US5087631A
Expired / Lapsed
US
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Oxathi(SIV)azol-5-one compounds
Assignee: GlaxoSmithKline LLC
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Filing: 1990-12-18
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Granted: 1992-02-11
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Expires: 2010-12-18
Abstract
Abstract The present invention relates to the compounds of formula (I). ##STR1## wherein R 1 is C 1-8 alkyl, C 2-8 alkenyl, C 5-8 cycloalkyl, aryl-C 1-4 alkyl, aryl or heteroaryl; or aryl or heteroaryl which is mono-, di-, or trisubstituted independently with halogen, nitro, C 1-4 alkyl, C 1-4 alkoxy, trifluoromethyl, amino or C 1-4 alkyl mono or disubstituted amino, pharmaceutical formulations containing these compounds and their use as vasodilators in the treatment of cardiovascular disorders.
Inventors
- 👤 Joel E. Shaffer
- 👤 Stephen A. Thomson
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-04 23:09
CPC Classifications
C; C07; C07D; C07D291/00; C07D291/02; C07D291/04; C07D419/00; C07D419/02; C07D419/04
Claims Analysis
Total Claims: 15
Claim 1
Independent Claim
95 words
A compound of formula (I) ##STR5## wherein R 1 is C 1-8 alkyl, C 2-8 alkenyl, C 5-8 cycloalkyl, aryl-C 1-4 alkyl, heteroaryl or aryl or heteroaryl which is mono-, di-, or trisubstituted independently with halogen, nitro, C 2-4 alkyl, C 1-4 alkoxy, trifluoromethyl, amino or C 1-4 alkyl mono or disubstituted amino with the proviso that R 1 can not be 4-bromophenyl or 2,3,4-trimethoxyphenyl, wherein said aryl is phenyl or naphthyl and said heteroaryl is a 5, 6 or 7 member heteroaryl ring interrupted by one or more N, S or O hetero atoms.
Claim 2
Dependent Claim
95 words
A compound of formula (I) ##STR5## wherein R 1 is C 1-8 alkyl, C 2-8 alkenyl, C 5-8 cycloalkyl, aryl-C 1-4 alkyl, heteroaryl or aryl or heteroaryl which is mono-, di-, or trisubstituted independently with halogen, nitro, C 2-4 alkyl, C 1-4 alkoxy, trifluoromethyl, amino or C 1-4 alkyl mono or disubstituted amino with the proviso that R 1 can not be 4-bromophenyl or 2,3,4-trimethoxyphenyl, wherein said aryl is phenyl or naphthyl and said heteroaryl is a 5, 6 or 7 member heteroaryl ring interrupted by one or more N, S or O hetero atoms.
Claim 3
Dependent Claim
23 words
A compound of claim 1 wherein R 1 is phenyl substituted with a halogen, nitro, C 2-4 alkyl or C 1-4 alkoxy group.
Claim 4
Dependent Claim
13 words
A compound of claim 1 selected from the group: 4-(4-methoxyphenyl)-5H-1,3,2-oxathi(SIV)azol-5-one 4-(4-nitrophenyl)-5H-1,3,2-oxathi(SIV)azol-5-one, and 4-methyl-5H-1,3,2-oxathi(SIV)azol-5-one.
Claim 5
Independent Claim
110 words
A method of treating a cardiovascular disorder by inducing vasodilation in a mammal suffering from said disorder comprising administration of an effective vasodilating amount of a compound of formula (I) ##STR6## wherein R 1 is C 1-8 alkyl, C 2-8 alkenyl, C 5-8 cycloalkyl, aryl-C 1-4 alkyl, aryl or heteroaryl; or aryl or heteroaryl which is mono-, di-, or trisubstituted independently with halogen, nitro, C 1-4 alkyl, C 1-4 alkoxy, trifluoromethyl, amino or C 1-4 alkyl mono or disubstituted amino, wherein said aryl is phenyl or naphthyl and said heteroaryl is a 5, 6 or 7 member heteroaryl ring interrupted by one or more N, S or O hetero atoms.
Claim 6
Independent Claim
110 words
A method of treating a cardiovascular disorder by inducing vasodilation in a mammal suffering from said disorder comprising administration of an effective vasodilating amount of a compound of formula (I) ##STR6## wherein R 1 is C 1-8 alkyl, C 2-8 alkenyl, C 5-8 cycloalkyl, aryl-C 1-4 alkyl, aryl or heteroaryl; or aryl or heteroaryl which is mono-, di-, or trisubstituted independently with halogen, nitro, C 1-4 alkyl, C 1-4 alkoxy, trifluoromethyl, amino or C 1-4 alkyl mono or disubstituted amino, wherein said aryl is phenyl or naphthyl and said heteroaryl is a 5, 6 or 7 member heteroaryl ring interrupted by one or more N, S or O hetero atoms.
Claim 7
Dependent Claim
12 words
A method of claim 4 wherein the cardiovascular disorder is angina pectoris.
Claim 8
Dependent Claim
13 words
A method of claim 4 wherein the cardiovascular disorder is congestive heart failure.
Claim 9
Dependent Claim
12 words
A method of claim 4 wherein the cardiovascular disorder is myocardial ischemia.
Claim 10
Dependent Claim
99 words
A pharmaceutical formulation comprising an effective vasodilating amount of a compound of formula (I) ##STR7## wherein R 1 is C 1-8 alkyl, C 2-8 alkenyl, C 5-8 cycloalkyl, aryl-C 1-4 alkyl, aryl or heteroaryl; or aryl or heteroaryl which is mono-, di-, or trisubstituted independently with halogen, nitro, C 1-4 alkyl, C 1-4 alkoxy, trifluoromethyl, amino or C 1-4 alkyl mono is disubstituted amino and a pharmaceutically acceptable carrier, wherein said aryl is phenyl or naphthyl and said heteroaryl is a 5, 6 or 7 member heteroaryl ring interrupted by one or more N, S or O hetero atoms.
Claim 11
Dependent Claim
99 words
A pharmaceutical formulation comprising an effective vasodilating amount of a compound of formula (I) ##STR7## wherein R 1 is C 1-8 alkyl, C 2-8 alkenyl, C 5-8 cycloalkyl, aryl-C 1-4 alkyl, aryl or heteroaryl; or aryl or heteroaryl which is mono-, di-, or trisubstituted independently with halogen, nitro, C 1-4 alkyl, C 1-4 alkoxy, trifluoromethyl, amino or C 1-4 alkyl mono is disubstituted amino and a pharmaceutically acceptable carrier, wherein said aryl is phenyl or naphthyl and said heteroaryl is a 5, 6 or 7 member heteroaryl ring interrupted by one or more N, S or O hetero atoms.
Claim 12
Dependent Claim
13 words
A formulation of claim 8 in the unit dose form of a tablet.
Claim 13
Dependent Claim
12 words
A formulation of claim 8 in the form of a transdermal system.
Claim 14
Dependent Claim
12 words
A formulation of claim 8 in the form of a sublingual aerosol.
Claim 15
Dependent Claim
13 words
A formulation of claim 8 in the unit dose form of a suppository.
References Cited (Backward Citations)
No citation records indexed.
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| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
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| 3.5 Years (Year 4) | 1995-02-10 | 1995-08-12 | 1996-02-11 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1999-02-10 | 1999-08-12 | 2000-02-11 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2003-02-10 | 2003-08-12 | 2004-02-11 | $7700.00 | Window Closed / Lapsed |