US3998950A
Expired / Lapsed
US
⏱️ 0.0 years remaining
7-αHydrazinoacetamido derivatives of cephalosporanic
Assignee: ISF SpA
•
Filing: 1975-03-28
•
Granted: 1976-12-21
•
Expires: 1995-03-28
Abstract
Abstract Derivatives of 7-aminocephalosporanic acid of the formula: ##STR1## wherein the carbon atom marked with an asterisk represents an asymmetry center of the molecule, A represents an aromatic nucleus, preferably phenyl which may be substituted by alkyl having 1-4 carbon atoms, halogen, hydroxy or alkoxy having 1-4 carbon atoms, or a heterocyclic nucleus, preferably 2- or 3-thiophene which may be, for example, substituted by halogen, R represents a hydrogen atom or a straight or branched chain lower alkyl radical, R 1 represents a hydrogen atom, a hydroxy group, an acetoxy or pyridinium group. The invention includes the compounds as such or in the form of separated epimers as well as the corresponding pharmaceutically acceptable salts with alkali or alkaline-earth metals, with suitable organic bases or corresponding suitable organic or inorganic acid addition salts. Also method of preparing same. The compounds have powerful antibacterial action against gram-positive and gram-negative bacteria.
Inventors
- 👤 Renato Broggi
- 👤 Giuseppe Libassi
- 👤 Giorgio Pifferi
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-08 14:24
CPC Classifications
C; C07; C07D; C07D501/00; C07D501/14; C07D501/16; C07D501/20; Y; Y02; Y02P; Y02P20/00; Y02P20/50; Y02P20/55
Claims Analysis
Total Claims: 37
Claim 1
Independent Claim
99 words
Hydrazinocephalosporins of the formula: ##STR5## wherein the carbon atom marked with the asterisk represents an asymmetry center of the molecule, A 1 represents a phenyl group which may be substituted by alkyl having 1-4 carbon atoms, halogen, hydroxy or alkoxy having 1-4 carbon atoms or a 2- or 3-thiophene group, which may be substituted by halogen, R represents a hydrogen atom or a straight or branched chain lower alkyl radical containing from 1 to 5 carbon atoms, R 1 represents a hydrogen atom, a hydroxy, acetoxy or pyridinium group; separated epimers thereof or the corresponding pharmaceutically acceptable salts thereof.
Claim 2
Dependent Claim
99 words
Hydrazinocephalosporins of the formula: ##STR5## wherein the carbon atom marked with the asterisk represents an asymmetry center of the molecule, A 1 represents a phenyl group which may be substituted by alkyl having 1-4 carbon atoms, halogen, hydroxy or alkoxy having 1-4 carbon atoms or a 2- or 3-thiophene group, which may be substituted by halogen, R represents a hydrogen atom or a straight or branched chain lower alkyl radical containing from 1 to 5 carbon atoms, R 1 represents a hydrogen atom, a hydroxy, acetoxy or pyridinium group; separated epimers thereof or the corresponding pharmaceutically acceptable salts thereof.
Claim 3
Dependent Claim
2 words
7-(α-Hydrazinophenylacetamido)-desacetoxycephalosporanic acid.
Claim 4
Dependent Claim
2 words
7-(α-Hydrazinophenylacetamido)-desacetoxycephalosporanic acid.
Claim 5
Dependent Claim
3 words
7-[R(-)- α-Hydrazinophenylacetamido]-desacetoxycephalosporanic acid.
Claim 6
Dependent Claim
3 words
7-[R(-)- α-Hydrazinophenylacetamido]-desacetoxycephalosporanic acid.
Claim 7
Dependent Claim
3 words
7-[S(+)- α-Hydrazinophenylacetamido]-desacetoxycephalosporanic acid.
Claim 8
Dependent Claim
3 words
7-[S(+)- α-Hydrazinophenylacetamido]-desacetoxycephalosporanic acid.
Claim 9
Dependent Claim
2 words
7-(α-Hydrazinophenylacetamido)-cephalosporanic acid.
Claim 10
Dependent Claim
2 words
7-(α-Hydrazinophenylacetamido)-cephalosporanic acid.
Claim 11
Dependent Claim
2 words
7-[R(-)-Hydrazinophenylacetamido]-cephalosporanic acid.
Claim 12
Dependent Claim
2 words
7-[R(-)-Hydrazinophenylacetamido]-cephalosporanic acid.
Claim 13
Dependent Claim
3 words
7-[S(+)- α-Hydrazinophenylacetamido]-cephalosporanic acid.
Claim 14
Dependent Claim
3 words
7-[S(+)- α-Hydrazinophenylacetamido]-cephalosporanic acid.
Claim 15
Dependent Claim
3 words
7-[α- (1-Methylhydrazino)phenylacetamido]-desacetoxycephalosporanic acid.
