US4908370A
Expired / Lapsed
US
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Anxiolytic-n-(1-azabicyclo(2.2.2)oct-3-yl) benzamides and thiobenzamides
Assignee: AH Robins Co Inc
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Filing: 1987-12-15
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Granted: 1990-03-13
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Expires: 2007-12-15
Abstract
Abstract Compounds of general formula I: ##STR1## wherein: X represents oxygen or sulphur; R 1 represents loweralkyl; R 2 represents hydrogen, halo, 4,5-benzo, loweralkoxy, amino, methylamino or dimethylamino; R 3 represents hydrogen or loweralkyl; and n is 1 or 2 and their pharmaceutically acceptable acid addition salts have anxiolytic activity. In particular, they have activity against anxiety induced by the withdrawal from ingested substances such as narcotics (e.g. cocaine), alcohol and nicotine.
Inventors
- 👤 Robert J. Naylor
- 👤 Brenda Naylor
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-09 20:18
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/435; A61K31/44; A61K31/445; C; C07; C07D; C07D453/00; C07D453/02
Claims Analysis
Total Claims: 17
Claim 1
Independent Claim
75 words
A method for the treatment or prophylaxis of anxiety comprising the administration to a warm-blooded animal requiring such treatment or prophylaxis of an anxiolytically effective amount of a compound of general formula I: ##STR10## wherein: X represents oxygen or sulphur; R 1 represents loweralkyl; R 2 represents hydrogen, halo, 4,5-benzo, loweralkoxy, amino, methylamino or dimethylamino; R 3 represents hydrogen or loweralkyl; and n is 1 or 2 or a pharmaceutically acceptable acid addition salt thereof.
Claim 2
Independent Claim
75 words
A method for the treatment or prophylaxis of anxiety comprising the administration to a warm-blooded animal requiring such treatment or prophylaxis of an anxiolytically effective amount of a compound of general formula I: ##STR10## wherein: X represents oxygen or sulphur; R 1 represents loweralkyl; R 2 represents hydrogen, halo, 4,5-benzo, loweralkoxy, amino, methylamino or dimethylamino; R 3 represents hydrogen or loweralkyl; and n is 1 or 2 or a pharmaceutically acceptable acid addition salt thereof.
Claim 3
Dependent Claim
18 words
A method as claimed in claim 1, wherein said anxiety is induced by withdrawal from an ingested substance.
Claim 4
Dependent Claim
24 words
A method as claimed in claim 2, wherein said ingested substance is selected from the class consisting of alcohol, narcotics, nicotine and mixtures thereof.
Claim 5
Dependent Claim
13 words
A method as claimed in claim 2 wherein said ingested substance is cocaine.
Claim 6
Dependent Claim
21 words
A method as claimed in claim 1, wherein, in general formula I, R 2 represents a 3- or 5- halo substituent.
Claim 7
Dependent Claim
21 words
A method as claimed in claim 1 wherein, in general formula I, R 2 represents a 4-amino, 4-methylamino or 4-dimethylamino substituent.
Claim 8
Dependent Claim
15 words
A method as claimed in claim 1, wherein, in general formula I, X represents oxygen.
Claim 9
Dependent Claim
18 words
A method as claimed in claim 1, wherein said compound is 4-amino-N-(1-azabicyclo[2.2.2]oct-3-yl)-5-chloro-2-methoxybenzamide, or a pharmaceutically acceptable salt thereof.
Claim 10
Dependent Claim
18 words
A method as claimed in claim 1, wherein said compound is N-(1-azabicyclo[2.2.2]oct-3-yl)-5-chloro-2-methoxy-4-methylaminobenzamide, or a pharmaceutically acceptable salt thereof.
Claim 11
Dependent Claim
18 words
A method as claimed in claim 1, wherein said compound is N-(1-azabicyclo[2.2.2]oct-3-yl)-2-methoxybenzamide, or a pharmaceutically acceptable salt thereof.
Claim 12
Dependent Claim
18 words
A method as claimed in claim 1, wherein said compound is N-(1-azabicyclo[2.2.2]oct-3-yl)-2,4-di-methoxybenzamide, or a pharmaceutically acceptable salt thereof.
Claim 13
Dependent Claim
18 words
A method as claimed in claim 1, wherein said compound is N-(1-azabicyclo[2.2.2]oct-3-yl)-2-propoxybenzamide, or a pharmaceutically acceptable salt thereof.
Claim 14
Dependent Claim
18 words
A method as claimed in claim 1, wherein said compound is 4-amino-N-(1-azabicyclo[2.2.2]oct-3-yl)-5-chloro-2-methoxybenzamide, or a pharmaceutically acceptable salt thereof.
Claim 15
Dependent Claim
18 words
A method as claimed in claim 1, wherein said compound is N-(1-azabicyclo[2.2.2]oct-3-yl)-5-chloro-2-methoxy-4-methylaminobenzamide, or a pharmaceutically acceptable salt thereof.
Claim 16
Dependent Claim
18 words
A method as claimed in claim 1, wherein said compound is N-(1-azabicyclo[2.2.2]oct-3-yl)-3-methoxy-2-naphthalenecarboximide, or a pharmaceutically acceptable salt thereof.
Claim 17
Dependent Claim
18 words
A method as claimed in claim 1, wherein said compound is 4-amino-N-(1-aza-2-methyl-bicyclo[2.2.2]-oct-3-yl)-5-chloro-2-methoxybenzamide, or a pharmaceutically acceptable salt thereof.
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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) | 1993-03-12 | 1993-09-11 | 1994-03-13 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1997-03-12 | 1997-09-11 | 1998-03-13 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2001-03-12 | 2001-09-11 | 2002-03-13 | $7700.00 | Window Closed / Lapsed |