US5250550A
Expired / Lapsed
US
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Complexes of nitric oxide with polyamines
Assignee: United States Department of Health and Human Services
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Filing: 1992-06-30
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Granted: 1993-10-05
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Expires: 2012-06-30
Abstract
Abstract There are disclosed novel complexes of nitric oxide and polyamines which are useful in treating cardiovascular disorders, including hypertension. The disclosed compounds release nitric oxide (endothelium-derived relaxing factor) under physiological conditions in a sustained and controllable fashion, and possess long mechanisms of action.
Inventors
- 👤 Larry K. Keefer
- 👤 Joseph A. Hrabie
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-30 05:50
CPC Classifications
C; C07; C07C; C07C243/00; C07C243/04; C07C243/06; A; A61; A61P; A61P9/00; A61P9/08; A61P9/10; A61P9/12; C01; C01B; C01B21/00; C01B21/20; C01B21/24; C07C211/00; C07C211/01; C07C211/02; C07C211/14
Claims Analysis
Total Claims: 19
Claim 1
Independent Claim
66 words
A compound of Formula II: ##STR7## and R 6 and R 7 , same or different, are hydrogen, C 3-8 cycloalkyl, C 1-12 straight or branched chain alkyl, benzyl, benzoyl, phthaloyl, acetyl, trifluoroacetyl, p-toluyl, t-butoxycarbonyl or 2,2,2-trichloro-t-butoxycarbonyl; f is 0 to 12, with the proviso that when B is the substituted piperazine moiety ##STR8## then f is 2 to 12; or a pharmaceutically acceptable salt thereof.
Claim 2
Dependent Claim
66 words
A compound of Formula II: ##STR7## and R 6 and R 7 , same or different, are hydrogen, C 3-8 cycloalkyl, C 1-12 straight or branched chain alkyl, benzyl, benzoyl, phthaloyl, acetyl, trifluoroacetyl, p-toluyl, t-butoxycarbonyl or 2,2,2-trichloro-t-butoxycarbonyl; f is 0 to 12, with the proviso that when B is the substituted piperazine moiety ##STR8## then f is 2 to 12; or a pharmaceutically acceptable salt thereof.
Claim 3
Dependent Claim
32 words
A compound as recited in claim 1, wherein: R 6 and R 7 , same or different, are hydrogen, C 5-6 cycloalkyl, C 1-4 straight or branched chain alkyl, benzyl or acetyl.
Claim 4
Dependent Claim
30 words
A compound as recited in claim 2, wherein: R 6 and R 7 , same or different, are hydrogen, methyl, ethyl, benzyl or acetyl; and f is 2 to 4.
Claim 5
Dependent Claim
22 words
A compound as recited in claim 3, wherein: R 6 and R 7 , same or different, are hydrogen, methyl, or acetyl.
Claim 6
Dependent Claim
57 words
A compound of Formula III: ##STR9## wherein: R 8 is hydrogen, C 3-8 cycloalkyl, C 1-12 straight or branched chain alkyl, benzyl, benzoyl, phthaloyl, acetyl, trifluoroacetyl, p-toluyl, t-butoxycarbonyl or 2,2,2-tri-chloro-t-butoxycarbonyl; R 9 is hydrogen or a C 1 -C 12 straight or branched chain alkyl; and g is 2 to 6; or a pharmaceutically acceptable salt thereof.
Claim 7
Dependent Claim
57 words
A compound of Formula III: ##STR9## wherein: R 8 is hydrogen, C 3-8 cycloalkyl, C 1-12 straight or branched chain alkyl, benzyl, benzoyl, phthaloyl, acetyl, trifluoroacetyl, p-toluyl, t-butoxycarbonyl or 2,2,2-tri-chloro-t-butoxycarbonyl; R 9 is hydrogen or a C 1 -C 12 straight or branched chain alkyl; and g is 2 to 6; or a pharmaceutically acceptable salt thereof.
Claim 8
Dependent Claim
24 words
A compound as recited in claim 5, wherein: R 8 is C 5-6 cycloalkyl, C 1-4 straight or branched chain alkyl, benzyl or acetyl.
Claim 9
Dependent Claim
22 words
A compound as recited in claim 6, wherein: R 8 is methyl, ethyl, benzyl or acetyl; and g is 2 to 4.
Claim 10
Dependent Claim
14 words
A compound as recited in claim 7, wherein: R 8 is methyl or acetyl.
Claim 11
Dependent Claim
20 words
A compound as recited in claim 5, wherein the Formula III compound is: ##STR10## or a pharmaceutically acceptable salt thereof.
Claim 12
Independent Claim
92 words
A method of treating cardiovascular disorders which are treatable by lowering blood pressure, the method comprising: administering to a mammal, in need thereof, an effective amount of a compound of Formula II: ##STR11## R 6 and R 7 , same or different, are hydrogen, C 3-8 cycloalkyl, C 1-12 straight or branched chain alkyl, benzyl, benzoyl, phthaloyl, acetyl, trifluoroacetyl, p-toluyl, t-butoxycarbonyl or 2,2,2-trichloro-t-butoxycarbonyl; f is 0 to 12, with the proviso that when B is the substituted piperazine moiety ##STR12## then f is 2 to 12; or a pharmaceutically acceptable salt thereof.
