← Back to Patent Explorer
US4042586A Expired / Lapsed US ⏱️ 0.0 years remaining

2-(3-Substituted amino-2-hydroxypropoxy)-3-substituted pyrazines

Assignee: Merck Sharp & Dohme (I.A.) Corp
•
Filing: 1975-06-06
•
Granted: 1977-08-16
•
Expires: 1995-06-06
📄 Original PDF 🌐 Google Patents 🔄 Sync Now

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 13:20
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

Assigned Categories & Tags

No categories assigned to this patent yet.

Assign Category Tag