US4016267A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Sulfacytosine derivatives
Assignee: Hoffmann La Roche Inc
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Filing: 1976-06-07
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Granted: 1977-04-05
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Expires: 1996-06-07
Abstract
Abstract N1-(1,2-dihydro-2-oxo-4-pyrimidinyl)sulfanilamides, bearing a lower alkyl, cycloalkyl or cycloalkyl-lower alkyl substituent in the 1-position, prepared by reaction of the corresponding 1-substituted-1,2-dihydro-2-oxo-4-aminopyrimidine and N-acylated sulfanilyl chloride with subsequent hydrolysis, are described. The end products are useful as antibacterial agents.
Inventors
- 👤 Harry Allen Albrecht
- 👤 John Thomas Plati
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-06 02:40
CPC Classifications
C; C07; C07D; C07D239/00; C07D239/02; C07D239/24; C07D239/28; C07D239/69; C07D239/20; C07D239/22
Claims Analysis
Total Claims: 15
Claim 1
Independent Claim
40 words
An antibacterial composition comprising as the active ingredient an antibacterially effective amount of a compound of the formula ##STR7## wherein R 1 is cyclo-lower alkyl or cyclo-lower alkyl-lower alkyl; or a pharmaceutically acceptable salt thereof and an inert carrier material.
Claim 2
Dependent Claim
40 words
An antibacterial composition comprising as the active ingredient an antibacterially effective amount of a compound of the formula ##STR7## wherein R 1 is cyclo-lower alkyl or cyclo-lower alkyl-lower alkyl; or a pharmaceutically acceptable salt thereof and an inert carrier material.
Claim 3
Dependent Claim
13 words
The antibacterial composition of claim 1 wherein R 1 is cyclo-lower alkyl-lower alkyl.
Claim 4
Dependent Claim
14 words
The antibacterial composition of claim 2 wherein the active ingredient is N 1 -(1-cyclopropyl-methyl-1,2-dihydro-2-oxo-4-pyrimidinyl)-sulfanilamide.
Claim 5
Dependent Claim
14 words
The antibacterial composition of claim 1 wherein the active ingredient is N 1 -(1-cyclopentyl-1,2-dihydro-2-oxo-4-pyrimidinyl)-sulfanilamide.
Claim 6
Dependent Claim
14 words
The antibacterial composition of claim 1 wherein the active ingredient is N 1 -(1-cyclopropyl-1,2-dihydro-2-oxo-4-pyrimidinyl)-sulfanilamide.
Claim 7
Dependent Claim
14 words
The antibacterial composition of claim 1 wherein the active ingredient is N 1 -(1-cyclohexyl-1,2-dihydro-2-oxo-4-pyrimidinyl)-sulfanilamide.
Claim 8
Independent Claim
41 words
A method for combatting bacteria comprising administering to a warmblooded animal requiring such treatment an antibacterially effective amount of a compound of the formula ##STR8## wherein R 1 is cyclo-lower alkyl or cyclo-lower alkyl-lower alkyl; or a pharmaceutically acceptable salt thereof.
Claim 9
Independent Claim
41 words
A method for combatting bacteria comprising administering to a warmblooded animal requiring such treatment an antibacterially effective amount of a compound of the formula ##STR8## wherein R 1 is cyclo-lower alkyl or cyclo-lower alkyl-lower alkyl; or a pharmaceutically acceptable salt thereof.
Claim 10
Dependent Claim
108 words
An antibacterial composition comprising an antibacterially effective combination of 1 to 40 parts of a sulfanilamide of the formula ##STR9## wherein R 1 is cyclo-lower alkyl or cyclo-lower alkyl-lower alkyl; or a pharmaceutically acceptable salt thereof, and 1 part of a pyrimidine of the formula ##STR10## wherein R 3 is hydrogen or lower alkyl, R 4 is hydrogen or lower alkoxy, R 5 is amino, lower alkylamino, di-lower alkylamino or lower alkoxy, and R 6 is lower alkoxy, provided that when R 3 is lower alkyl, R 4 is hydrogen and R 5 is lower alkoxy, or pharmaceutically acceptable acid addition salt thereof and an inert carrier material.
Claim 11
Dependent Claim
108 words
An antibacterial composition comprising an antibacterially effective combination of 1 to 40 parts of a sulfanilamide of the formula ##STR9## wherein R 1 is cyclo-lower alkyl or cyclo-lower alkyl-lower alkyl; or a pharmaceutically acceptable salt thereof, and 1 part of a pyrimidine of the formula ##STR10## wherein R 3 is hydrogen or lower alkyl, R 4 is hydrogen or lower alkoxy, R 5 is amino, lower alkylamino, di-lower alkylamino or lower alkoxy, and R 6 is lower alkoxy, provided that when R 3 is lower alkyl, R 4 is hydrogen and R 5 is lower alkoxy, or pharmaceutically acceptable acid addition salt thereof and an inert carrier material.
Claim 12
Dependent Claim
18 words
The composition of claim 8 wherein the sulfanilamide is N 1 -(1-cyclohexyl-1,2-dihydro-2-oxo-4-pyrimidinyl)-sulfanilamide and wherein the pyrimidine is 2,4-diamino-5-(3,4,5-trimethoxybenzyl)-pyrimidine.
Claim 13
Dependent Claim
18 words
The composition of claim 8 wherein the sulfanilamide is N 1 -(1-cyclohexyl-1,2-dihydro-2-oxo-4-pyrimidinyl)-sulfanilamide and wherein the pyrimidine is 2,4-diamino-5-(4-amino-3,5-dimethoxybenzyl)-pyrimidine.
Claim 14
Independent Claim
117 words
A method for combatting bacteria comprising administering to a warmblooded animal requiring such treatment an antibacterially effective amount of a composition comprising 1 to 40 parts of a compound of the formula ##STR11## wherein R 1 is cyclo-lower alkyl or cyclo-lower alkyl-lower alkyl; or a pharmaceutically acceptable salt thereof, and 1 part of a compound of the formula ##STR12## wherein R 3 is hydrogen or lower alkyl; R 4 is hydrogen or lower alkoxy, R 5 is amino, lower alkylamino, di-lower alkylamino or lower alkoxy, and R 6 is lower alkoxy, provided that when R 3 is lower alkyl, R 4 is hydrogen and R 5 is lower alkoxy, or a pharmaceutically acceptable acid addition salt thereof.
Claim 15
Independent Claim
117 words
A method for combatting bacteria comprising administering to a warmblooded animal requiring such treatment an antibacterially effective amount of a composition comprising 1 to 40 parts of a compound of the formula ##STR11## wherein R 1 is cyclo-lower alkyl or cyclo-lower alkyl-lower alkyl; or a pharmaceutically acceptable salt thereof, and 1 part of a compound of the formula ##STR12## wherein R 3 is hydrogen or lower alkyl; R 4 is hydrogen or lower alkoxy, R 5 is amino, lower alkylamino, di-lower alkylamino or lower alkoxy, and R 6 is lower alkoxy, provided that when R 3 is lower alkyl, R 4 is hydrogen and R 5 is lower alkoxy, or a pharmaceutically acceptable acid addition 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) | 1980-04-04 | 1980-10-04 | 1981-04-05 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1984-04-04 | 1984-10-04 | 1985-04-05 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1988-04-04 | 1988-10-04 | 1989-04-05 | $7700.00 | Window Closed / Lapsed |