US4442103A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Treating sedation with 1-(3-substituted-2-pyridinyl) piperazines
Assignee: Merck and Co Inc
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Filing: 1982-09-30
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Granted: 1984-04-10
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Expires: 2002-09-30
Abstract
Abstract 1-(3-Substituted-2-pyridinyl)piperazines and their acid addition salts are selective alpha 2-adrenergic receptor antagonists and thereby useful as antidepressant agents and for treating sedation caused by antihypertensive therapy.
Inventors
- 👤 Walfred S. Saari
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-28 23:23
CPC Classifications
C; C07; C07D; C07D213/00; C07D213/02; C07D213/04; C07D213/60; C07D213/72; C07D213/74; A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/495
Claims Analysis
Total Claims: 6
Claim 1
Independent Claim
97 words
A method of treating sedation caused by presynaptic α 2 -adrenergic receptor stimulation by antihypertensive drug therapy in a patient in need of such treatment which comprises the administration of 0.01 to 20 mg/kg/day 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; and R 1 is (1) hydrogen, or (2) C 1-3 alkyl; with the proviso that if R is fluoro, chloro or bromo, R 1 is C 1-3 alkyl.
Claim 2
Independent Claim
97 words
A method of treating sedation caused by presynaptic α 2 -adrenergic receptor stimulation by antihypertensive drug therapy in a patient in need of such treatment which comprises the administration of 0.01 to 20 mg/kg/day 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; and R 1 is (1) hydrogen, or (2) C 1-3 alkyl; with the proviso that if R is fluoro, chloro or bromo, R 1 is C 1-3 alkyl.
Claim 3
Dependent Claim
22 words
The method of claim 1, wherein R is hydrogen, halo, methyl, cyano, nitro or trifluoromethyl; and R 1 is hydrogen or methyl.
Claim 4
Dependent Claim
103 words
A pharmaceutical composition for treating sedation caused by presynaptic α 2 -adrenergic receptor stimulation by antihypertensive drug therapy which comprises a pharmaceutical carrier, an effective amount of a presynaptic α 2 -adrenergic receptor stimulating antihypertensive agent and an effective amount of 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; and R 1 is (1) hydrogen, or (2) C 1-3 alkyl; with the proviso that if R is fluoro, chloro or bromo, R 1 is C 1-3 alkyl.
Claim 5
Dependent Claim
103 words
A pharmaceutical composition for treating sedation caused by presynaptic α 2 -adrenergic receptor stimulation by antihypertensive drug therapy which comprises a pharmaceutical carrier, an effective amount of a presynaptic α 2 -adrenergic receptor stimulating antihypertensive agent and an effective amount of 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; and R 1 is (1) hydrogen, or (2) C 1-3 alkyl; with the proviso that if R is fluoro, chloro or bromo, R 1 is C 1-3 alkyl.
Claim 6
Dependent Claim
22 words
The composition of claim 3, wherein R is hydrogen, halo, methyl, cyano, nitro or trifluoromethyl; and R 1 is hydrogen or methyl.
References Cited (Backward Citations)
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1987-04-10 | 1987-10-10 | 1988-04-10 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1991-04-10 | 1991-10-10 | 1992-04-10 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1995-04-10 | 1995-10-10 | 1996-04-10 | $7700.00 | Window Closed / Lapsed |