Patent US5393772A successfully refreshed from Google Patents.
US5393772A
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Use of, and method of treatment using, hydroxycarbazole compounds for inhibition of smooth muscle migration and proliferation
Assignee: BOEHRINGER MANNHEIM PHARMACEUTICALS CORPORATION-SMITHKLINE BEECHAM Corp NO 1 LP
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Filing: 1993-11-24
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Granted: 1995-02-28
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Expires: 2013-11-24
Abstract
Abstract The present invention provides a new medical use of the hydroxycarbazole compounds of Formula (I), preferably the hydroxylated metabolites of 1-(carbazol-4-yloxy-3-[[2-(o-methoxyphenoxy)ethyl]amino]-2-propanol)(carvedilol), for inhibiting the migration and proliferation of smooth muscle cells. In particular, the present invention provides a new use for the hydroxycarbazole compounds of Formula (I) for prevention of restenosis following percutaneous transluminal coronary angioplasty (PTCA), suppression of the progression of vascular hypertrophy associated with hypertension, and prevention of development of atherosclerosis. <IMAGE> (I) wherein: R1-R9 are independently -H or -OH, with the proviso that a at least one of R1-R9 is OH.
Inventors
- 👤 Tian-Li Yue
- 👤 Eliot H. Ohlstein
- 👤 Giora Z. Feuerstein
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 15:19
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/40; A61P; A61P9/00; A61P9/08; A61P9/10; A61P9/12
Claims Analysis
Total Claims: 33
Claim 1
Independent Claim
65 words
A method of treatment for inhibition of proliferation and migration of smooth muscle cells in mammals comprising internally administering to a mammal in need thereof an effective amount of a compound of Formula (I): ##STR6## wherein: R 1 -R 9 are independently --H or --OH, with the proviso that at least one of R 1 -R 9 is OH, or a pharmaceutically acceptable salt thereof.
Claim 2
Independent Claim
65 words
A method of treatment for inhibition of proliferation and migration of smooth muscle cells in mammals comprising internally administering to a mammal in need thereof an effective amount of a compound of Formula (I): ##STR6## wherein: R 1 -R 9 are independently --H or --OH, with the proviso that at least one of R 1 -R 9 is OH, or a pharmaceutically acceptable salt thereof.
Claim 3
Dependent Claim
13 words
A method of treatment according to claim 1 wherein said mammal is human.
Claim 4
Dependent Claim
26 words
A method of treatment according to claim 1 wherein in said compound of Formula (I), R 1 is OH and R 2 -R 9 are H.
Claim 5
Dependent Claim
30 words
A method of treatment according to claim 1 wherein in said compound of Formula (I), R 2 is OH and R 1 , and R 3 -R 9 are H.
Claim 6
Dependent Claim
33 words
A method of treatment according to claim 1 wherein in said compound of Formula (I), R 3 is OH and R 1 , R 2 , and R 4 -R 9 are H.
Claim 7
Dependent Claim
31 words
A method of treatment according to claim 1 wherein in said compound of Formula (I), R 5 is OH and R 1 -R 4 and R 6 -R 9 are H.
Claim 8
Dependent Claim
31 words
A method of treatment according to claim 1 wherein in said compound of Formula (I), R 6 is OH and R 1 -R 5 and R 7 -R 9 are H.
Claim 9
Dependent Claim
29 words
A method of treatment according to claim 1 wherein in said compound of Formula (I), R 8 is OH and R 1 -R 7 and R 9 are H.
Claim 10
Dependent Claim
44 words
A method of treatment according to claim 1 wherein human patients surviving percutaneous transluminal coronary angioplasty (PTCA) are administered an effective dose of a pharmaceutical composition comprising a compound of Formula (I), to inhibit restenosis by angioplasty-induced neointimal proliferation in blood vessels following PTCA.
Claim 11
Dependent Claim
17 words
A method of treatment according to claim 9 wherein said pharmaceutical composition is suitable for parenteral administration.
Claim 12
Dependent Claim
26 words
A method of treatment according to claim 9 wherein in said compound of Formula (I), R 1 is OH and R 2 -R 9 are H.
