Use of diphenylbutyl-piperazinecarboxamides in the treatment of substance disorders

• US 5,434,156 A
• Filed: 10/12/1993
• Issued: 07/18/1995
• Est. Priority Date: 03/22/1991
• Status: Expired due to Fees

• Current Assignee: Biovitrum AB (Swedish Orphan Biovitrum AB (publ))
• Original Assignee: Pharmacia AB (Pharmacia Corp.)
• Inventors: Bjork, Anders, Christensson, Erik
• Primary Examiner(s): HENLEY III, RAYMOND J
• Application Number:
  US07/949,869
• Time in Patent Office: 644 Days
• Field of Search: 514/255, 514/810, 514/811, 514/812, 514/813
• US Class Current: 514/255.01
• CPC Class Codes: A61K 31/495 having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazinesA61K31/48 takes precedence ; with three nitrogen atoms A61K31/53
• CPC Class Codes: A61P 25/30 for treating abuse or dependence
• CPC Class Codes: A61P 25/32 Alcohol-abuse
• CPC Class Codes: A61P 39/02 Antidotes
• CPC Class Codes: C07D 295/215 Radicals derived from nitrogen analogues of carbonic acid

Abstract

The present invention relates to the relief or prevention of withdrawal syndrome resulting from addiction to alcohol and/or the suppression of dependence on alcohol by administering to a person in need thereof, an effective amount certain diphenylbutyl-piperazine-carboxamides including 4-[4,4-bis(4-fluorophenyl)butyl]-N-ethyl-1-piperazine-carboxamide which is also known as amperozide.

Claims

1. A method for the relief or prevention of a withdrawal syndrome resulting from addiction to alcohol and/or for the suppression of dependence on alcohol which comprises administering an effective amount of a diphenylbutyl-piperazinecarboxamide of the formula ##STR2## wherein R₁ and R₂ are groups independently selected from the group of H, alkyl chains, straight or branched, with 1-10 carbon atoms, cycloalkyl with 3-8 carbon atoms, aralkyl with 7-9 carbon atoms, alkenyl with 2-10 carbon atoms, phenyl unsubstituted or substituted by one to three groups selected from halogen, lower alkyl with 1-5 carbon atoms, lower alkoxy with with 1-5 carbon atoms, amine unsubstituted or substituted by one or two lower alkyl groups with 1-5 carbon atoms, --CF₃ and --CN groups,

R₃, R₄, R₅ and R₆ are groups independently selected from H, lower alkyl having from 1-3 carbon atoms and phenyl,

R₇ is selected from hydrogen, halogen lower alkoxy with 1-3 carbon atoms and --CF₃, and

X is O or S,

or a physiologically acceptable salt thereof.

2. A method according to claim 1 wherein

R₁ is methyl, ethyl or n-, iso- or cyclopropyl,

R₂ is H,

R₃, R₄, R₅ and R₆ are hydrogen or R₃ and R₆ are hydrogen and R₄ and R₅ are methyl, or R₄ and R₅ are hydrogen and R₃ and R₆ are methyl,

R₇ is hydrogen or halogen, and

X is O.

3. A method according to claim 2, wherein the diphenylbutylpiperazinecarboxamide is 4-[4,4-bis(4-fluorophenyl)butyl]-N-ethyl-1-piperazinecarboxamide or a physiologically acceptable salt thereof.

4. A method according to claim 3, wherein the diphenylbutylpiperazinecarboxamide is administered in a daily dose of from 0.1 to 40 mg.