Method of treating neurodegenerative diseases using D4 and 5-HT2A antagonists, inverse agonists or partial agonists
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Abstract
The present invention relates to methods of treating neurodegenerative diseases or disorders, such as Parkinson disease and related cognitive diseases or disorders with compounds and compositions of compounds having D4 and/or 5-HT2A antagonistic, partial agonistic or inverse agonistic activity in combination with other compounds for treating said diseases. The invention also relates to pharmaceutical compositions for administration to a patient diagnosed as having a neurodegenerative disease or disorder and/or a cognitive disease or disorder, said 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 or compositions of said compounds in combination with another compound for treating said diseases or disorders to augment the therapeutic effect or to provide a faster onset of the therapeutic effect of said other compound.
65 Citations
91 Claims
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1-40. -40. (canceled)
- 41. A method for treating neurodegenerative diseases or disorders comprising administering to a patient a first 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, comprising administering said compound simultaneously with, separate from or prior to administering a second compound to the patient to augment the therapeutic effect or to provide a faster onset of the therapeutic effect of said second compound.
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49. 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 dopamine receptor agonist, as a combined preparation for simultaneous, separate or sequential use for treating a neurodegenerative disease or disorder such as Parkinson Disease. - View Dependent Claims (88)
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50. A pharmaceutical composition comprising:
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(a) pipamperone in a dose ranging between 5 to 15 mg of the active ingredient, and (b) pergolide in a dose ranging between 0.5 and 10 mg of the active ingredient, as a combined preparation for simultaneous, separate or sequential use for treating a neurodegenerative disease or disorder such as Parkinson Disease.
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54. 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 levodopa associated with a decarboxylase inhibitor, as a combined preparation for simultaneous, separate or sequential use for treating a neurodegenerative disease or disorder such as Parkinson Disease. - View Dependent Claims (89)
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55. A pharmaceutical composition comprising:
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(a) pipamperone in a dose ranging between 5 and 15 mg of the active ingredient, and (b) levodopa/carbidopa in a dose ranging between 2000 mg/200 mg and 100 mg/10 mg of the active ingredients, as a combined preparation for simultaneous, separate or sequential use for treating a neurodegenerative disease or disorder such as Parkinson Disease.
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59. 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 mono-amine oxidase B (MAO-B) inhibitor, as a combined preparation for simultaneous, separate or sequential use for treating a neurodegenerative disease or disorder such as Parkinson Disease. - View Dependent Claims (90)
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60. A pharmaceutical composition comprising:
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(a) pipamperone in a dose ranging between 5 and 15 mg of the active ingredient, and (b) selegilinehydrochloride is administered in a dose ranging between 2 and 25 mg of the active ingredient, as a combined preparation for simultaneous, separate or sequential use for treating a neurodegenerative disease or disorder such as Parkinson Disease.
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- 61. A method for treating a neurodegenerative disease or disorder comprising administering to a patient (a) a first compound having 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, (b) a second 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 third compound, wherein said first and second compounds are administered simultaneously with, separate from or prior to administering said third compound to the patient to augment the therapeutic effect or to provide a faster onset of the therapeutic effect of said third compound.
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68. 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 dopamine receptor agonist, as a combined preparation for simultaneous, separate or sequential use for treating a neurodegenerative disease or disorder such as Parkinson Disease.
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72. 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) levodopa associated with a decarboxylase inhibitor, as a combined preparation for simultaneous, separate or sequential use for treating a neurodegenerative disease or disorder such as Parkinson Disease.
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76. 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 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 mono-amine oxidase B (MAO-B) inhibitor, as a combined preparation for simultaneous, separate or sequential use for treating a neurodegenerative disease or disorder such as Parkinson Disease.
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Specification