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US4473572A
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α2 -Adrenoceptor antagonistic benzoquinolizines
Assignee: John Wyeth and Brother Ltd
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Filing: 1983-03-03
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Granted: 1984-09-25
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Expires: 2003-03-03
Abstract
Abstract The invention concerns benzoquinolizines of formula ##STR1## and their pharmaceutically acceptable acid addition salts. In the formula, R 1 and R 2 which may be the same or different, each represent hydrogen, lower alkyl, lower alkoxy or halogen, R 3 represents methyl or ethyl and R 4 represents halo(lower)alkyl. The compounds possess α 2 -adrenoceptor antagonistic activity and can be incorporated into pharmaceutical compositions.
Inventors
- 👤 Terence J. Ward
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-07 17:56
CPC Classifications
C; C07; C07D; C07D455/00; C07D455/03; C07D455/04; C07D455/06
Claims Analysis
Total Claims: 10
Claim 1
Independent Claim
49 words
A compound selected from the group consisting of a benzoquinolizine of the formula ##STR7## and a pharmaceutically acceptable acid addition salt thereof, wherein R 1 and R 2 each represent hydrogen, lower alkyl, lower alkoxy or halogen, R 3 represents methyl or ethyl and R 4 represents mono- poly-halo(lower)alkyl.
Claim 2
Dependent Claim
49 words
A compound selected from the group consisting of a benzoquinolizine of the formula ##STR7## and a pharmaceutically acceptable acid addition salt thereof, wherein R 1 and R 2 each represent hydrogen, lower alkyl, lower alkoxy or halogen, R 3 represents methyl or ethyl and R 4 represents mono- poly-halo(lower)alkyl.
Claim 3
Dependent Claim
17 words
A compound according to claim 1 which is N-methyl-N-(1,3,4,6,7,11bα-hexahydro-2H-benzo[a]quinolizin-2β-yl)-trifluoromethanesulphonamide or a pharmaceutically acceptable acid addition salt thereof.
Claim 4
Dependent Claim
17 words
A compound according to claim 1 which is N-methyl-N-(1,3,4,6,7,11bα-hexahydro-2H-benzo[a]quinolizin-2β-yl)-2',2',2'-trifluoroethanesulphonamide or a pharmaceutically acceptable acid addition salt thereof.
Claim 5
Dependent Claim
17 words
A compound according to claim 1 which is N-methyl-N-(1,3,4,6,7,11bα-hexahydro-2H-benzo[a]quinolizin-2β-yl)chloromethanesulphonamide or a pharmaceutically acceptable acid addition salt thereof.
Claim 6
Dependent Claim
17 words
A compound according to claim 1 which is N-methyl-N-(1,3,4,6,7,11bα-hexahydro-2H-benzo[a]quinolizin-2β-yl)-3'-chloropropanesulphonamide or a pharmaceutically acceptable acid addition salt thereof.
Claim 7
Dependent Claim
67 words
A pharmaceutical composition having α 2 -adrenoceptor antagonistic activity comprising an amount effective to antagonise α 2 -adrenoceptors of a compound selected from the group consisting of a benqoquinolizine of the formula ##STR8## and a pharmaceutically acceptable acid addition salt thereof, wherein R 1 and R 2 each represent hydrogen, lower alkyl, lower alkoxy or halogen, R 3 represents methyl or ethyl and R 4 represents halo(lower)alkyl.
Claim 8
Dependent Claim
67 words
A pharmaceutical composition having α 2 -adrenoceptor antagonistic activity comprising an amount effective to antagonise α 2 -adrenoceptors of a compound selected from the group consisting of a benqoquinolizine of the formula ##STR8## and a pharmaceutically acceptable acid addition salt thereof, wherein R 1 and R 2 each represent hydrogen, lower alkyl, lower alkoxy or halogen, R 3 represents methyl or ethyl and R 4 represents halo(lower)alkyl.
Claim 9
Independent Claim
69 words
A method of antagonising α 2 -adrenoceptors in warm blooded animals which comprises administering to the animal an effective amount of a compound selected from the group consisting of a benzoquinolizine of the formula ##STR9## and a pharmaceutically acceptable acid addition salt thereof, wherein R 1 and R 2 each represent hydrogen, lower alkyl, lower alkoxy or halogen, R 3 represents methyl or ethyl and R 4 represents halo(lower)alkyl.
Claim 10
Independent Claim
69 words
A method of antagonising α 2 -adrenoceptors in warm blooded animals which comprises administering to the animal an effective amount of a compound selected from the group consisting of a benzoquinolizine of the formula ##STR9## and a pharmaceutically acceptable acid addition salt thereof, wherein R 1 and R 2 each represent hydrogen, lower alkyl, lower alkoxy or halogen, R 3 represents methyl or ethyl and R 4 represents halo(lower)alkyl.
References Cited (Backward Citations)
US4076820A
Cited
GB2083029A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1987-09-25 | 1988-03-26 | 1988-09-25 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1991-09-25 | 1992-03-26 | 1992-09-25 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1995-09-25 | 1996-03-26 | 1996-09-25 | $7700.00 | Window Closed / Lapsed |