Method of treating mental disorders using D4 and 5-HT2A antagonists, inverse agonists or partial agonists
First Claim
1. A method for treating a disease or disorder with an underlying dysregulation of emotional functionality comprising administering to a patient a compound having (i) a 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) a 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, wherein said compound is administered to said patient in a dose ranging between 5 and 15 mg of the active ingredient.
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Abstract
The present invention relates to methods of treating of the underlying dysregulation of the emotional functionality of mental disorders (i.e. affect instability-hypersensitivity-hyperaesthesia-dissociative phenomena- . . . ) using compounds and compositions of compounds having D4 and/or 5-HT2A antagonistic, partial agonistic or inverse agonistic activity for. 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/or (ii) compounds having 5-HT2A antagonistic, partial agonistic or inverse agonistic, and/or (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.
41 Citations
63 Claims
- 1. A method for treating a disease or disorder with an underlying dysregulation of emotional functionality comprising administering to a patient a compound having (i) a 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) a 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, wherein said compound is administered to said patient in a dose ranging between 5 and 15 mg of the active ingredient.
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5. (canceled)
- 11. A method for treating a disease or disorder with an underlying dysregulation of emotional functionality comprising administering to a patient a first compound having (i) a selective affinity for the 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 a second compound having (ii) a 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.
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16. (canceled)
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37. A method for preparing a compound having a selective D4 and 5-HT2A antagonist, reverse agonist or partial agonist activity comprising the following steps:
- (a) measuring the selective affinity of a test compound to the D4 receptor and selecting a compound that has a pKi value equal to or greater than 8 towards the D4 receptor in respect to all the other D receptors, and measuring the selective efficacy of the selected compound to the D4 receptor and selecting a compounds which is a selective antagonist, inverse agonist or partial agonist of the D4 receptor;
(b) measuring the selective affinity of a test compound to the 5-HT2A receptor and selecting a compound that has a pKi value equal to or greater than 8 towards the 5-HT2A receptor in respect to all the other 5HT receptors, and measuring the selective efficacy of the selected compound to the 5-HT2A receptor and selecting a compounds which is a selective antagonist, inverse agonist or partial agonist of the 5-HT2A receptor;
(c) identifying a compound which is selected in (a) and (b), (d) preparing the compound identified in (c). - View Dependent Claims (38)
- (a) measuring the selective affinity of a test compound to the D4 receptor and selecting a compound that has a pKi value equal to or greater than 8 towards the D4 receptor in respect to all the other D receptors, and measuring the selective efficacy of the selected compound to the D4 receptor and selecting a compounds which is a selective antagonist, inverse agonist or partial agonist of the D4 receptor;
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62. A pharmaceutical composition comprising:
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(a) a compound having (i) a 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) a 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, and (b) a COX-2 inhibitor, as a combined preparation for simultaneous, separate or sequential use for treating a muscoskeletal disease or disorder.
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63. A pharmaceutical composition comprising:
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(a) a compound having a 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, (b) a compound having a 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, and (c) a COX-2 inhibitor, as a combined preparation for simultaneous, separate or sequential use for treating a muscoskeletal disease or disorder.
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Specification