Patent US4154830A successfully refreshed from Google Patents.
US4154830A
Expired / Lapsed
US
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Unsaturated derivatives of 7-acylamido-3-cephem-4-carboxylic acid
Assignee: Pfizer Italia SRL
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Filing: 1977-08-08
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Granted: 1979-05-15
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Expires: 1997-08-08
Abstract
Abstract Unsaturated derivatives of 7-acylamido-3-cephem-4-carboxylic acid are disclosed which exhibit antibacterial activity against Gram-positive and Gram-negative microorganisms and can be used to treat infections caused by such microorganisms.
Inventors
- 👤 Giuliano Nannini
- 👤 Ettore Perrone
- 👤 Dino Severino
- 👤 Giuseppe Meinardi
- 👤 Gisella Monti
- 👤 Alberta Bianchi
- 👤 Angelo Forgione
- 👤 Carlo Confalonieri
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-10 00:54
CPC Classifications
C; C07; C07D; C07D501/00; C07D501/14; C07D501/16; C07D501/20; C07D501/24; C07D501/26; C07D501/28; C07C; C07C323/00; C07C323/50; C07C323/51; C07C323/60; A; A61; A61P; A61P31/00; A61P31/04; C07D501/36
Claims Analysis
Total Claims: 33
Claim 1
Independent Claim
84 words
A compound of formula (I) ##STR29## wherein Z is cyano or carbamoyl; A is trans --CH═CH or cis --CH═CH; B is -S-Het wherein Het is one of the following groups ##STR30## wherein R is hydrogen or methyl, or ##STR31## wherein R 1 and R 2 are independently selected from the goup consisting of hydrogen and methyl; X is a free or esterified carboxy group, and the pharmaceutically or veterinarily acceptable salts of the compound of formula (I) wherein X is a free carboxy group.
Claim 2
Dependent Claim
84 words
A compound of formula (I) ##STR29## wherein Z is cyano or carbamoyl; A is trans --CH═CH or cis --CH═CH; B is -S-Het wherein Het is one of the following groups ##STR30## wherein R is hydrogen or methyl, or ##STR31## wherein R 1 and R 2 are independently selected from the goup consisting of hydrogen and methyl; X is a free or esterified carboxy group, and the pharmaceutically or veterinarily acceptable salts of the compound of formula (I) wherein X is a free carboxy group.
Claim 3
Dependent Claim
17 words
Compound of claim 1, wherein X is a free carboxy group or a pharmaceutically acceptable salt thereof.
Claim 4
Dependent Claim
35 words
The compound of claim 1, wherein Z is cyano, A is cis--CH═CH--, B is ##STR32## wherein R, R 1 and R 2 are as defined in claim 1 and X is free or salified carboxy.
Claim 5
Dependent Claim
13 words
The compound of claim 3, wherein A is cis--CH═CH-- and B is ##STR33##
Claim 6
Dependent Claim
2 words
7-[β-cyano-ethylene(trans)-thio-acetamido]-3-[(1-methyl-1,2,3,4-tetrazol-5-yl)-thiomethyl]-3-cephem-4-carboxylic acid.
Claim 7
Dependent Claim
2 words
7-[β-cyano-ethylene(trans)-thio-acetamido]-3-[(1-methyl-1,2,3,4-tetrazol-5-yl)-thiomethyl]-3-cephem-4-carboxylic acid.
Claim 8
Dependent Claim
2 words
7-[β-cyano-ethylene(trans)-thio-acetamido]-[(1,3,4-thiadiazol-2-yl)-thiomethyl]-3-cephem-4-carboxylic acid.
Claim 9
Dependent Claim
2 words
7-[β-cyano-ethylene(trans)-thio-acetamido]-[(1,3,4-thiadiazol-2-yl)-thiomethyl]-3-cephem-4-carboxylic acid.
Claim 10
Dependent Claim
2 words
7-[β-cyano-ethylene(cis)-thio-acetamido]-[(1-methyl-1,2,3,4-tetrazol-5-yl)-thiomethyl]-3-cephem-4-carboxylic acid.
Claim 11
Dependent Claim
2 words
7-[β-cyano-ethylene(cis)-thio-acetamido]-[(1-methyl-1,2,3,4-tetrazol-5-yl)-thiomethyl]-3-cephem-4-carboxylic acid.
Claim 12
Dependent Claim
2 words
7-[β-cyano-ethylene(cis)-thio-acetamido]-3-[(1,3,4-thiadiazol-2-yl)-thiomethyl]-3-cephem-4-carboxylic acid.