Claim 13
Dependent Claim
30 words
A method of treatment according to claim 9 wherein in said compound of Formula (I), R 2 is OH and R 1 , and R 3 -R 9 are H.
Claim 14
Dependent Claim
33 words
A method of treatment according to claim 9 wherein in said compound of Formula (I), R 3 is OH and R 1 , R 2 , and R 4 -R 9 are H.
Claim 15
Dependent Claim
31 words
A method of treatment according to claim 9 wherein in said compound of Formula (I), R 5 is OH and R 1 -R 4 and R 6 -R 9 are H.
Claim 16
Dependent Claim
31 words
A method of treatment according to claim 9 wherein in said compound of Formula (I), R 6 is OH and R 1 -R 5 and R 7 -R 9 are H.
Claim 17
Dependent Claim
29 words
A method of treatment according to claim 9 wherein in said compound of Formula (I), R 8 is OH and R 1 -R 7 and R 9 are H.
Claim 18
Dependent Claim
31 words
A method of treatment according to claim 1 wherein human patients are administered an effective dose of a pharmaceutical comprising a compound of Formula (I) for inhibition of development of atherosclerosis.
Claim 19
Dependent Claim
17 words
A method of treatment according to claim 17 wherein said pharmaceutical composition is suitable for parenteral administration.
Claim 20
Dependent Claim
26 words
A method of treatment according to claim 17 wherein in said compound of Formula (I), R 1 is OH and R 2 -R 9 are H.
Claim 21
Dependent Claim
30 words
A method of treatment according to claim 17 wherein in said compound of Formula (I), R 2 is OH and R 1 , and R 3 -R 9 are H.
Claim 22
Dependent Claim
33 words
A method of treatment according to claim 17 wherein in said compound of Formula (I), R 3 is OH and R 1 , R 2 , and R 4 -R 9 are H.
Claim 23
Dependent Claim
31 words
A method of treatment according to claim 17 wherein in said compound of Formula (I), R 5 is OH and R 1 -R 4 and R 6 -R 9 are H.
Claim 24
Dependent Claim
31 words
A method of treatment according to claim 17 wherein in said compound of Formula (I), R 6 is OH and R 1 -R 5 and R 7 -R 9 are H.
Claim 25
Dependent Claim
29 words
A method of treatment according to claim 17 wherein in said compound of Formula (I), R 8 is OH and R 1 -R 7 and R 9 are H.
Claim 26
Dependent Claim
36 words
A method of treatment according to claim 1 wherein human patients are administered an effective dose of a pharmaceutical composition comprising a compound of Formula (I) for suppressing the progression of vascular hypertrophy associated with hypertension.
Claim 27
Dependent Claim
18 words
A method of treatment according to claim 25 wherein in said pharmaceutical composition is suitable for parenteral treatment.
Claim 28
Dependent Claim
26 words
A method of treatment according to claim 25 wherein in said compound of Formula (I), R 1 is OH and R 2 -R 9 are H.
Claim 29
Dependent Claim
30 words
A method of treatment according to claim 25 wherein in said compound of Formula (I), R 2 is OH and R 1 , and R 3 -R 9 are H.
Claim 30
Dependent Claim
33 words
A method of treatment according to claim 25 wherein in said compound of Formula (I), R 3 is OH and R 1 , R 2 , and R 4 -R 9 are H.
Claim 31
Dependent Claim
31 words
A method of treatment according to claim 25 wherein in said compound of Formula (I), R 5 is OH and R 1 -R 4 and R 6 -R 9 are H.
Claim 32
Dependent Claim
31 words
A method of treatment according to claim 25 wherein in said compound of Formula (I), R 6 is OH and R 1 -R 5 and R 7 -R 9 are H.
Claim 33
Dependent Claim
29 words
A method of treatment according to claim 25 wherein in said compound of Formula (I), R 8 is OH and R 1 -R 7 and R 9 are H.
References Cited (Backward Citations)
US5308862A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1998-02-27 | 1998-08-29 | 1999-02-28 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 2002-02-27 | 2002-08-29 | 2003-02-28 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2006-02-27 | 2006-08-29 | 2007-02-28 | $7700.00 | Window Closed / Lapsed |