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Use of D4 and 5-HT2A antagonists, inverse agonists or partial agonists

a technology of inverse agonists and antagonists, applied in the field of neuropsychiatry, can solve the problems of inability to achieve remission and inadequate early treatment, and achieve the effect of accelerating accelerating the onset of the therapeutic effect of said second compound

Inactive Publication Date: 2011-08-25
BUNTINX ERIK
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The present invention relates to the use of compounds with specific activity against the D4 and 5-HT2A receptors for the treatment of mental disorders with emotion dysregulation. The compounds have high selectivity for these receptors and can be administered in a pharmaceutical composition. The invention also includes the use of a combination of two compounds with different modes of action to enhance the therapeutic effect. The compounds can be used to treat a variety of mental disorders such as anxiety, eating disorders, premenstrual syndrome, somatoform disorders, and more. The invention also provides a method for preparing the compounds with selective activity against the D4 and 5-HT2A receptors.

Problems solved by technology

Clinical causes of not attaining remission by the Current Psychopharmacological Compounds are inadequate early treatment, underlying emotion dysregulation (affecting instability-hypersensitivity-hyperaesthesia-dissociative phenomena, etc.) and competitive antagonism.

Method used

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  • Use of D4 and 5-HT2A antagonists, inverse agonists or partial agonists
  • Use of D4 and 5-HT2A antagonists, inverse agonists or partial agonists
  • Use of D4 and 5-HT2A antagonists, inverse agonists or partial agonists

Examples

Experimental program
Comparison scheme
Effect test

example 1

Measuring pKi Values of Test Compounds

[0682]In Table 1, the pKi values of test compounds are given for each of the dopamine receptors, 5HT receptors, adrenergic receptors and the histamine1 receptor. The affinity of test compounds for the respective receptors has been performed according to conventional procedures known in the art.

[0683]An indication “0” means that no affinity has been measured between the test compound and the receptor.

[0684]The columns displaying the pKi values for the D4 and the 5-HT2A receptor are filled with dark grey. pKi values between 8 and 9 and higher than 9 are represented by light grey boxes.

example 2

Foregoing Pipamperon-Citalopram Treatment in Major Depressive Disorder: a Placebo and Active Controlled Period Finding Clinical Trial

[0685]Table 2 represents the set-up of a clinical trial comprising for treatment groups:

[0686]Group Plc—Active / Day 0 represents the group receiving 10 mg citalopram, twice a day, starting the first day (Day 0) of active treatment in the clinical trial. This administration regime is also indicated as the mono therapy.

[0687]Group Pip—Active / Day 0 represents the group receiving a combination of 4 mg pipamperon and 10 mg citalopram, twice a day, starting the first day (Day 0) of active treatment in the clinical trial. This administration regime is also indicated as the non-foregoing combo therapy.

[0688]Group Pip—Active / Day 4 represents the group receiving 4 mg pipamperon, twice a day, starting the first day (Day 0) of active treatment in the clinical trial, followed by a combination of 4 mg pipamperon and 10 mg citalopram, twice a day, starting the fifth (...

example 3

Combo Pipamperon-Citalopram: Therapeutic Use in Major Depression

Purpose

[0705]Pipamperon (1′-[3-(p-Fluorobenzoyl)propyl]-[1,4′-bipiperidine]-4′-carboxamide), the active ingredient of Dipiperon (Janssen-Cilag B.V), administered to patients in a dose ranging between 8 and 12 mg is claimed via its specific pharmacological properties to be a booster of the antidepressant effect of the selective serotonin re-uptake inhibitor citalopram. Preferably, pipamperon is administered daily at least 4-5 days before administering said antidepressant. The mechanism of boosting of pipamperon has to deal with (i) the selective affinity for the dopamine-4 (D4) receptor with a pKi value equal to or higher than 8 towards the D4 receptor and less than 8 towards other dopamine receptors, and (ii) the selective affinity for the 5-HT2A receptor with a pKi value equal to or higher than 8 towards the 5-HT2A receptor and less than 8 towards other 5HT receptors. This semi-naturalistic open label study investigate...

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Abstract

The present invention relates to the use of compounds and compositions of compounds having D4 and 5-HT2A antagonistic, partial agonistic or inverse agonistic activity for the treatment of the underlying dysregulation of the emotional functionality of mental disorders (i.e. affect instability—hypersensitivity—hyperaesthesia—dissociative phenomena—etc). The invention also relates to methods comprising administering to a patient diagnosed as having a neuropsychiatric disorder a pharmaceutical composition containing (i) compounds having D4 antagonistic, partial agonistic or inverse agonistic activity and (ii) compounds having 5-HT2A antagonistic, partial agonistic or inverse agonistic, and (iii) any known medicinal compound and compositions of said compounds. The combined D4 and 5-HT2A antagonistic, partial agonistic or inverse agonistic effects may reside within the same chemical or biological compound or in two different chemical and / or biological compounds.

Description

CROSS REFERENCE TO RELATED APPLICATIONS[0001]This application is a continuation of U.S. patent application Ser. No. 10 / 580,962, filed on May 31, 2006, which is a national stage entry under 35 U.S.C. §371 of PCT International Application No. PCT / BE2004 / 000172, filed Dec. 2, 2004, and claims priority of U.S. patent application Ser. No. 10 / 725,965, filed Dec. 2, 2003, now U.S. Pat. No. 7,884,096, Canadian Patent Application No. 2,451,798, filed Dec. 2, 2003, European Patent Application No. 03447279.5, filed Dec. 2, 2003, European Patent Application No. 04447001.1, filed Jan. 5, 2004, U.S. patent application Ser. No. 10 / 752,423, filed Jan. 6, 2004, now U.S. Pat. No. 7,855,195, European Patent Application No. 04447066.4, filed Mar. 18, 2004, U.S. patent application Ser. No. 10 / 803,793, filed Mar. 18, 2004, Canadian Patent Application No. 2,461,248, filed Mar. 18, 2004, European Patent Application No. 04025035.9, filed Oct. 21, 2004, Japanese Patent Application No. 2004-349085, filed Nov....

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/4545A61P25/18A61K31/00A61K31/343G01N33/48
CPCA61K31/343A61K31/4545A61K2300/00A61P25/00A61P25/16A61P25/18A61P25/22A61P25/24A61P25/28
Inventor BUNTINX, ERIK
Owner BUNTINX ERIK
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