US4252802A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Hydroxamic acid derivatives of 7-[(2-amino-4-thiazolyl)-oximino] cephalosporins
Assignee: ER Squibb and Sons LLC
•
Filing: 1980-03-13
•
Granted: 1981-02-24
•
Expires: 2000-03-13
Abstract
Abstract A compound of the formula ##STR1## wherein R is hydrogen, alkali metal, ##STR2## or ##STR3## R 1 is hydrogen or methyl; R 2 is hydrogen or methyl; R 3 is hydrogen, lower alkyl or lower alkylphenyl; R 4 is hydrogen, --OCONH 2 , ##STR4## R 7 is hydrogen or lower alkyl; R 8 is hydrogen or --CONH 2 ; R 9 is hydrogen, lower alkyl, ##STR5## or --(CH 2 ) p --N--(lower alkyl) 2 ; R 10 is hydrogen or lower alkyl; R 11 is hydrogen, sodium or potassium; n is 1, 2, 3 or 4; m is 0, 1 or 2; p is 1, 2, 3 or 4.
Inventors
- 👤 Theodor Denzel
- 👤 Hermann Breuer
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-01 08:20
CPC Classifications
C; C07; C07D; C07D209/00; C07D209/02; C07D209/44; C07D209/48; A; A61; A61P; A61P31/00; A61P31/04; C07D277/00; C07D277/02; C07D277/20; C07D277/587; Y; Y02; Y02P; Y02P20/00; Y02P20/50; Y02P20/55
Claims Analysis
Total Claims: 10
Claim 1
Independent Claim
98 words
A compound of the formula ##STR122## wherein R is hydrogen, alkali metal, ##STR123## R 1 is hydrogen or methyl; R 2 is hydrogen or methyl; R 3 is hydrogen, lower alkyl or lower alkylphenyl; R 4 is hydrogen, --OCONH 2 , ##STR124## R 7 is hydrogen or lower alkyl; R 8 is hydrogen or --CONH 2 ; R 9 is hydrogen, lower alkyl, ##STR125## R 10 is hydrogen or lower alkyl; R 11 is hydrogen, sodium or potassium; n is 1, 2, 3 or 4; m is 0, 1 or 2; p is 1, 2, 3 or 4.
Claim 2
Dependent Claim
98 words
A compound of the formula ##STR122## wherein R is hydrogen, alkali metal, ##STR123## R 1 is hydrogen or methyl; R 2 is hydrogen or methyl; R 3 is hydrogen, lower alkyl or lower alkylphenyl; R 4 is hydrogen, --OCONH 2 , ##STR124## R 7 is hydrogen or lower alkyl; R 8 is hydrogen or --CONH 2 ; R 9 is hydrogen, lower alkyl, ##STR125## R 10 is hydrogen or lower alkyl; R 11 is hydrogen, sodium or potassium; n is 1, 2, 3 or 4; m is 0, 1 or 2; p is 1, 2, 3 or 4.
Claim 3
Dependent Claim
106 words
The compound of claim 1 wherein the ##STR126## group is in the syn configuration; n is one or two m is zero or one provided that when m is one the sulfoxide is in the β-configuration; R is hydrogen, sodium, potassium, ##STR127## or --CH 2 O--CO--lower alkyl; R 1 and R 2 are independently selected from hydrogen and methyl; R 3 is hydrogen, lower alkyl or lower alkylphenyl; R 4 is ##STR128## R 8 is hydrogen or ##STR129## R 9 is hydrogen, methyl, --(CH 2 ) p --N(CH 3 ) 2 , ##STR130## R 11 is hydrogen, sodium or potassium and p is 1 or 2.
Claim 4
Dependent Claim
10 words
The compound of claim 2 wherein R 4 is ##STR131##
Claim 5
Dependent Claim
8 words
The compound of claim 3, [6R-[6α, 7β(Z)]]-3-[acetyloxy)methyl]-7-[[(2-amino-4-thiazolyl)]2-oxo-2-[(phenylmethoxy)-amino]ethoxy]imino]acetyl]amino]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid.
Claim 6
Dependent Claim
10 words
The compound of claim 3, [6R-[6α, 7β(Z)]]-3-[(acetyloxy)methyl]-7-[[(2-amino-4-thiazolyl)[[2-oxo-2-[(phenylmethoxy)-amino]ethoxy]imino]acetyl]amino]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid, sodium salt.
Claim 7
Dependent Claim
17 words
The compound of claim 2 wherein R 4 is ##STR132## and R 9 is hydrogen or methyl.
Claim 8
Dependent Claim
125 words
An antibacterial pharmaceutical composition comprising a pharmaceutically acceptable carrier and an effective amount of one or more antibacterially active compounds of the formula ##STR133## wherein R is hydrogen, alkali metal, ##STR134## R 1 is hydrogen or methyl; R 2 is hydrogen or methyl; R 3 is hydrogen, lower alkyl or lower alkylphenyl; R 4 is hydrogen, --OCONH 2 , ##STR135## R 7 is hydrogen or lower alkyl; R 8 is hydrogen or --CONH 2 ; R 9 is hydrogen, lower alkyl, ##STR136## or --(CH 2 ) p --N--(lower alkyl) 2 ; R 10 is hydrogen or lower alkyl; R 11 is hydrogen, sodium or potassium; n is 1, 2, 3 or 4; m is 0, 1 or 2; p is 1, 2, 3 or 4.
Claim 9
Dependent Claim
125 words
An antibacterial pharmaceutical composition comprising a pharmaceutically acceptable carrier and an effective amount of one or more antibacterially active compounds of the formula ##STR133## wherein R is hydrogen, alkali metal, ##STR134## R 1 is hydrogen or methyl; R 2 is hydrogen or methyl; R 3 is hydrogen, lower alkyl or lower alkylphenyl; R 4 is hydrogen, --OCONH 2 , ##STR135## R 7 is hydrogen or lower alkyl; R 8 is hydrogen or --CONH 2 ; R 9 is hydrogen, lower alkyl, ##STR136## or --(CH 2 ) p --N--(lower alkyl) 2 ; R 10 is hydrogen or lower alkyl; R 11 is hydrogen, sodium or potassium; n is 1, 2, 3 or 4; m is 0, 1 or 2; p is 1, 2, 3 or 4.
Claim 10
Dependent Claim
23 words
The method of treating antibacterial infections in a mammalian specie which comprises internally administering an effective amount of the composition of claim 7.
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) | 1984-02-24 | 1984-08-25 | 1985-02-24 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1988-02-24 | 1988-08-25 | 1989-02-24 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1992-02-24 | 1992-08-25 | 1993-02-24 | $7700.00 | Window Closed / Lapsed |