US4235905A
Expired / Lapsed
US
⏱️ 0.0 years remaining
1H-Pyrimido[4,5-c]-1,2-diazepines
Assignee: SmithKline Beecham Corp
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Filing: 1979-09-17
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Granted: 1980-11-25
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Expires: 1999-09-17
Abstract
Abstract Compounds of the general formula (I) ##STR1## wherein R 1 and R 2 are selected from a lower alkyl group, a phenyl group (optionally substituted by one or more hydroxy or lower alkoxy groups), a pyridyl group or a group --CO 2 R where R is a lower alkyl group, (provided that when R 1 is a group --CO 2 R, R 2 is a lower alkyl group) are disclosed. The compounds of formula (I) are useful as intermediates to compounds of other ring systems which are of pharmacological interest. Certain of the compounds of formula (I) are also useful as antimicrobial agents.
Inventors
- 👤 Robert W. Morrison, Jr.
- 👤 William R. Mallory
- 👤 Virgil L. Styles
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-04 16:08
CPC Classifications
C; C07; C07D; C07D239/00; C07D239/02; C07D239/24; C07D239/28; C07D239/46; C07D239/48; A; A61; A61P; A61P31/00; A61P31/04; A61P33/00; A61P33/02; C07D471/00; C07D471/02; C07D471/04; C07D487/00; C07D487/02; C07D487/04
Claims Analysis
Total Claims: 25
Claim 1
Independent Claim
68 words
A compound of formula (I) or a tautomer or a pharmaceutically acceptable salt thereof ##STR32## wherein R 1 and R 2 are the same or different and are selected from lower alkyl, phenyl, phenyl substituted by one or more hydroxy or lower alkoxy, pyridyl or --CO 2 R in which R is lower alkyl; provided that when R 1 is --CO 2 R, R 2 is lower alkyl.
Claim 2
Dependent Claim
68 words
A compound of formula (I) or a tautomer or a pharmaceutically acceptable salt thereof ##STR32## wherein R 1 and R 2 are the same or different and are selected from lower alkyl, phenyl, phenyl substituted by one or more hydroxy or lower alkoxy, pyridyl or --CO 2 R in which R is lower alkyl; provided that when R 1 is --CO 2 R, R 2 is lower alkyl.
Claim 3
Dependent Claim
25 words
A compound according to claim 1 wherein R 1 is phenyl optionally substituted by one or more hydroxy and R 2 is --CO 2 R.
Claim 4
Dependent Claim
30 words
A compound according to claim 1 wherein R 1 is phenyl optionally substituted by one or more lower alkoxy and R 2 is selected from phenyl and --CO 2 R.
Claim 5
Dependent Claim
14 words
The compound of claim 1 in which R 1 and R 2 are phenyl.
Claim 6
Dependent Claim
14 words
The compound of claim 1 in which R 1 and R 2 are methyl.
Claim 7
Dependent Claim
24 words
The compound of claim 1 in which R 1 is C 6 H 4 OH and R 2 is CO 2 CH 3 .
Claim 8
Dependent Claim
20 words
The compound of claim 1 in which R 1 is 3-pyridyl and R 2 is CO 2 CH 3 .
Claim 9
Dependent Claim
25 words
The compound of claim 1 in which R 1 is C 6 H 5 and R 2 is CO 2 C 2 H 5 .
Claim 10
Dependent Claim
20 words
The compound of claim 1 in which R 1 is 3,4,5-trimethoxyphenyl and R 2 is CO 2 CH 3 .
Claim 11
Dependent Claim
22 words
The compound of claim 1 in which R 1 is 2,4-dimethoxyphenyl and R 2 is CO 2 C 2 H 5 .
Claim 12
Dependent Claim
21 words
The compound of claim 1 in which R 1 is CH 3 and R 2 is CO 2 C 2 H5.
Claim 13
Dependent Claim
23 words
The compound of claim 1 in which R 1 is CO 2 C 2 H 5 and R 2 is CH 3 .
Claim 14
Dependent Claim
44 words
A method of preparing a compound of formula (I) as defined in claim 1 which comprises the reaction of a compound of formula (IV): ##STR33## with a compound of formula (V): ##STR34## wherein R 1 and R 2 are as defined in claim 1.
Claim 15
Dependent Claim
34 words
A formulation for use as an anti-microbial agent comprising an effective antimicrobial amount of a compound of formula (I) as defined in either claim 2 or claim 3 together with an acceptable carrier therefor.
Claim 16
Dependent Claim
10 words
A formulation according to claim 5 in unit dosage form.
Claim 17
Dependent Claim
14 words
The formulation of claim 14 in which R 1 and R 2 are phenyl.
Claim 18
Dependent Claim
24 words
The formulation of claim 14 in which R 1 is C 6 H 4 OH and R 2 is CO 2 CH 3 .
Claim 19
Dependent Claim
25 words
The formulation of claim 5 in which R 1 is C 6 H 5 and R 2 is CO 2 C 2 H 5 .
Claim 20
Dependent Claim
20 words
The formulation of claim 14 in which R 1 is 3,4,5-trimethoxyphenyl and R 2 is CO 2 CH 3 .
Claim 21
Dependent Claim
23 words
The formulation of claim 14 in which R 1 is CH 3 and R 2 is CO 2 C 2 H 5 .
Claim 22
Dependent Claim
23 words
The formulation of claim 14 in which R 1 is CO 2 C 2 H 5 and R 2 is CH 3 .
Claim 23
Dependent Claim
22 words
The formulation of claim 14 in which R 1 is 2,4-dimethoxyphenyl and R 2 is CO 2 C 2 H 5 .
Claim 24
Dependent Claim
30 words
The formulation of claim 14 in which R 1 is phenyl optionally substituted by one or more lower alkoxy and R 2 is selected from phenyl and --CO 2 R.
Claim 25
Dependent Claim
25 words
The formulation of claim 14 in which R 1 is phenyl optionally substituted by one or more hydroxy and R 2 is --CO 2 R.
References Cited (Backward Citations)
US3947442A
Cited
EP0000383A1
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1983-11-25 | 1984-05-26 | 1984-11-25 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1987-11-25 | 1988-05-26 | 1988-11-25 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1991-11-25 | 1992-05-26 | 1992-11-25 | $7700.00 | Window Closed / Lapsed |