Patent US4649147A successfully refreshed from Google Patents.
US4649147A
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Treating elastin degradation with 1-(alkenoyl)azacycloalkyl carboxylic acids and derivatives
Assignee: GD Searle LLC
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Filing: 1985-07-08
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Granted: 1987-03-10
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Expires: 2005-07-08
Abstract
Abstract This invention relates to 1-(alkenoyl)azacycloalkyl carboxylic acids and derivatives that prevent or reduce the degradation of elastin and other proteins and that thereby prevent or retard the disease states caused by said degradation.
Inventors
- 👤 Richard A. Mueller
- 👤 Richard A. Partis
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-27 03:46
CPC Classifications
C; C07; C07D; C07D211/00; C07D211/04; C07D211/06; C07D211/36; C07D211/60; A; A61; A61P; A61P29/00; A61P3/00; A61P3/06; A61P43/00; A61P9/00; A61P9/12; C07D207/00; C07D207/02; C07D207/04; C07D207/10; C07D207/16; C07D211/62; C07D211/64
Claims Analysis
Total Claims: 16
Claim 1
Independent Claim
152 words
A compound of the formula: ##STR11## wherein R 1 is: (a) alkenyl of 14 to 22 carbon atoms, inclusive; (b) alkadienyl of 14 to 22 carbon atoms, inclusive; or (c) alkapolyenyl of 14 to 22 carbon atoms, inclusive; wherein R 2 is: (a) hydrogen; or (b) phenyl; wherein R 3 is: (a) hydrogen; (b) alkyl of 1 to 6 carbon atoms, inclusive; (c) alkali metal; (d) alkaline earth metal; or (e) NR 4 R 5 R 6 R 7+ ; wherein R 4 , R 5 , R 6 , and R 7 , each being the same or different, are: (a) hydrogen; (b) alkyl or 1 to 6 carbon atoms, inclusive; or (c) hydroxyalkyl of 2 to 4 carbon atoms, inclusive; wherein m is 0, 1, or 2; and wherein n is an integer from 1 to 5, inclusive, with the proviso that the sum (m+n) is 2 to 5, inclusive.
Claim 2
Dependent Claim
152 words
A compound of the formula: ##STR11## wherein R 1 is: (a) alkenyl of 14 to 22 carbon atoms, inclusive; (b) alkadienyl of 14 to 22 carbon atoms, inclusive; or (c) alkapolyenyl of 14 to 22 carbon atoms, inclusive; wherein R 2 is: (a) hydrogen; or (b) phenyl; wherein R 3 is: (a) hydrogen; (b) alkyl of 1 to 6 carbon atoms, inclusive; (c) alkali metal; (d) alkaline earth metal; or (e) NR 4 R 5 R 6 R 7+ ; wherein R 4 , R 5 , R 6 , and R 7 , each being the same or different, are: (a) hydrogen; (b) alkyl or 1 to 6 carbon atoms, inclusive; or (c) hydroxyalkyl of 2 to 4 carbon atoms, inclusive; wherein m is 0, 1, or 2; and wherein n is an integer from 1 to 5, inclusive, with the proviso that the sum (m+n) is 2 to 5, inclusive.
Claim 3
Dependent Claim
25 words
A compound according to claim 1 having the formula: ##STR12## wherein R 3 is: (a) hydrogen; (b) alkyl of 1 to 6 carbon atoms, inclusive.
Claim 4
Dependent Claim
9 words
A compound according to claim 2, which is 1-(1-oxo-9Z-octadecenyl)proline.
Claim 5
Dependent Claim
11 words
A compound according to claim 2, which is 1-(1-oxo-9Z-octadecenyl)proline methyl ester.
Claim 6
Dependent Claim
25 words
A compound according to claim 1 having the formula: ##STR13## wherein R 3 is: (a) hydrogen; (b) alkyl of 1 to 6 carbon atoms, inclusive.
Claim 7
Dependent Claim
10 words
A compound according to claim 5, which is 1-(1-oxo-9Z-octadecenyl)-3-piperidinecarboxylic acid.
Claim 8
Dependent Claim
34 words
A compound according to claim 1 having the formula: ##STR14## wherein R 2 is: (a) hydrogen; or (b) phenyl; wherein R 3 is: (a) hydrogen; (b) alkyl of 1 to 6 carbon atoms, inclusive.
Claim 9
Dependent Claim
10 words
A compound according to claim 7, which is 1-(1-oxo-9Z-octadecenyl)-4-piperidinecarboxylic acid.
Claim 10
Dependent Claim
10 words
A compound according to claim 7, which is 1-(1-oxo-9Z-octadecenyl)-4-phenyl-4-piperidinecarboxylic acid.
Claim 11
Dependent Claim
10 words
A compound according to claim 7, which is ethyl 1-(1-oxo-9Z-octadecenyl)-4-phenyl-4-piperidinecarboxylate.
Claim 12
Dependent Claim
37 words
A pharmaceutical composition for treating protease-induced degradation of elastin and other proteins in mammals comprising a therapeutically effective amount of at least one compound according to claim 1, together with one or more non-toxic pharmaceutically acceptable carriers.
Claim 13
Dependent Claim
30 words
A pharmaceutical composition according to claim 11 wherein said compound is selected from the group consisting of: 1-(1-oxo-9Z-octadecenyl)proline, 1-(1-oxo-9Z-octadecenyl)proline methyl ester, 1-(1-oxo-9Z-octadecenyl)-3-piperidinecarboxylic acid, 1-(1-oxo-9Z-octadecenyl)-4-piperidinecarboxylic acid, 1-(1-oxo-9Z-octadecenyl)-4-phenyl-4-piperidinecarboxylic acid, and ethyl 1-(1-oxo-9Z-octadecenyl)-4-phenyl-4-piperidinecarboxylate.
Claim 14
Dependent Claim
35 words
A method for treating protease-induced degradation of elastin and other proteins in mammals comprising administering a therapeutically effective amount of at least one compound of claim 1 to a mammal in need of such treatment.
Claim 15
Dependent Claim
29 words
A method according to claim 13 wherein said compound is selected from the group consisting of: 1-(1-oxo-9Z-octadecenyl)proline, 1-(1-oxo-9Z-octadecenyl)proline methyl ester, 1-(1-oxo-9Z-octadecenyl)-3-piperidinecarboxylic acid, 1-(1-oxo-9Z-octadecenyl)-4-piperidinecarboxylic acid, 1-(1-oxo-9Z-octadecenyl)-4-phenyl-4-piperidinecarboxylic acid and ethyl 1-(1-oxo-9Z-octadecenyl)-4-phenyl-4-piperidinecarboxylate.
Claim 16
Dependent Claim
34 words
A method for treating protease-induced degradation of elastin and other proteins in mammals comprising administering a therapeutically effective amount of a pharmaceutical composition of claim 11 to a mammal in need of such treatment.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1990-03-09 | 1990-09-08 | 1991-03-10 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1994-03-09 | 1994-09-08 | 1995-03-10 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1998-03-09 | 1998-09-08 | 1999-03-10 | $7700.00 | Window Closed / Lapsed |