US4246406A
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Heterocyclic substituted pyrazinoylguanidines
Assignee: Merck and Co Inc
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Filing: 1979-03-27
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Granted: 1981-01-20
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Expires: 1999-03-27
Abstract
Abstract The case involves novel heterocyclic substituted pyrazinoylguanidines and a process for preparing same. The heterocyclic pyrazinoylguanidines are eukalemic agents possessing diuretic and natriuretic properties.
Inventors
- 👤 Edward J. Cragoe, Jr.
- 👤 Otto W. WOLTERSDORF, Jr.
- 👤 Susan J. deSolms
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-30 19:29
CPC Classifications
C; C07; C07D; C07D241/00; C07D241/02; C07D241/10; C07D241/14; C07D241/24; C07D241/26; A; A61; A61P; A61P7/00; A61P7/10
Claims Analysis
Total Claims: 10
Claim 1
Independent Claim
91 words
A compound of the formula: ##STR6## wherein R 1 is hydrogen, lower alkyl having from 1 to 5 carbon atoms; R 2 is hydrogen, lower alkyl having 1 to 5 carbon atoms; R 3 is a 5 or 6 membered heterocyclic ring containing from 1 to 3 heterocyclic atoms selected from the elements N, O or S, said ring containing from 0 to 2 substituents selected from lower alkyl having 1 to 5 carbon atoms, halo, oxy or hydroxy; X is halo, and the pharmaceutically acceptable non-toxic acid addition salts thereof.
Claim 2
Dependent Claim
91 words
A compound of the formula: ##STR6## wherein R 1 is hydrogen, lower alkyl having from 1 to 5 carbon atoms; R 2 is hydrogen, lower alkyl having 1 to 5 carbon atoms; R 3 is a 5 or 6 membered heterocyclic ring containing from 1 to 3 heterocyclic atoms selected from the elements N, O or S, said ring containing from 0 to 2 substituents selected from lower alkyl having 1 to 5 carbon atoms, halo, oxy or hydroxy; X is halo, and the pharmaceutically acceptable non-toxic acid addition salts thereof.
Claim 3
Dependent Claim
81 words
A compound of the formula: ##STR7## wherein R 1 is hydrogen; R 2 is hydrogen or lower alkyl having from 1 to 3 carbon atoms; R 3 is a 5 or 6 membered heterocyclic ring containing from 1 to 3 heterocyclic atoms selected from the elements N, O or S, said ring containing from 0 to 2 substituents selected from lower alkyl having 1 to 5 carbon atoms, halo, oxy or hydroxy and the pharmaceutically acceptable non-toxic acid addition salts thereof.
Claim 4
Dependent Claim
81 words
A compound of the formula: ##STR7## wherein R 1 is hydrogen; R 2 is hydrogen or lower alkyl having from 1 to 3 carbon atoms; R 3 is a 5 or 6 membered heterocyclic ring containing from 1 to 3 heterocyclic atoms selected from the elements N, O or S, said ring containing from 0 to 2 substituents selected from lower alkyl having 1 to 5 carbon atoms, halo, oxy or hydroxy and the pharmaceutically acceptable non-toxic acid addition salts thereof.
Claim 5
Dependent Claim
10 words
A compound of claim 1 wherein R 3 is ##STR8##
Claim 6
Dependent Claim
21 words
A compound of claim 2 wherein R 1 is hydrogen; R 2 is hydrogen; R 3 is ##STR9## to yield 3,5-diamino-6-chloro-N-[(2-thiazolinylamino)aminomethylene]-2-pyrazinecarboxamide.
Claim 7
Dependent Claim
21 words
A compound of claim 2 wherein R 1 is hydrogen; R 2 is isopropyl; R 3 is ##STR10## to yield 3-amino-6-chloro-5-isopropylamino-N-[(2-thiazolinylamino)aminomethylene]-2-pyrazinecarboxamide.
Claim 8
Dependent Claim
21 words
A compound of claim 2 wherein R 1 is hydrogen; R 2 is hydrogen; R 3 is ##STR11## to yield 3,5-diamino-6-chloro-N-[(2-oxazolinylamino)aminomethylene]-2-pyrazinecarboxamide.
Claim 9
Dependent Claim
21 words
A compound of claim 2 wherein R 1 is hydrogen; R 2 is hydrogen; R 3 is ##STR12## to yield 3,5-diamino-N-[(2-thiazolylamino)aminomethylene]-6-chloro-2-pyrazinecarboxamide.
Claim 10
Dependent Claim
23 words
A compound of claim 2 wherein R 1 is hydrogen; R 2 is hydrogen; R 3 is ##STR13## to yield 3,5-diamino-6-chloro-N-{[2-(4,5-dihydro)thiazinylamino]aminomethylene}-2-pyrazinecarboxamide hydrochloride hemihydrate.
References Cited (Backward Citations)
US3328404A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1984-01-20 | 1984-07-21 | 1985-01-20 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1988-01-20 | 1988-07-21 | 1989-01-20 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1992-01-20 | 1992-07-21 | 1993-01-20 | $7700.00 | Window Closed / Lapsed |