Claim 13
Dependent Claim
2 words
7-[β-cyano-ethylene(cis)-thio-acetamido]-3-[(1,3,4-thiadiazol-2-yl)-thiomethyl]-3-cephem-4-carboxylic acid.
Claim 14
Dependent Claim
2 words
7-[β-carboxyamido-ethylene(trans)-thio-acetamido]-3-[(1-methyl-1,2,3,4-tetrazol-5-yl)-thiomethyl]-3-cephem-4-carboxylic acid.
Claim 15
Dependent Claim
2 words
7-[β-carboxyamido-ethylene(trans)-thio-acetamido]-3-[(1-methyl-1,2,3,4-tetrazol-5-yl)-thiomethyl]-3-cephem-4-carboxylic acid.
Claim 16
Dependent Claim
2 words
7-[β-carboxamido-ethylene(cis)-thio-acetamido]-3-[(1-methyl-1,2,3,4-tetrazol-5-yl)-thiomethyl]-3-cephem-4-carboxylic acid.
Claim 17
Dependent Claim
2 words
7-[β-carboxamido-ethylene(cis)-thio-acetamido]-3-[(1-methyl-1,2,3,4-tetrazol-5-yl)-thiomethyl]-3-cephem-4-carboxylic acid.
Claim 18
Dependent Claim
2 words
7-[β-cyano-ethylene(cis)-thio-acetamido]-3-[(5-methyl-1,3,4-triazol-2-yl)-thiomethyl]-3-cephem-4-carboxylic acid.
Claim 19
Dependent Claim
2 words
7-[β-cyano-ethylene(cis)-thio-acetamido]-3-[(5-methyl-1,3,4-triazol-2-yl)-thiomethyl]-3-cephem-4-carboxylic acid.
Claim 20
Dependent Claim
2 words
7-[β-cyano-ethylene(cis)-thio-acetamido]-3-[(1-methyl-1,3,4-triazol-2-yl)-thiomethyl]-3-cephem-4-carboxylic acid.
Claim 21
Dependent Claim
2 words
7-[β-cyano-ethylene(cis)-thio-acetamido]-3-[(1-methyl-1,3,4-triazol-2-yl)-thiomethyl]-3-cephem-4-carboxylic acid.
Claim 22
Dependent Claim
2 words
7-[β-cyano-ethylene(trans)-thio-acetamido]-3-[(1-methyl-1,3,4-triazol-2-yl)-thiomethyl]-3-cephem-4-carboxylic acid,
Claim 23
Dependent Claim
2 words
7-[β-cyano-ethylene(trans)-thio-acetamido]-3-[(1-methyl-1,3,4-triazol-2-yl)-thiomethyl]-3-cephem-4-carboxylic acid,
Claim 24
Dependent Claim
22 words
A pharmaceutically or veterinarily acceptable salt of each of the compounds of claims 5 to 8, 9, 10 and 11 to 13.
Claim 25
Dependent Claim
12 words
The salt of claim 14, wherein said salt is an alkaline salt.
Claim 26
Dependent Claim
12 words
The salt of claim 15 wherein said salt is the sodium salt.
Claim 27
Dependent Claim
12 words
The salt of claim 15, wherein said salt is the potassium salt.
Claim 28
Dependent Claim
15 words
Compound of claim 1, wherein Het is ##STR34## wherein R is defined in claim 1.
Claim 29
Dependent Claim
28 words
A compound of the formula (I) ##STR35## wherein Z is cyano or carbamoyl; A is cis--CH═CH--; ##STR36## X is carboxy, and the pharmaceutically or veterinarily acceptable salts thereof.
Claim 30
Dependent Claim
28 words
A compound of the formula (I) ##STR35## wherein Z is cyano or carbamoyl; A is cis--CH═CH--; ##STR36## X is carboxy, and the pharmaceutically or veterinarily acceptable salts thereof.
Claim 31
Dependent Claim
37 words
A pharmaceutical or veterinary composition suitable for the treatment of Gram-positive and Gram-negative microorganisms, said composition comprising a therapeutically effective amount of a compound according to claim 1, and a pharmaceutically or veterinarily acceptable carrier or diluent.
Claim 32
Dependent Claim
32 words
A method of treating a patient suffering from conditions caused by Gram-positive and Gram-negative microorganisms, said method comprising administering to said patient a therapeutically effective amount of a compound of claim 1.
Claim 33
Dependent Claim
14 words
A method according to claim 21, wherein said compound is administered orally or parenterally.
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) | 1982-05-14 | 1982-11-13 | 1983-05-15 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1986-05-14 | 1986-11-13 | 1987-05-15 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1990-05-14 | 1990-11-13 | 1991-05-15 | $7700.00 | Window Closed / Lapsed |