Claim 13
Independent Claim
92 words
A method of treating cardiovascular disorders which are treatable by lowering blood pressure, the method comprising: administering to a mammal, in need thereof, an effective amount of a compound of Formula II: ##STR11## R 6 and R 7 , same or different, are hydrogen, C 3-8 cycloalkyl, C 1-12 straight or branched chain alkyl, benzyl, benzoyl, phthaloyl, acetyl, trifluoroacetyl, p-toluyl, t-butoxycarbonyl or 2,2,2-trichloro-t-butoxycarbonyl; f is 0 to 12, with the proviso that when B is the substituted piperazine moiety ##STR12## then f is 2 to 12; or a pharmaceutically acceptable salt thereof.
Claim 14
Independent Claim
84 words
A method of treating cardiovascular disorders which are treatable by lowering blood pressure, the method comprising: administering to a mammal, in need thereof, an effective amount of a compound of Formula III: ##STR13## wherein: R 8 is hydrogen, C 3-8 cycloalkyl, C 1-12 straight or branched chain alkyl, benzyl, benzoyl, phthaloyl, acetyl, trifluoroacetyl, p-toluyl, t-butoxycarbonyl or 2,2,2-trichloro-t-butoxycarbonyl; R 9 is hydrogen or a C 1 -C 12 straight or branched chain alkyl; and g is 2 to 6; or a pharmaceutically acceptable salt thereof.
Claim 15
Independent Claim
84 words
A method of treating cardiovascular disorders which are treatable by lowering blood pressure, the method comprising: administering to a mammal, in need thereof, an effective amount of a compound of Formula III: ##STR13## wherein: R 8 is hydrogen, C 3-8 cycloalkyl, C 1-12 straight or branched chain alkyl, benzyl, benzoyl, phthaloyl, acetyl, trifluoroacetyl, p-toluyl, t-butoxycarbonyl or 2,2,2-trichloro-t-butoxycarbonyl; R 9 is hydrogen or a C 1 -C 12 straight or branched chain alkyl; and g is 2 to 6; or a pharmaceutically acceptable salt thereof.
Claim 16
Dependent Claim
92 words
A pharmaceutical composition, comprising: an effective amount of a compound of Formula II for treating a cardiovascular disorder which is treatable by lowering blood pressure; ##STR14## R 6 and R 7 , same or different, are hydrogen, C 3-8 cycloalkyl, C 1-12 straight or branched chain alkyl, benzyl, benzoyl, phthaloyl, acetyl, trifluoroacetyl, p-toluyl, t-butoxycarbonyl or 2,2,2-trichloro-t butoxycarbonyl, f is 0 to 12, with the proviso that when B is the substituted piperazine moiety ##STR15## then f is 2 to 12, or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable carrier therefor.
Claim 17
Dependent Claim
92 words
A pharmaceutical composition, comprising: an effective amount of a compound of Formula II for treating a cardiovascular disorder which is treatable by lowering blood pressure; ##STR14## R 6 and R 7 , same or different, are hydrogen, C 3-8 cycloalkyl, C 1-12 straight or branched chain alkyl, benzyl, benzoyl, phthaloyl, acetyl, trifluoroacetyl, p-toluyl, t-butoxycarbonyl or 2,2,2-trichloro-t butoxycarbonyl, f is 0 to 12, with the proviso that when B is the substituted piperazine moiety ##STR15## then f is 2 to 12, or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable carrier therefor.
Claim 18
Dependent Claim
81 words
A pharmaceutical composition, comprising: an effective amount of a compound of Formula III for treating a cardiovascular disorder that is treatable by lowering blood pressure: ##STR16## wherein: R 8 is hydrogen, C 3-8 cycloalkyl, C 1-12 straight or branched chain alkyl, benzyl, benzoyl, phthaloyl, acetyl, trifluoroacetyl, p-toluyl, t-butoxycarbonyl or 2,2,2-trichloro-t-butoxycarbonyl, R 9 is hydrogen or a Chd 1-C 12 straight or branched chain alkyl, and g is 2 to 6, or a pharmaceutically acceptable salt thereof; and a pharmaceutically carrier therefor.
Claim 19
Dependent Claim
81 words
A pharmaceutical composition, comprising: an effective amount of a compound of Formula III for treating a cardiovascular disorder that is treatable by lowering blood pressure: ##STR16## wherein: R 8 is hydrogen, C 3-8 cycloalkyl, C 1-12 straight or branched chain alkyl, benzyl, benzoyl, phthaloyl, acetyl, trifluoroacetyl, p-toluyl, t-butoxycarbonyl or 2,2,2-trichloro-t-butoxycarbonyl, R 9 is hydrogen or a Chd 1-C 12 straight or branched chain alkyl, and g is 2 to 6, or a pharmaceutically acceptable salt thereof; and a pharmaceutically carrier therefor.
References Cited (Backward Citations)
No citation records indexed.
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1996-10-04 | 1997-04-05 | 1997-10-05 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 2000-10-04 | 2001-04-05 | 2001-10-05 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2004-10-04 | 2005-04-05 | 2005-10-05 | $7700.00 | Window Closed / Lapsed |