/00; Y02P20/50; Y02P20/55
Claims Analysis
Total Claims: 8
Claim 1
Independent Claim
51 words
3,7-disubstituted-3-cephem-4-carboxylic acid (syn isomer) compounds of the formula: ##STR7## wherein R 1 is 1,2,3-thiadiazolyl; R 2 is lower alkyl; R 3 is carboxy or carboxy group protected by an eliminatable protective group; and R 4 is tetrazolylthio which may be substituted with lower alkyl or di(lower)alkylamino(lower)alkyl; and pharmaceutically acceptable salts thereof.
Claim 2
Dependent Claim
51 words
3,7-disubstituted-3-cephem-4-carboxylic acid (syn isomer) compounds of the formula: ##STR7## wherein R 1 is 1,2,3-thiadiazolyl; R 2 is lower alkyl; R 3 is carboxy or carboxy group protected by an eliminatable protective group; and R 4 is tetrazolylthio which may be substituted with lower alkyl or di(lower)alkylamino(lower)alkyl; and pharmaceutically acceptable salts thereof.
Claim 3
Dependent Claim
10 words
The compounds of claim 1, wherein R 3 is carboxy.
Claim 4
Dependent Claim
17 words
The compounds of claim 2, wherein R 4 is tetrazolylthio having a lower alkyl or a di(lower)alkylamino(lower)alkyl.
Claim 5
Dependent Claim
21 words
The compounds of claim 3, wherein R 2 is methyl, and R 4 is 1H-tetrazolylthio having a methyl or a dimethylaminoethyl.
Claim 6
Dependent Claim
11 words
The compound of claim 4, which is 7-[2-methoxyimino-2-(1,2,3-thiadiazol-4-yl)acetamido]-3-(1-methyl-1H-tetrazol-5-yl)thiomethyl-3-cephem-4-carboxylic acid (syn isomer.)
Claim 7
Dependent Claim
11 words
The compound of claim 4, which is 7-[2-methoxyimino-2-(1,2,3-thiadiazol-4-yl)acetamido]-3-[1-(2-dimethylaminoethyl)-1H-tetrazol-5-yl]thiomethyl-3-cephem-4-carboxylic acid (syn isomer).
Claim 8
Dependent Claim
20 words
An antibacterial composition comprising a compound of claim 1 in association with a pharmaceutically acceptable, substantially non-toxic carrier or excipient.
References Cited (Backward Citations)
US4091209A
Cited
US4076936A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1984-04-20 | 1984-10-20 | 1985-04-21 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1988-04-20 | 1988-10-20 | 1989-04-21 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1992-04-20 | 1992-10-20 | 1993-04-21 | $7700.00 | Window Closed / Lapsed |