US5034528A
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US
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Compositions for the control of hyperlipidemia
Assignee: North Carolina Central University
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Filing: 1988-07-27
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Granted: 1991-07-23
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Expires: 2008-07-27
Abstract
Abstract The invention provides pharmaceutical compositions comprising hypolipidemically active derivatives of 1,2,4-triazolidine-3,5-diones, 1,3,5-triazabicyclo[3.1.0]hexane-2,4-diones, and 1,3,5-triazine-2,4(1_H,3_H)-diones in a pharmaceutically acceptable carrier for treating hyperlipidemia in mammals, particularly humans.
Inventors
- 👤 Robert A. Izydore
- 👤 Iris H. Hall
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-03 16:06
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/41; A61K31/53
Claims Analysis
Total Claims: 6
Claim 1
Independent Claim
378 words
A pharmaceutical compound for controlling hyperlipidemia in mammals having the following structural formula: ##STR6## wherein R 1 hydrogen, a C 1 to C 18 alkyl or substituted alkyl, a C 2 to C 18 alkenyl or substituted alkenyl, a C 2 to C 18 alkynyl or substituted alkynyl, a C 4 to C 10 cycloalkyl or substituted cycloalkyl, a C 4 to C 10 cycloalkenyl or substituted cycloalkenyl, phenyl, a substituted phenyl, cyano, phenalkyl, --CO--R 9 or --Y--CO--R 9 ; R 5 and R 6 be the same or different and are each hydrogen, a C 1 to C 18 alkyl or substituted alkyl, a C 2 to C 18 alkenyl or substituted alkenyl, a C 2 to C 18 alkynyl or substituted alkynyl, a C 4 to C 10 cycloalkyl or substituted cycloalkyl, a C 4 to C 10 cycloalkyl or substituted cycloalkenyl, phenyl or substituted phenyl, phenalkyl, --CO--R 9 , or --Y--CO--R 9 , with the proviso that R 5 and R 6 are not both aromatic; R 9 is hydrogen, a C 1 to C 5 alkyl or substituted alkyl, a C 2 to C 5 alkenyl or substituted alkenyl, a C 2 to C 5 alkynyl or substituted alkynyl, phenyl or substituted phenyl, phenoxy or substituted phenoxy, a C 1 to C 5 alkoxy or substituted alkoxy, a C 4 to C 10 cycloalkyl or substituted cycloalkenyl, --NHC 6 H 5 , --NR 10 R 11 wherein R 10 and R 11 can be the same or different and are each hydrogen, a C 1 to C 5 alkyl or substituted alkyl, phenyl or substituted phenyl; and Y is a C 1 to C 10 alkylene or substituted alkylene; and the pharmaceutically acceptable salts thereof, and mixtures thereof; provided that R 1 is not phenyl, chlorophenyl, methoxyphenyl or n-butyl when R 5 is hydrogen, R 6 is --CO--R 9 , and R 9 is ethoxy or when R 6 is hydrogen, R 5 is --CO--R 9 , and R 9 is ethoxy; and further provided that R 1 is not phenyl when R 5 is hydrogen, R 6 is --CO--R 9 , and R 9 is methoxy or when R 6 is hydrogen, R 5 is --CO--R 9 , and R 9 is methoxy.
Claim 2
Dependent Claim
378 words
A pharmaceutical compound for controlling hyperlipidemia in mammals having the following structural formula: ##STR6## wherein R 1 hydrogen, a C 1 to C 18 alkyl or substituted alkyl, a C 2 to C 18 alkenyl or substituted alkenyl, a C 2 to C 18 alkynyl or substituted alkynyl, a C 4 to C 10 cycloalkyl or substituted cycloalkyl, a C 4 to C 10 cycloalkenyl or substituted cycloalkenyl, phenyl, a substituted phenyl, cyano, phenalkyl, --CO--R 9 or --Y--CO--R 9 ; R 5 and R 6 be the same or different and are each hydrogen, a C 1 to C 18 alkyl or substituted alkyl, a C 2 to C 18 alkenyl or substituted alkenyl, a C 2 to C 18 alkynyl or substituted alkynyl, a C 4 to C 10 cycloalkyl or substituted cycloalkyl, a C 4 to C 10 cycloalkyl or substituted cycloalkenyl, phenyl or substituted phenyl, phenalkyl, --CO--R 9 , or --Y--CO--R 9 , with the proviso that R 5 and R 6 are not both aromatic; R 9 is hydrogen, a C 1 to C 5 alkyl or substituted alkyl, a C 2 to C 5 alkenyl or substituted alkenyl, a C 2 to C 5 alkynyl or substituted alkynyl, phenyl or substituted phenyl, phenoxy or substituted phenoxy, a C 1 to C 5 alkoxy or substituted alkoxy, a C 4 to C 10 cycloalkyl or substituted cycloalkenyl, --NHC 6 H 5 , --NR 10 R 11 wherein R 10 and R 11 can be the same or different and are each hydrogen, a C 1 to C 5 alkyl or substituted alkyl, phenyl or substituted phenyl; and Y is a C 1 to C 10 alkylene or substituted alkylene; and the pharmaceutically acceptable salts thereof, and mixtures thereof; provided that R 1 is not phenyl, chlorophenyl, methoxyphenyl or n-butyl when R 5 is hydrogen, R 6 is --CO--R 9 , and R 9 is ethoxy or when R 6 is hydrogen, R 5 is --CO--R 9 , and R 9 is ethoxy; and further provided that R 1 is not phenyl when R 5 is hydrogen, R 6 is --CO--R 9 , and R 9 is methoxy or when R 6 is hydrogen, R 5 is --CO--R 9 , and R 9 is methoxy.
