Patent US4381302A successfully refreshed from Google Patents.
US4381302A
Expired / Lapsed
US
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(6aα,10aα,11aα)-2-(2-Pyridinyl)-1,3,4,6,6a,7,8,9,10,10a,11,11a-dodecahydro-2H-pyrazino]1,2-b]isoquinoline and derivatives
Assignee: Merck and Co Inc
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Filing: 1981-05-26
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Granted: 1983-04-26
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Expires: 2001-05-26
Abstract
Abstract (6a alpha ,10a alpha ,11a alpha )-2-(2-pyridinyl)-1,3,4,6,6a,7,8,9,10,10a,11,11a-dodecahydro-2H-pyrazi no[1,2-b]isoquinoline and derivatives or acid addition salts thereof are selective alpha 2-adrenergic receptor antagonists and thereby useful as antidepressant agents and for treating sedation caused by antihypertensive therapy.
Inventors
- 👤 Joel R. Huff
- 👤 Stella W. King
- 👤 Walfred S. Saari
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-28 10:03
CPC Classifications
C; C07; C07D; C07D471/00; C07D471/02; C07D471/04; C07D217/00; C07D217/22; C07D217/26
Claims Analysis
Total Claims: 12
Claim 1
Independent Claim
60 words
A method of selectively antagonizing α 2 -adrenergic receptors in a patient in need of such treatment which comprises the administration of an effective amount of a compound of structural formula: ##STR4## or a pharmaceutically acceptable salt thereof wherein R is (1) hydrogen, (2) halo, (3) C 1-4 alkyl, (4) cyano, (5) C 1-4 alkoxy, (6) trifluoromethyl, or (7) nitro.
Claim 2
Independent Claim
60 words
A method of selectively antagonizing α 2 -adrenergic receptors in a patient in need of such treatment which comprises the administration of an effective amount of a compound of structural formula: ##STR4## or a pharmaceutically acceptable salt thereof wherein R is (1) hydrogen, (2) halo, (3) C 1-4 alkyl, (4) cyano, (5) C 1-4 alkoxy, (6) trifluoromethyl, or (7) nitro.
Claim 3
Dependent Claim
16 words
The method of claim 1 wherein R is hydrogen, fluoro, methyl, cyano, methoxy, trifluoromethyl or nitro.
Claim 4
Dependent Claim
11 words
The method of claim 2 wherein R is hydrogen or fluoro.
Claim 5
Dependent Claim
34 words
A compound of structural formula: ##STR5## or a pharmaceutically acceptable salt thereof, wherein R is (1) hydrogen, (2) halo, (3) C 1-4 alkyl, (4) cyano, (5) C 1-4 alkoxy, (6) trifluoromethyl, or (7) nitro.
Claim 6
Dependent Claim
34 words
A compound of structural formula: ##STR5## or a pharmaceutically acceptable salt thereof, wherein R is (1) hydrogen, (2) halo, (3) C 1-4 alkyl, (4) cyano, (5) C 1-4 alkoxy, (6) trifluoromethyl, or (7) nitro.
Claim 7
Dependent Claim
16 words
The compound of claim 4, wherein R is hydrogen, fluoro, methyl, cyano, methoxy, trifluoromethyl or nitro.
Claim 8
Dependent Claim
11 words
The compound of claim 5, wherein R is hydrogen or fluoro.
Claim 9
Dependent Claim
60 words
A selective α 2 -adrenergic receptor antagonist pharmaceutical composition consisting essentially of a pharmaceutically acceptable carrier and an effective α 2 -adrenergic receptor antagonist amount of a compound of structural formula: ##STR6## or a pharmaceutically acceptable salt thereof wherein R is (1) hydrogen, (2) halo, (3) C 1-4 alkyl, (4) cyano, (5) C 1-4 alkoxy, (6) trifluoromethyl, or (7) nitro.
Claim 10
Dependent Claim
60 words
A selective α 2 -adrenergic receptor antagonist pharmaceutical composition consisting essentially of a pharmaceutically acceptable carrier and an effective α 2 -adrenergic receptor antagonist amount of a compound of structural formula: ##STR6## or a pharmaceutically acceptable salt thereof wherein R is (1) hydrogen, (2) halo, (3) C 1-4 alkyl, (4) cyano, (5) C 1-4 alkoxy, (6) trifluoromethyl, or (7) nitro.
Claim 11
Dependent Claim
17 words
The pharmaceutical composition of claim 7 wherein R is hydrogen, fluoro, methyl, cyano, methoxy, trifluoromethyl or nitro.
Claim 12
Dependent Claim
12 words
The pharmaceutical composition of claim 8 wherein R is hydrogen or fluoro.
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) | 1986-04-25 | 1986-10-25 | 1987-04-26 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1990-04-25 | 1990-10-25 | 1991-04-26 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1994-04-25 | 1994-10-25 | 1995-04-26 | $7700.00 | Window Closed / Lapsed |