Patent US3954802A successfully refreshed from Google Patents.
US3954802A
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Substituted-ureido derivatives of penam 3-carboxylic acid and cephem 4-carboxylic acid
Assignee: Novartis Corp
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Filing: 1973-03-22
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Granted: 1976-05-04
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Expires: 1993-03-22
Abstract
Abstract 6-Acylamino-penam-3-carboxylic acids and 7-acylamino-3-cephem-4-carboxylic acids in which the acyl group has the formula ##EQU1## in which R 1 is hydrogen, R 2 is optionally substituted phenyl, thienyl or furyl, or R 1 and R 2 together are optionally substituted cycloalkyl, and B is a radical which is bonded via a sulphur atom or is bonded to oxygen or sulphur with the interposition of an optionally substituted CH 2 -group.
Inventors
- 👤 Karoly Kocsis
- 👤 Bruno Fechtig
- 👤 Hans Bickel
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-01 10:54
CPC Classifications
C; C07; C07C; C07C265/00; C07C265/16; C07D; C07D307/00; C07D307/02; C07D307/34; C07D307/38; C07D307/52; C07D307/56; C07D307/68; C07D333/00; C07D333/02; C07D333/04; C07D333/26; C07D333/38; C07D499/00
Claims Analysis
Total Claims: 13
Claim 1
Independent Claim
146 words
A compound of the formula ##EQU14## wherein R 3 denotes a free carboxyl group and, if R 1 and R 2 are separate, R 1 is hydrogen and R 2 is phenyl, thienyl or furyl, and, if R 1 and R 2 are combined, they form together with the carbon atom, cycloalkyl of 4 to 7 carbon atoms, and wherein B denotes a radical of the formula ##EQU15## wherein x represents carbonyloxy or sulphonyl, R 5 represents hydrogen, lower alkyl, phenyl, thienyl, furyl or pyridyl and R 6 represents (a) lower alkyl or lower alkyl mono substituted by halogen, lower alkoxy, phenoxy or lower alkanoloxy or (b) phenyl, naphthyl, benzyl, furyl, thienyl, furfuryl, thenyl, pyridyl, pyrazinyl or pyrimidyl or phenyl, naphthyl, benzyl, furyl, thienyl, furfuryl, thenyl, pyridyl, pyrazinyl or pyrimidyl mono substituted by lower alkyl, lower alkoxy, halogen or nitro, or a pharmaceutically acceptable salt thereof.
Claim 2
Dependent Claim
146 words
A compound of the formula ##EQU14## wherein R 3 denotes a free carboxyl group and, if R 1 and R 2 are separate, R 1 is hydrogen and R 2 is phenyl, thienyl or furyl, and, if R 1 and R 2 are combined, they form together with the carbon atom, cycloalkyl of 4 to 7 carbon atoms, and wherein B denotes a radical of the formula ##EQU15## wherein x represents carbonyloxy or sulphonyl, R 5 represents hydrogen, lower alkyl, phenyl, thienyl, furyl or pyridyl and R 6 represents (a) lower alkyl or lower alkyl mono substituted by halogen, lower alkoxy, phenoxy or lower alkanoloxy or (b) phenyl, naphthyl, benzyl, furyl, thienyl, furfuryl, thenyl, pyridyl, pyrazinyl or pyrimidyl or phenyl, naphthyl, benzyl, furyl, thienyl, furfuryl, thenyl, pyridyl, pyrazinyl or pyrimidyl mono substituted by lower alkyl, lower alkoxy, halogen or nitro, or a pharmaceutically acceptable salt thereof.
Claim 3
Dependent Claim
97 words
A compound according to claim 1 wherein R 3 denotes a free carboxyl group, R 1 represents hydrogen and R 2 represents phenyl and B represents ##EQU16## and wherein R 5 ' represents hydrogen, lower alkyl, phenyl, thienyl, furyl or pyridyl and R 6 ' represents (a) lower alkyl or lower alkyl mono substituted by halogen, lower alkoxy, phenoxy or lower alkanoloxy or (b) phenyl, naphthyl, benzyl, furyl, thienyl, furfuryl, thenyl, pyridyl, pyrazinyl or pyrimidyl or phenyl, naphthyl, benzyl, furyl, thienyl, furfuryl, thenyl, pyridyl, pyrazinyl or pyrimidyl mono substituted by lower alkyl, lower alkoxy, halogen or nitro.
Claim 4
Dependent Claim
33 words
A compound according to claim 1 wherein R 3 denotes a free carboxyl group, R 1 represents hydrogen and R 2 represents phenyl and B denotes lower alkanoyloxymethyl, α-lower alkanoyloxyethyl or α-lower alkanoyloxybenzyl.
Claim 5
Dependent Claim
29 words
A compound according to claim 1 wherein R 3 denotes a free carboxyl group, R1 represents hydrogen and R 2 represents phenyl and B denotes phenyl sulphonylmethyl or naphthylsulphonylmethyl.
Claim 6
Dependent Claim
19 words
A compound as claimed in claim 1, which is 6-[D-α-(3-α-(2-thenoyloxy)- propionyl-1-ureido)- phenyl-acetamido]-penicillanic acid or a pharmaceutically acceptable salt thereof.
Claim 7
Dependent Claim
27 words
A compound as claimed in claim 1, which 6-[D-α-(3-p-chlorophenylsulphonylacetyl-1-ureido)-phenylacetamido]-penicillanic acid or a pharmaceutically acceptable alkali metal, alkaline earth metal, earth metal, ammonium or amine addition salt thereof.
Claim 8
Dependent Claim
17 words
A compound as claimed in claim 1 which is 6-[D(-)-α-(3-L(+)-α-(2-furoyloxy)-propionyl-1-ureido)-phenylacetamido]-penicillanic acid or a pharmaceutically acceptable salt thereof.
Claim 9
Dependent Claim
17 words
A compound as claimed in claim 1, which is 6-[D(-)-α-(3-D,L-α-acetoxy-(2-furylacetyl)-1-ureido-phenylacetamido]-penicillanic acid or a pharmaceutically acceptable salt thereof.
Claim 10
Dependent Claim
17 words
A compound as claimed in claim 1, which is 6-[D(-)-α-(3-D,L-α-acetoxy-(2-thienylacetyl)-1-ureido)-phenylacetamido]-penicillanic acid or a pharmaceutically acceptable salt thereof.
Claim 11
Dependent Claim
17 words
A compound as claimed in claim 1, which is 6-[D(-)-α-(3-L(+)-α-(p-nitrobenzoyloxy)-propionyl-1-ureido)-phenylacetamido]-penicillanic acid or a pharmaceutically acceptable salt thereof.
Claim 12
Dependent Claim
17 words
A compound as claimed in claim 1, which is 6-[D(-)-α-(3-L(+)-α-chloroacetoxy-propionyl-1-ureido)-phenylacetamido]-penicillanic acid or a pharmaceutically acceptable salt thereof.
Claim 13
Dependent Claim
16 words
A compound as claimed in claim 1, which is 6-[D(-)-α-(3-L(+)-α-phenoxyacetoxy-propionyl-1-ureido)-phenylacetamido]-penicillanic acid or 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) | 1979-05-04 | 1979-11-03 | 1980-05-04 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1983-05-04 | 1983-11-03 | 1984-05-04 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1987-05-04 | 1987-11-03 | 1988-05-04 | $7700.00 | Window Closed / Lapsed |