Patent US5198447A successfully refreshed from Google Patents.
US5198447A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Medicaments
Assignee: Glaxo Group Ltd
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Filing: 1991-07-16
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Granted: 1993-03-30
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Expires: 2011-07-16
Abstract
Abstract The invention relates to the use of compounds which act as antagonists of 5-hydroxytryptamine (5-HT) at 5-HT3 receptors for the relief or prevention of a withdrawal syndrome resulting from addiction to a drug or substance of abuse and/or for the suppression of dependence on drugs or substances of abuse.
Inventors
- 👤 Michael B. Tyers
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-09 20:25
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/435; A61K31/46
Claims Analysis
Total Claims: 20
Claim 1
Independent Claim
266 words
A method of treatment for the relief or prevention of a withdrawal syndrome resulting from addiction to a drug or substance of abuse and/or for the suppression of dependence on drugs or substances of abuse, which comprises administering to a human or animal subject suffering from or liable to suffer from said withdrawal syndrome and/or dependent on a drug or substance of abuse an effective amount of a compound of formula (VIII): ##STR12## wherein: L is NH or O; R 29 and R 30 are independently selected from hydrogen, halogen, CF 3 , C 1-6 alkyl, C 1-6 alkoxy, C 1-6 alkylthio, C 1-7 acyl, C 1-7 acylamino, C 1-6 alkylsulphonylamino, N-(C 1-6 alkylsulphonyl)-N-(C 1-4 alkylamino, C 1-6 alkylsulphinyl, hydroxy, nitro or amino, aminocarbonyl, aminosulphonyl, aminosulphonylamino or N-(aminosulphonyl)-C 1-4 alkylamino optionally N-substituted by one or two groups selected from C 1-6 alkyl, C 3-8 cycloalkyl, C 3-8 cycloalkylC 1-4 alkyl, phenyl or phenylC 1-4 alkyl groups or optionally N-disubstituted by C 4-5 polymethylene; D and E are independently selected from hydrogen or C 1-4 alkyl, or together are a bond; R 31 and R 32 are independently selected from hydrogen, C 1-6 alkyl, C 2-6 alkenylC 1-4 alkyl, or together are C 2-4 polymethylene; M is a group of formula (a), (b) or (c): ##STR13## wherein t is 2 or 3; u is 1 or 2; v is 1 to 3; w is 1 to 3; and R 33 or R 34 is C 1-7 alkyl, C 3-8 cycloalkyl, C 3-8 cycloalkylC 1-2 alkyl or C 2-7 alkenylC 1-4 alkenyl; or a pharmaceutically acceptable salt thereof.
Claim 2
Independent Claim
266 words
A method of treatment for the relief or prevention of a withdrawal syndrome resulting from addiction to a drug or substance of abuse and/or for the suppression of dependence on drugs or substances of abuse, which comprises administering to a human or animal subject suffering from or liable to suffer from said withdrawal syndrome and/or dependent on a drug or substance of abuse an effective amount of a compound of formula (VIII): ##STR12## wherein: L is NH or O; R 29 and R 30 are independently selected from hydrogen, halogen, CF 3 , C 1-6 alkyl, C 1-6 alkoxy, C 1-6 alkylthio, C 1-7 acyl, C 1-7 acylamino, C 1-6 alkylsulphonylamino, N-(C 1-6 alkylsulphonyl)-N-(C 1-4 alkylamino, C 1-6 alkylsulphinyl, hydroxy, nitro or amino, aminocarbonyl, aminosulphonyl, aminosulphonylamino or N-(aminosulphonyl)-C 1-4 alkylamino optionally N-substituted by one or two groups selected from C 1-6 alkyl, C 3-8 cycloalkyl, C 3-8 cycloalkylC 1-4 alkyl, phenyl or phenylC 1-4 alkyl groups or optionally N-disubstituted by C 4-5 polymethylene; D and E are independently selected from hydrogen or C 1-4 alkyl, or together are a bond; R 31 and R 32 are independently selected from hydrogen, C 1-6 alkyl, C 2-6 alkenylC 1-4 alkyl, or together are C 2-4 polymethylene; M is a group of formula (a), (b) or (c): ##STR13## wherein t is 2 or 3; u is 1 or 2; v is 1 to 3; w is 1 to 3; and R 33 or R 34 is C 1-7 alkyl, C 3-8 cycloalkyl, C 3-8 cycloalkylC 1-2 alkyl or C 2-7 alkenylC 1-4 alkenyl; or a pharmaceutically acceptable salt thereof.
