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US4670450A
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Cardiotonic thiazolones
Assignee: Aventis Pharmaceuticals Inc
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Filing: 1985-11-13
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Granted: 1987-06-02
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Expires: 2005-11-13
Abstract
Abstract Thiazolones enhance myocardial contractile force and are useful as cardiotonics in the treatment of heart failure.
Inventors
- 👤 Richard A. Schenttler
- 👤 Winton D. Jones, Jr.
- 👤 George P. Claxton
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-05 22:05
CPC Classifications
C; C07; C07D; C07D417/00; C07D417/02; C07D417/04; A; A61; A61P; A61P9/00; A61P9/04; C07D277/00; C07D277/02; C07D277/20; C07D277/32; C07D277/34; C07D277/36
Claims Analysis
Total Claims: 19
Claim 1
Independent Claim
194 words
A thiazolone of the formula ##STR4## wherein Y is an oxygen or sulfur group; R 1 is a hydrogen or a (C 1 -C 5 ) group where R 2 is R; R 2 is a hydrogen or a (C 1 -C 5 ) group where R 1 is R; and R is a phenyl group substituted with one or two members of the group consisting of (C 1 -C 5 ) alkyl, (C 1 -C 5 ) alkoxy, (C 1 -C 5 ) alkylthio, (C 1 -C 5 ) alkylsulfinyl, (C 1 -C 5 )alkylsulfonyl, hydroxy, halogen, cyano, carboxy, carb(C 1 -C 5 )alkoxy, (C 1 -C 5 ) alkanoylamino, imidazolyl or trifluoromethyl, or with a methylenedioxy group; or a 2-, 3- or 4- pyridyl group optionally substituted with a hydroxy, halogen, (C 1 -C 5 ) alkyl, (C 1 -C 5 ) alkoxy, (C 1 -C 5 ) alkylthio, (C 1 -C 5 ) alkylsulfinyl, (C 1 -C 5 ) alkylsulfonyl, cyano, carboxy, carb(C 1 -C 5 ) alkoxy, (C 1 -C 5 )alkanoylamino, imidazolyl, or R is a 2- or 3- furanyl, 2- or 3- thienyl or 2- or 3-pyranyl group.
Claim 2
Dependent Claim
194 words
A thiazolone of the formula ##STR4## wherein Y is an oxygen or sulfur group; R 1 is a hydrogen or a (C 1 -C 5 ) group where R 2 is R; R 2 is a hydrogen or a (C 1 -C 5 ) group where R 1 is R; and R is a phenyl group substituted with one or two members of the group consisting of (C 1 -C 5 ) alkyl, (C 1 -C 5 ) alkoxy, (C 1 -C 5 ) alkylthio, (C 1 -C 5 ) alkylsulfinyl, (C 1 -C 5 )alkylsulfonyl, hydroxy, halogen, cyano, carboxy, carb(C 1 -C 5 )alkoxy, (C 1 -C 5 ) alkanoylamino, imidazolyl or trifluoromethyl, or with a methylenedioxy group; or a 2-, 3- or 4- pyridyl group optionally substituted with a hydroxy, halogen, (C 1 -C 5 ) alkyl, (C 1 -C 5 ) alkoxy, (C 1 -C 5 ) alkylthio, (C 1 -C 5 ) alkylsulfinyl, (C 1 -C 5 ) alkylsulfonyl, cyano, carboxy, carb(C 1 -C 5 ) alkoxy, (C 1 -C 5 )alkanoylamino, imidazolyl, or R is a 2- or 3- furanyl, 2- or 3- thienyl or 2- or 3-pyranyl group.
Claim 3
Dependent Claim
11 words
A thiazolone of claim 1 wherein Y is an oxygen group.
Claim 4
Dependent Claim
20 words
A thiazolone of claim 2 wherein R 1 or R 2 is a (C 1 -C 5 ) alkyl group.
Claim 5
Dependent Claim
18 words
A thiazolone of claim 2 wherein R 2 is an optionally substituted phenyl or optionally substituted pyridyl group.
Claim 6
Dependent Claim
15 words
A thiazolone of claim 2 wherein R 1 is a methyl, ethyl or propyl group.
Claim 7
Dependent Claim
17 words
A thiazolone of claim 5 wherein R 2 is an unsubstituted phenyl group or unsubstituted 4-pyridyl group.
Claim 8
Dependent Claim
28 words
A method of treating heart failure in a patient in need thereof which comprises administering to the patient a cardiotonically effective amount of a thiazolone of claim 1.
Claim 9
Dependent Claim
11 words
A method of claim 7 wherein Y is an oxygen group.
Claim 10
Dependent Claim
20 words
A method of claim 8 wherein R 1 or R 2 is a (C 1 -C 5 ) alkyl group.
Claim 11
Dependent Claim
18 words
A method of claim 8 wherein R 2 is an optionally substituted phenyl or optionally substituted pyridyl group.
Claim 12
Dependent Claim
15 words
A method of claim 8 wherein R 1 is a methyl, ethyl or propyl group.
Claim 13
Dependent Claim
17 words
A method of claim 11 wherein R 2 is an unsubstituted phenyl group or unsubstituted 4-pyridyl group.
Claim 14
Dependent Claim
28 words
A method of enhancing myocardial contractile force in a patient in need thereof which comprises administering to the patient an effective amount of a method of claim 1.
Claim 15
Dependent Claim
11 words
A method of claim 13 wherein Y is an oxygen group.
Claim 16
Dependent Claim
20 words
A method of claim 14 wherein R 1 or R 2 is a (C 1 -C 5 ) alkyl group.
Claim 17
Dependent Claim
18 words
A method of claim 14 wherein R 2 is an optionally substituted phenyl or optionally substituted pyridyl group.
Claim 18
Dependent Claim
15 words
A method of claim 14 wherein R 1 is a methyl, ethyl or propyl group.
Claim 19
Dependent Claim
17 words
A method of claim 17 wherein R 2 is an unsubstituted phenyl group or unsubstituted 4-pyridyl group.
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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) | 1990-06-01 | 1990-12-01 | 1991-06-02 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1994-06-01 | 1994-12-01 | 1995-06-02 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1998-06-01 | 1998-12-01 | 1999-06-02 | $7700.00 | Window Closed / Lapsed |