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US4124762A
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7-[(Pyridylthiomethyl)phenyl]acetamido-cephalosporin derivatives
Assignee: Yeda Research and Development Co Ltd
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Filing: 1977-11-07
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Granted: 1978-11-07
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Expires: 1997-11-07
Abstract
Abstract Novel pyridylthiomethyl substituted cephalosporin compounds having the formula ##STR1## wherein R is 2-pyridyl, 3-pyridyl or 4-pyridyl.
Inventors
- 👤 Fortuna Haviv
- 👤 Abraham Patchornik
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-05 15:20
CPC Classifications
C; C07; C07D; C07D501/00; C07D501/14; C07D501/16; C07D501/20
Claims Analysis
Total Claims: 7
Claim 1
Independent Claim
302 words
A compound of the formula ##STR11## wherein R is 2-pyridyl, 3-pyridyl or 4-pyridyl; Y is hydrogen, chlorine, bromine, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, or an alkoxy group of from 1 to 4 carbon atoms; Z is a bond, oxygen or sulfur; W is hydrogen, methyl, amino, hydroxy, SO 3 H, or COOR 4 wherein R 4 is hydrogen or 5-indanyl with the proviso that when Z is oxygen or sulfur, W is other than hydroxy; R 1 is hydrogen or methoxy; R 2 is hydrogen or acetoxy; R 3 is hydrogen, a cation of an alkali metal or an alkaline earth metal, ammonium, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, a straight or branched alkanoyloxymethyl group in which the alkanoyl moiety has from 2 to 5 carbon atoms and is straight or branched, an alkanoylaminomethyl group in which the alkanoyl moiety is straight or branched and has from 2 to 5 carbon atoms and the amine nitrogen may be substituted with a straight or branched lower alkyl group having 1 to 4 carbon atoms; an alkoxycarbonylaminomethyl group in which the alkoxy moiety is straight or branched and has from 1 to 4 carbon atoms and the amine nitrogen may be substituted with a straight or branched lower alkyl group of from 1 to 4 carbon atoms, a p-(alkanoyloxy)benzyl group in which the alkanoyl moiety is straight or branched and has from 2 to 5 carbon atoms; an aminoalkanoyloxy methyl group in which the alkanoyl moiety has from 2 to 15 carbon atoms and the amino nitrogen may be mono- or di- substituted with a straight or branched lower alkyl group having from 1 to 4 carbon atoms; and pharmaceutically acceptable salts and individual optical isomers thereof.
Claim 2
Dependent Claim
302 words
A compound of the formula ##STR11## wherein R is 2-pyridyl, 3-pyridyl or 4-pyridyl; Y is hydrogen, chlorine, bromine, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, or an alkoxy group of from 1 to 4 carbon atoms; Z is a bond, oxygen or sulfur; W is hydrogen, methyl, amino, hydroxy, SO 3 H, or COOR 4 wherein R 4 is hydrogen or 5-indanyl with the proviso that when Z is oxygen or sulfur, W is other than hydroxy; R 1 is hydrogen or methoxy; R 2 is hydrogen or acetoxy; R 3 is hydrogen, a cation of an alkali metal or an alkaline earth metal, ammonium, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, a straight or branched alkanoyloxymethyl group in which the alkanoyl moiety has from 2 to 5 carbon atoms and is straight or branched, an alkanoylaminomethyl group in which the alkanoyl moiety is straight or branched and has from 2 to 5 carbon atoms and the amine nitrogen may be substituted with a straight or branched lower alkyl group having 1 to 4 carbon atoms; an alkoxycarbonylaminomethyl group in which the alkoxy moiety is straight or branched and has from 1 to 4 carbon atoms and the amine nitrogen may be substituted with a straight or branched lower alkyl group of from 1 to 4 carbon atoms, a p-(alkanoyloxy)benzyl group in which the alkanoyl moiety is straight or branched and has from 2 to 5 carbon atoms; an aminoalkanoyloxy methyl group in which the alkanoyl moiety has from 2 to 15 carbon atoms and the amino nitrogen may be mono- or di- substituted with a straight or branched lower alkyl group having from 1 to 4 carbon atoms; and pharmaceutically acceptable salts and individual optical isomers thereof.
Claim 3
Dependent Claim
17 words
A compound of claim 1 wherein W is hydrogen, amino, hydroxy, CO 2 H, SO 3 H.
Claim 4
Dependent Claim
10 words
A compound of claim 2 wherein Z is a bond.
Claim 5
Dependent Claim
9 words
A compound of claim 3 wherein Y is hydrogen.
Claim 6
Dependent Claim
15 words
A compound of claim 4 which is 3-[(acetyloxy)methyl]-8-oxo-7-[[[4-[(4-pyridinylthio)methyl]phenyl]acetyl]amino]-5-thia-1-azabicyclo[4.2.0.]oct-2-ene-2-carboxylic acid or a pharmaceutically acceptable salt thereof.
Claim 7
Dependent Claim
15 words
A compound of claim 4 which is 3-[(acetyloxy)methyl]-8-oxo-7-[[[4-[(2-pyridinylthio)methyl]phenyl]acetyl]amino]-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid or a pharmaceutically acceptable salt thereof.
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) | 1981-11-06 | 1982-05-08 | 1982-11-07 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1985-11-06 | 1986-05-08 | 1986-11-07 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1989-11-06 | 1990-05-08 | 1990-11-07 | $7700.00 | Window Closed / Lapsed |