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US4792557A
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2,4-diamino-5[4-amino (or dimethylamino)-3,5-dimethoxybenzyl]pyrimidine and antibacterial composition thereof
Assignee: Hoffmann La Roche Inc
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Filing: 1987-01-14
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Granted: 1988-12-20
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Expires: 2007-01-14
Abstract
Abstract 2,4-Diamino-5-benzylpyrimidines of the formula ##STR1## wherein R 1 , R 2 , A, Z and n are as hereinafter set forth, are described. The 2,4-diamino-5-benzylpyrimidines of the invention have useful antibacterial activity. More particularly, they inhibit bacterial dihydrofolate reductase and potentiate the antibacterial activity of sulfonamides.
Inventors
- 👤 Ivan Kompis
- 👤 G/e/ rald Rey-Bellet
- 👤 Guido Zanetti
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-01 16:58
CPC Classifications
C; C07; C07D; C07D207/00; C07D207/02; C07D207/30; C07D207/32; C07D207/325; C07C; C07C255/00; C07D207/327; C07D239/00; C07D239/02; C07D239/24; C07D239/28; C07D239/46; C07D239/48; C07D239/49; C07D295/00; C07D295/04; C07D295/14; C07D295/155
Claims Analysis
Total Claims: 13
Claim 1
Independent Claim
18 words
An antibacterial composition comprising 2,4-diamino-5-(4-amino-3,5-dimethoxybenzyl)pyrimidine or a pharmaceutically acceptable acid addition salt thereof and a compatible pharmaceutical carrier.
Claim 2
Dependent Claim
18 words
An antibacterial composition comprising 2,4-diamino-5-(4-amino-3,5-dimethoxybenzyl)pyrimidine or a pharmaceutically acceptable acid addition salt thereof and a compatible pharmaceutical carrier.
Claim 3
Dependent Claim
14 words
A composition according to claim 1, wherein the compound of formula I is 2,4-(diamino-5-(4-amino-3,5-dimethoxybenzyl)pyrimidine.
Claim 4
Dependent Claim
15 words
A composition according to claim 1 wherein the compound of formula I is 2,4-diamino-5-(4-amino-3,5-dimethoxybenzyl)pyrimidine monohydrochloride.
Claim 5
Dependent Claim
15 words
A composition according to claim 1 wherein the compound of formula I is 2,4-diamino-5-(4-amino-3,5-dimethoxybenzyl)pyrimidine dihydrochloride.
Claim 6
Dependent Claim
19 words
An antibacterial composition comprising 2,4-diamino-5-[4-(dimethylamino)-3,5-dimethoxybenzyl]pyrimidine, or a pharmaceutically acceptable acid addition salt thereof, and a pharmaceutically compatible carrier material.
Claim 7
Dependent Claim
19 words
An antibacterial composition comprising 2,4-diamino-5-[4-(dimethylamino)-3,5-dimethoxybenzyl]pyrimidine, or a pharmaceutically acceptable acid addition salt thereof, and a pharmaceutically compatible carrier material.
Claim 8
Dependent Claim
11 words
A composition according to claim 1, which further comprises a sulfonamide.
Claim 9
Dependent Claim
29 words
A composition according to claim 6, wherein the weight ratio of 2,4-diamino-5-(4-amino-3,5-dimethoxybenzyl)pyrimidine or a pharmaceutically acceptable acid addition salt thereof and the sulfonamide is about 1:40 to about 5:1.
Claim 10
Dependent Claim
30 words
A composition according to claim 7, wherein the weight ratio of the 2,4-diamino-5-(4-amino-3,5-dimethoxybenzyl)pyrimidine or a pharmaceutically acceptable acid addition salt thereof and the sulfonamide is about 1:1 to about 1:5.
Claim 11
Dependent Claim
11 words
A composition according to claim 5, which further comprises a sulfonamide.
Claim 12
Dependent Claim
29 words
A composition according to claim 9, wherein the weight ratio of 2,4-diamino-5-[4-(dimethylamino)-3,5-dimethoxybenzyl]pyrimidine or a pharmaceutically acceptable acid addition salt thereof and the sulfonamide is about 1:40 to about 5:1.
Claim 13
Dependent Claim
29 words
A composition according to claim 10, wherein the weight ratio of 2,4-diamino-5-[4-(dimethylamino)-3,5-dimethoxybenzyl]pyrimidine or a pharmaceutically acceptable acid addition salt thereof and the sulfonamide is about 1:1 to about 1:5.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1991-12-20 | 1992-06-20 | 1992-12-20 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1995-12-20 | 1996-06-20 | 1996-12-20 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1999-12-20 | 2000-06-20 | 2000-12-20 | $7700.00 | Window Closed / Lapsed |