US4086340A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Cephalosporins and their production
Assignee: Bayer AG
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Filing: 1976-05-12
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Granted: 1978-04-25
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Expires: 1996-05-12
Abstract
Abstract Cephalosporins of the formula <IMAGE> their pharmaceutically-acceptable, nontoxic salts, and hydrates thereof are produced, wherein A is hydrogen; unsubstituted or substituted alkyl; aryl; or R1-X-, wherein X is -CO- or -SO2-, and R1 is hydrogen, unsubstituted or substituted alkyl; aryl; thienyl; furyl; amino; alkylamino; dialkylamino; pyrrolidyl; or piperidyl; OR WHEN X is -CO-, R1 can also be alkoxy; B is phenyl, methylphenyl, chlorophenyl, hydroxyphenyl or the moiety <IMAGE> E is hydrogen, hydroxyl or acetoxy; and C is a center of chirality.
Inventors
- 👤 Wilfried Schrock
- 👤 Hans-Bodo Konig
- 👤 Michael Preiss
- 👤 Karl Georg Metzger
- 👤 Michael Walkowiak
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-10 02:28
CPC Classifications
C; C07; C07D; C07D501/00; C07D501/14; C07D501/16; C07D501/20
Claims Analysis
Total Claims: 21
Claim 1
Independent Claim
92 words
A compound selected from the group consisting of a cephalosporin derivative of the formula: ##STR87## the nontoxic salts thereof and the hydrates thereof wherein the carbon atom designated * constitutes a center of chirality; E is hydrogen; hydroxy; or acetoxy; B is phenyl; methylphenyl; chlorophenyl; hydroxyphenyl; or cyclohexa-1,4-dien-1-yl; and A is phenyl or naphthyl unsubstituted or substituted by one to five substituents selected from the group consisting of halo, cyano, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, and alkylsulfamyl of 1 to 4 carbon atoms.
Claim 2
Dependent Claim
92 words
A compound selected from the group consisting of a cephalosporin derivative of the formula: ##STR87## the nontoxic salts thereof and the hydrates thereof wherein the carbon atom designated * constitutes a center of chirality; E is hydrogen; hydroxy; or acetoxy; B is phenyl; methylphenyl; chlorophenyl; hydroxyphenyl; or cyclohexa-1,4-dien-1-yl; and A is phenyl or naphthyl unsubstituted or substituted by one to five substituents selected from the group consisting of halo, cyano, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, and alkylsulfamyl of 1 to 4 carbon atoms.
Claim 3
Dependent Claim
34 words
A compound according to claim 1 wherein A is phenyl, unsubstituted or substituted by chloro, bromo, fluoro, cyano, methyl, ethyl, methoxy, ethoxy, methylsulfamyl or ethylsulfamyl; and B is phenyl; 4-methylphenyl; 4-chlorophenyl; 4hydroxyphenyl; or cyclohexa-1,4-dien-1-yl.
Claim 4
Dependent Claim
12 words
A compound according to claim 2 wherein E is hydrogen or acetoxy.
Claim 5
Dependent Claim
17 words
A compound according to claim 3 wherein the configuration relative to carbon atom designated * is R.
Claim 6
Dependent Claim
17 words
A compound according to claim 2 wherein the configuration relative to carbon atom designated * is R.
Claim 7
Dependent Claim
51 words
A compound according to claim 1 which is a salt selected from the group consisting of the sodium, potassium, magnesium, calcium, aluminum, ammonium, mono-, di- or tri-alkylamines of 1 to 4 carbon atoms in the alkyl moiety, procaine, dibenzylamine, N,N'-dibenzylethylenediamine, N benzyl-β-phenylethylamine, N-methylmorpholine, N-ethylmorpholine, 1-ephenamine, dehydrobietylamine, N,N'-bis-dehydroabiethylethylenediamine, or N-lower alkylpiperidine salt.
Claim 8
Dependent Claim
13 words
A compound according to claim 1 which is the sodium or potassium salt.
Claim 9
Dependent Claim
16 words
The compound according to claim 1 which is 7-{D-α -[(2-oxo-3-phenyl-imidazolidin-1-yl)-carbonylamino]-phenylacetamido}-3-methyl-ceph-3-em-4-carboxylic acid, or the sodium salt thereof.
Claim 10
Dependent Claim
10 words
The compound according to claim 1 which is sodium 7-{D-α-[(2-oxo-3-m-chlorophenyl-imidazolidin-1-yl)-carbonylamino]-phenylacetamido}-3-acetoxymethyl-ceph-3-em-4-carboxylate.
Claim 11
Dependent Claim
10 words
The compound according to claim 1 which is sodium 7-{D-α-[(2-oxo-3-m-cyanophenyl-imidazolidin-1-yl)-carbonylamino]-phenylacetamido}-3-acetoxymethyl-ceph-3-em-4-carboxylate.
Claim 12
Dependent Claim
10 words
The compound according to claim 1 which is sodium 7-{D-α-[(2-oxo-3-p-methoxyphenyl-imidazolidin-1-yl)-carbonylamino]-phenylacetamido}-3-acetoxymethoxy-ceph-3-em-4-carboxylate.
Claim 13
Dependent Claim
10 words
The compound according to claim 1 which is sodium 7-{D-α-[(2-oxo-3-o-methoxyphenyl-imidazolidin-1-yl)-carbonylamino]-phenylacetamido}-3acetoxy-methyl-ceph-3-em-4-carboxylate.
Claim 14
Dependent Claim
10 words
The compound according to claim 1 which is sodium 7-{D-α-[(2-oxo-3-p-methylaminosulfonylphenyl-imidazolidin-1-yl)-carbonylamino]-phenylacetamido}-3-acetoxymethyl-ceph-3-em-4-carboxylate.
Claim 15
Dependent Claim
34 words
A pharmaceutical composition useful for treating bacterial infections in humans and animals which comprises an antibacterially-effective amount of a compound of claim 1 in combination with a pharmaceutically acceptable nontoxic, inert diluent or carrier.
Claim 16
Dependent Claim
27 words
A method of treating bacterial infections in humans and animals which comprises administering to such human or animal an antibacterially-effective amount of a compound of claim 1.
Claim 17
Dependent Claim
55 words
A pharmaceutical composition useful for treating bacterial infections in humans and animals which comprises an antibacterially-effective amount of a compound of claim 1 in combination with an antibacterially-effective amount of a compound selected from the group consisting of Gentamicin, Sisomicin, Kanamicin, Amikacin and Tobramicin, in combination with a pharmaceutically acceptable nontoxic, inert diluent or carrier.
Claim 18
Dependent Claim
43 words
A method of treating bacterial infections in humans and animals which comprises administering an antibacterially-effective amount of a compound of claim 1 in combination with an antibacterially-effective amount of a compound selected from the group consisting of Gentamicin, Sisomicin, Kanamicin, Amikacin and Tobramicin.
Claim 19
Dependent Claim
19 words
An animal feedstuff which comprises an antibacterially-effective amount of a compound of claim 1 in combination with nutritious material.
Claim 20
Dependent Claim
20 words
A growth-promoting composition which comprise an antibacterially-effective amount of a compound of claim 1 in combination with an edible material.
Claim 21
Dependent Claim
28 words
A method of promoting growth in animals which comprises administering to said animal a growth-promoting amount of a compound of claim 1 in combination with an edible material.
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) | 1981-04-24 | 1981-10-24 | 1982-04-25 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1985-04-24 | 1985-10-24 | 1986-04-25 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1989-04-24 | 1989-10-24 | 1990-04-25 | $7700.00 | Window Closed / Lapsed |