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US4042586A
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2-(3-Substituted amino-2-hydroxypropoxy)-3-substituted pyrazines
Assignee: Merck Sharp & Dohme (I.A.) Corp
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Filing: 1975-06-06
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Granted: 1977-08-16
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Expires: 1995-06-06
Abstract
Abstract 2-(3-Substituted amino-2-hydroxypropoxy)-3-substituted pyrazine compounds optionally having substituents in the 5 and/or 6 positions, possessing β-adrenergic blocking properties are described. The products are prepared by reaction of a 2-chloro(or hydroxy)pyrazine with a 5-hydroxy-methyl(or sulfonyloxymethyl)oxazolidine followed by acid hydrolysis.
Inventors
- 👤 Burton Kendall Wasson
- 👤 Leonard M. Weinstock
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-09 13:48
CPC Classifications
C; C07; C07D; C07D413/00; C07D413/02; C07D413/04; C07D209/00; C07D209/02; C07D209/04; C07D209/10; C07D209/14; C07D263/00; C07D263/02; C07D263/04; C07D263/06
Claims Analysis
Total Claims: 10
Claim 1
Independent Claim
102 words
A pyrazine compound having the structure ##STR19## or a pharmacologically acceptable salt thereof wherein R represents morpholino or thiomorpholino; R 1 represents a straight or branched chain C 3-6 alkyl, a straight or branched chain hydroxy substituted C 3-6 alkyl, a straight or branched chain C 3-6 alkinyl, phenyl-C 1-6 alkyl or iodolyl-C 1-6 alkyl; R 2 and R 3 can represent the same or different substituents and represent hydrogen, C 1-3 alkyl, C 5-7 cycloalkyl, C 1-3 alkoxy, phenoxy, phenyl, substituted phenyl wherein the substituent is C 1-3 alkyl, C 1-3 alkoxy, amino, acetylamino, nitro or halo; or morpholino or thiomorpholino.
Claim 2
Dependent Claim
102 words
A pyrazine compound having the structure ##STR19## or a pharmacologically acceptable salt thereof wherein R represents morpholino or thiomorpholino; R 1 represents a straight or branched chain C 3-6 alkyl, a straight or branched chain hydroxy substituted C 3-6 alkyl, a straight or branched chain C 3-6 alkinyl, phenyl-C 1-6 alkyl or iodolyl-C 1-6 alkyl; R 2 and R 3 can represent the same or different substituents and represent hydrogen, C 1-3 alkyl, C 5-7 cycloalkyl, C 1-3 alkoxy, phenoxy, phenyl, substituted phenyl wherein the substituent is C 1-3 alkyl, C 1-3 alkoxy, amino, acetylamino, nitro or halo; or morpholino or thiomorpholino.
Claim 3
Dependent Claim
17 words
A pyrazine compound as claimed in claim 1 wherein R 2 and R 3 are each hydrogen.
Claim 4
Dependent Claim
19 words
A pyrazine compound of claim 1 wherein R 2 and R 3 are each hydrogen, and R is morpholino.
Claim 5
Dependent Claim
27 words
A pyrazine compound of claim 1 wherein R 2 and R 3 are each hydrogen and R 1 is a straight or branched chain C 3-6 alkyl.
Claim 6
Dependent Claim
13 words
A pyrazine compound as claimed in claim 4 wherein R 1 is tert-butyl.
Claim 7
Dependent Claim
10 words
A pyrazine compound of claim 1 wherein R is thiomorpholino.
Claim 8
Dependent Claim
12 words
A pyrazine compound as claimed in claim 1 wherin R is morpholino.
Claim 9
Dependent Claim
13 words
A pyrazine compound as claimed in claim 1 wherein R 2 is hydrogen.
Claim 10
Dependent Claim
13 words
A pyrazine compound as claimed in claim 1 wherein R 3 is hydrogen.
References Cited (Backward Citations)
DE2405930A1
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1980-08-15 | 1981-02-14 | 1981-08-16 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1984-08-15 | 1985-02-14 | 1985-08-16 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1988-08-15 | 1989-02-14 | 1989-08-16 | $7700.00 | Window Closed / Lapsed |