US4376772A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Use of piperazinyl-imidazo[1,2-a]pyrazines in sedation
Assignee: Merck and Co Inc
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Filing: 1981-12-09
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Granted: 1983-03-15
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Expires: 2001-12-09
Abstract
Abstract Piperazinyl-imidazo[1,2-a]pyrazines and their acid addition salts are selective alpha 2-adrenergic receptor antagonists and are thereby useful for treating sedation caused by antihypertensive drug therapy.
Inventors
- 👤 Walfred S. Saari
- 👤 Joel R. Huff
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-27 23:14
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/495
Claims Analysis
Total Claims: 9
Claim 1
Independent Claim
69 words
A method of treating sedation caused by antihypertensive drug therapy through stimulation of presynaptic α 2 -adrenergic receptors in a patient in need of such treatment which comprises the administration of 0.01-20 mg/kg/day of a compound of structural formula: ##STR5## or a pharmaceutically acceptable salt thereof, wherein R 1 , R 2 and R 3 are independently hydrogen or halogen; and R 4 is hydrogen or C 1-3 alkyl.
Claim 2
Independent Claim
69 words
A method of treating sedation caused by antihypertensive drug therapy through stimulation of presynaptic α 2 -adrenergic receptors in a patient in need of such treatment which comprises the administration of 0.01-20 mg/kg/day of a compound of structural formula: ##STR5## or a pharmaceutically acceptable salt thereof, wherein R 1 , R 2 and R 3 are independently hydrogen or halogen; and R 4 is hydrogen or C 1-3 alkyl.
Claim 3
Dependent Claim
12 words
The method of claim 1, wherein R 4 is hydrogen or methyl.
Claim 4
Dependent Claim
10 words
The method of claim 1, wherein the compound is 8-(1-piperazinyl)imidazo[1,2-a]pyrazine.
Claim 5
Dependent Claim
83 words
A pharmaceutical composition for treating hypertension and sedation caused thereby which comprises a pharmaceutical carrier, an effective amount of an antihypertensive agent known to cause sedation through stimulation of presynaptic α 2 -adrenergic receptors and an amount of a compound to provide a dosage of 0.01-20 mg/kg/day wherein the compounds has structural formula: ##STR6## or a pharmaceutically acceptable salt thereof, wherein R 1 , R 2 and R 3 are independently hydrogen or halogen; and R 4 is hydrogen or C 1-3 alkyl.
Claim 6
Dependent Claim
83 words
A pharmaceutical composition for treating hypertension and sedation caused thereby which comprises a pharmaceutical carrier, an effective amount of an antihypertensive agent known to cause sedation through stimulation of presynaptic α 2 -adrenergic receptors and an amount of a compound to provide a dosage of 0.01-20 mg/kg/day wherein the compounds has structural formula: ##STR6## or a pharmaceutically acceptable salt thereof, wherein R 1 , R 2 and R 3 are independently hydrogen or halogen; and R 4 is hydrogen or C 1-3 alkyl.
Claim 7
Dependent Claim
12 words
The formulation of claim 4, wherein R 4 is hydrogen or methyl.
Claim 8
Dependent Claim
11 words
The formulation of claim 4, wherein the antisedative compound is 8-(1-piperazinyl)imidazo[1,2-a]pyrazine.
Claim 9
Dependent Claim
14 words
The formulation of claims 4, 5 or 6 wherein the antihypertensive agent is methyldopa.
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) | 1986-03-14 | 1986-09-13 | 1987-03-15 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1990-03-14 | 1990-09-13 | 1991-03-15 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1994-03-14 | 1994-09-13 | 1995-03-15 | $7700.00 | Window Closed / Lapsed |