Claim 3
Independent Claim
74 words
A method of treatment for the relief or prevention of a withdrawal syndrome resulting from addiction to a drug or substance of abuse and/or for the suppression of dependence on drugs or substances of abuse, which comprises administering to a human or animal subject suffering from or liable to suffer from said withdrawal syndrome and/or dependent on a drug or substance of abuse an effective amount of endo-N-(8-methyl-8-azabicyclo[3.2.1]oct-3-yl)-2,3-dihydro-3,3-dimethylindole-1-carboxamide or a pharmaceutically acceptable salt thereof.
Claim 4
Independent Claim
74 words
A method of treatment for the relief or prevention of a withdrawal syndrome resulting from addiction to a drug or substance of abuse and/or for the suppression of dependence on drugs or substances of abuse, which comprises administering to a human or animal subject suffering from or liable to suffer from said withdrawal syndrome and/or dependent on a drug or substance of abuse an effective amount of endo-N-(8-methyl-8-azabicyclo[3.2.1]oct-3-yl)-2,3-dihydro-3,3-dimethylindole-1-carboxamide or a pharmaceutically acceptable salt thereof.
Claim 5
Dependent Claim
36 words
A method according to claim 1 wherein said compound of formula (VIII) or a pharmaceutically acceptable salt thereof is administered in a unit dose of 0.05 to 1000 mg from 1 to 4 times per day.
Claim 6
Dependent Claim
17 words
A method according to claim 3 wherein the total daily dose is from 0.0001 to 50 mg/kg.
Claim 7
Dependent Claim
23 words
A method according to claim 1 wherein said compound of formula (VIII) is administered orally, buccally, parenterally, rectally or as a depot preparation.
Claim 8
Dependent Claim
16 words
A method according to claim 1 wherein said drug or substance of abuse is an opiate.
Claim 9
Dependent Claim
15 words
A method according to claim 1 wherein said drug or substance of abuse is cocaine.
Claim 10
Dependent Claim
16 words
A method according to claim 1 wherein said drug or substance of abuse is a benzodiazepine.
Claim 11
Dependent Claim
15 words
A method according to claim 1 wherein said drug or substance of abuse is alcohol.
Claim 12
Dependent Claim
15 words
A method according to claim 1 wherein said drug or substance of abuse is nicotine.
Claim 13
Dependent Claim
33 words
A method according to claim 2 wherein said compound or a pharmaceutically acceptable salt thereof is administered in a unit dose of 0.05 to 1000 mg from 1 to 4 times per day.
Claim 14
Dependent Claim
17 words
A method according to claim 11 wherein the total daily dose is from 0.0001 to 50 mg/kg.
Claim 15
Dependent Claim
20 words
A method according to claim 2 wherein said compound is administered orally, buccally, parenterally, rectally or as a depot preparation.
Claim 16
Dependent Claim
16 words
A method according to claim 2 wherein said drug or substance of abuse is an opiate.
Claim 17
Dependent Claim
15 words
A method according to claim 2 wherein said drug or substance of abuse is cocaine.
Claim 18
Dependent Claim
16 words
A method according to claim 2 wherein said drug or substance of abuse is a benzodiazepine.
Claim 19
Dependent Claim
15 words
A method according to claim 2 wherein said drug or substance of abuse is alcohol.
Claim 20
Dependent Claim
15 words
A method according to claim 2 wherein said drug or substance of abuse is nicotine.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
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| 3.5 Years (Year 4) | 1996-03-29 | 1996-09-28 | 1997-03-30 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 2000-03-29 | 2000-09-28 | 2001-03-30 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2004-03-29 | 2004-09-28 | 2005-03-30 | $7700.00 | Window Closed / Lapsed |