Claim 16
Dependent Claim
3 words
7-[α- (1-Methylhydrazino)phenylacetamido]-desacetoxycephalosporanic acid.
Claim 17
Dependent Claim
2 words
7-(α-Hydrazino-2-thienylacetamido)-desacetoxycephalosporanic acid.
Claim 18
Dependent Claim
2 words
7-(α-Hydrazino-2-thienylacetamido)-desacetoxycephalosporanic acid.
Claim 19
Dependent Claim
2 words
7-(α-Hydrazino-2-thienylacetamido)-cephalosporanic acid.
Claim 20
Dependent Claim
2 words
7-(α-Hydrazino-2-thienylacetamido)-cephalosporanic acid.
Claim 21
Dependent Claim
2 words
7-(α-Hydrazino-3-thienylacetamido)-desacetoxycephalosporanic acid.
Claim 22
Dependent Claim
2 words
7-(α-Hydrazino-3-thienylacetamido)-desacetoxycephalosporanic acid.
Claim 23
Dependent Claim
2 words
7-(α-Hydrazino-3-thienylacetamido)-cephalosporanic acid.
Claim 24
Dependent Claim
2 words
7-(α-Hydrazino-3-thienylacetamido)-cephalosporanic acid.
Claim 25
Dependent Claim
2 words
7-[α-Hydrazino-3-(2,5-dichloro)-thienylacetamido]-cephalosporanic acid.
Claim 26
Dependent Claim
2 words
7-[α-Hydrazino-3-(2,5-dichloro)-thienylacetamido]-cephalosporanic acid.
Claim 27
Dependent Claim
3 words
7 -[α-Hydrazino-3-(2,5-dichloro)thienylactamido]-desacetoxycephalosporanic acid.
Claim 28
Dependent Claim
3 words
7 -[α-Hydrazino-3-(2,5-dichloro)thienylactamido]-desacetoxycephalosporanic acid.
Claim 29
Dependent Claim
88 words
Trichloroethylesters of hydrazinocephalosporanic acid of the formula: ##STR6## wherein the carbon atom marked with the asterisk represents an asymmetry center of the molecule, A represents a phenyl group which may be substituted by alkyl having 1-4 carbon atoms, halogen, hydroxy or alkoxy having 1-4 carbon atoms or a 2- or 3-thiophene group, which may be substituted by halogen, R represents a hydrogen atom or a straight or branched chain lower alkyl radical, R 1 represents a hydrogen atom, a hydroxy, acetoxy or pyridinium group or; separated epimers thereof.
Claim 30
Dependent Claim
88 words
Trichloroethylesters of hydrazinocephalosporanic acid of the formula: ##STR6## wherein the carbon atom marked with the asterisk represents an asymmetry center of the molecule, A represents a phenyl group which may be substituted by alkyl having 1-4 carbon atoms, halogen, hydroxy or alkoxy having 1-4 carbon atoms or a 2- or 3-thiophene group, which may be substituted by halogen, R represents a hydrogen atom or a straight or branched chain lower alkyl radical, R 1 represents a hydrogen atom, a hydroxy, acetoxy or pyridinium group or; separated epimers thereof.
Claim 31
Dependent Claim
5 words
7-(α-Hydrazinophenylacetamido)-desacetoxycephalosporanic acid β, β, β-trichloroethylester.
Claim 32
Dependent Claim
5 words
7-(α-Hydrazinophenylacetamido)-desacetoxycephalosporanic acid β, β, β-trichloroethylester.
Claim 33
Dependent Claim
5 words
7-[R(-)-α-Hydrazinophenylacetamido]desacetoxycephalosporanic acid β, β, β-trichloroethylester.
Claim 34
Dependent Claim
5 words
7-[R(-)-α-Hydrazinophenylacetamido]desacetoxycephalosporanic acid β, β, β-trichloroethylester.
Claim 35
Dependent Claim
6 words
7-[S(+)- α-Hydrazinophenylacetamido]-desacetoxycephalosporanic acid β, β, β-trichloroethylester.
Claim 36
Dependent Claim
6 words
7-[S(+)- α-Hydrazinophenylacetamido]-desacetoxycephalosporanic acid β, β, β-trichloroethylester.
Claim 37
Dependent Claim
21 words
A pharmaceutical composition comprising an anti-bacterially effective amount of a compound as defined in claim 1 and a pharmaceutically acceptable carrier.
References Cited (Backward Citations)
US3518260A
Cited
US3489752A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1979-12-21 | 1980-06-21 | 1980-12-21 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1983-12-21 | 1984-06-21 | 1984-12-21 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1987-12-21 | 1988-06-21 | 1988-12-21 | $7700.00 | Window Closed / Lapsed |