Claim 3
Dependent Claim
77 words
The pharmaceutical compound of claim 1 wherein R 1 is selected from the group consisting of phenyl, halophenyl, alkylphenyl wherein the alkyl group has from 1 to 5 carbon atoms, alkoxyphenyl wherein the alkoxy group has from 1 to 5 carbon atoms; and R 5 and R 6 may be the same or different and are each selected from the group consisting of hydrogen and alkoxycarbonyl wherein the alkoxy group has from 1 to 5 carbon atoms.
Claim 4
Dependent Claim
292 words
A pharmaceutical compound for controlling hyperlipidemia in mammals having the following structural formula: ##STR7## wherein R 1 hydrogen, a C 1 to C 5 alkyl or substituted alkyl, a C 2 to C 5 alkenyl or substituted alkenyl, a C 2 to C 5 alkynyl or substituted alkynyl, phenyl or a substituted phenyl, phenyalkyl, --CO--R 9 or --Y--CO--R 9 ; R 5 and R 6 be the same or different and are each hydrogen, a C 1 to C 5 alkyl or substituted alkyl, a C 2 to C 5 alkenyl or substituted alkenyl, a C 1 to C 5 alkynyl or substituted alkynyl, phenyl or substituted phenyl, phenalkyl, --CO--R 9 , or --Y--CO--R 9 , with the proviso that R 5 and R 6 are not both aromatic; R 9 is hydrogen, a C 1 to C 5 alkyl or substituted alkyl, a C 2 to C 5 alkenyl or substituted alkenyl, a C 2 to C 5 alkynyl or substituted alkynyl, phenyl or substituted phenyl, phenoxy or substituted phenoxy, a C 1 to C 5 alkoxy or substituted alkoxy, or --NHC 6 H 5 and Y is a C 1 to C 5 alkylene or substituted alkylene; and the pharmaceutically acceptable salts, and mixtures thereof; provided that R' is not phenyl, chlorophenyl, methoxyphenyl or n-butyl when R 5 is hydrogen, R 6 is --CO--R 9 , and R 9 is ethoxy or when R 6 is hydrogen, R 5 is --CO--R 9 , and R 9 is ethoxy; and further provided that R 1 is not phenyl when R 5 is hydrogen, R 6 is --CO--R 9 , and R 9 is methoxy or when R 6 is hydrogen, R 5 is --CO--R 9 , and R 9 is methoxy.
Claim 5
Dependent Claim
292 words
A pharmaceutical compound for controlling hyperlipidemia in mammals having the following structural formula: ##STR7## wherein R 1 hydrogen, a C 1 to C 5 alkyl or substituted alkyl, a C 2 to C 5 alkenyl or substituted alkenyl, a C 2 to C 5 alkynyl or substituted alkynyl, phenyl or a substituted phenyl, phenyalkyl, --CO--R 9 or --Y--CO--R 9 ; R 5 and R 6 be the same or different and are each hydrogen, a C 1 to C 5 alkyl or substituted alkyl, a C 2 to C 5 alkenyl or substituted alkenyl, a C 1 to C 5 alkynyl or substituted alkynyl, phenyl or substituted phenyl, phenalkyl, --CO--R 9 , or --Y--CO--R 9 , with the proviso that R 5 and R 6 are not both aromatic; R 9 is hydrogen, a C 1 to C 5 alkyl or substituted alkyl, a C 2 to C 5 alkenyl or substituted alkenyl, a C 2 to C 5 alkynyl or substituted alkynyl, phenyl or substituted phenyl, phenoxy or substituted phenoxy, a C 1 to C 5 alkoxy or substituted alkoxy, or --NHC 6 H 5 and Y is a C 1 to C 5 alkylene or substituted alkylene; and the pharmaceutically acceptable salts, and mixtures thereof; provided that R' is not phenyl, chlorophenyl, methoxyphenyl or n-butyl when R 5 is hydrogen, R 6 is --CO--R 9 , and R 9 is ethoxy or when R 6 is hydrogen, R 5 is --CO--R 9 , and R 9 is ethoxy; and further provided that R 1 is not phenyl when R 5 is hydrogen, R 6 is --CO--R 9 , and R 9 is methoxy or when R 6 is hydrogen, R 5 is --CO--R 9 , and R 9 is methoxy.
Claim 6
Dependent Claim
38 words
A pharmaceutical composition for use in controlling hyperlipidemia in mammals which comprises a hypolipidemically effective amount of a compound having hypolipidemic activity and a structural formula as defined in claim 1 in combination with a pharmaceutically acceptable carrier.
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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) | 1994-07-22 | 1995-01-21 | 1995-07-23 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1998-07-22 | 1999-01-21 | 1999-07-23 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2002-07-22 | 2003-01-21 | 2003-07-23 | $7700.00 | Window Closed / Lapsed |