← Back to Patent Explorer
US5198447A Expired / Lapsed US ⏱️ 0.0 years remaining

Medicaments

Assignee: Glaxo Group Ltd
•
Filing: 1991-07-16
•
Granted: 1993-03-30
•
Expires: 2011-07-16
📄 Original PDF 🌐 Google Patents 🔄 Sync Now

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 19:48
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.

References Cited (Backward Citations)

GB2125398A Cited
EP0189002A2 Cited
US4883803A Cited
US4808581A Cited
GB2193633A Cited
US4847281A Cited
US4908370A Cited
US4973594A Cited
US4985437A Cited
GB2206788A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
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

Assigned Categories & Tags

No categories assigned to this patent yet.

Assign Category Tag