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

• US 20110207776A1
• Filed: 03/25/2011
• Published: 08/25/2011
• Est. Priority Date: 12/02/2003
• Status: Abandoned Application

• Current Assignee: Erik Buntinx
• Original Assignee: Erik Buntinx
• Inventors: Buntinx, Erik
• Application Number:
  US13/065,638
• Publication Number:
  US 20110207776A1
• Time in Patent Office: Days
• US Class Current: 514/316
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/343 condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
• CPC Class Codes: A61K 31/4545 containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system
• CPC Class Codes: A61P 25/16 Anti-Parkinson drugs
• CPC Class Codes: A61P 25/18 Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
• CPC Class Codes: A61P 25/22 Anxiolytics
• CPC Class Codes: A61P 25/24 Antidepressants
• CPC Class Codes: A61P 25/28 for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia

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.

Claims

1-81. -81. (canceled)

82. A pharmaceutical composition for treating a psychotic disorder comprising:

(a) pipamperone,

(b) a D2 receptor antagonist,

and a pharmaceutically acceptable carrier,

wherein the composition provides a daily dose of 5-15 mg pipamperone.

83. The pharmaceutical composition of claim 82 for treating schizophrenia.

84. The pharmaceutical composition of claim 82, wherein the composition provides a daily dose of 5 mg pipamperone.

85. The pharmaceutical composition of claim 83, wherein the composition provides a daily dose of 5 mg pipamperone.

86. The pharmaceutical composition of claim 82, wherein the composition provides a daily dose of 10 mg pipamperone.

87. The pharmaceutical composition of claim 83, wherein the composition provides a daily dose of 10 mg pipamperone.

88. The pharmaceutical composition of claim 82, wherein the composition provides a daily dose of 15 mg pipamperone.

89. The pharmaceutical composition of claim 83, wherein the composition provides a daily dose of 15 mg pipamperone.

90. The pharmaceutical composition of claim 82, wherein pipamperone is in the form of a pharmaceutically acceptable salt.

91. The pharmaceutical composition of claim 83, wherein pipamperone is in the form of a pharmaceutically acceptable salt.

92. The pharmaceutical composition of claim 82, wherein said D2 receptor antagonist is in the form of a pharmaceutically acceptable salt.

93. The pharmaceutical composition of claim 83, wherein said D2 receptor antagonist is in the form of a pharmaceutically acceptable salt.

94. A pharmaceutical composition comprising:

(a) 5-15 mg pipamperone,

(b) a D2 receptor antagonist,

and a pharmaceutically acceptable carrier.

95. The pharmaceutical composition of claim 94, wherein pipamperone

and said D2 receptor antagonist are present in an amount effective to treat a psychotic disorder.

96. The pharmaceutical composition of claim 94, wherein pipamperone and said D2 receptor antagonist are present in an amount effective to treat schizophrenia.

97. The pharmaceutical composition of claim 94, wherein pipamperone is present in a dose of 5 mg.

98. The pharmaceutical composition of claim 94, wherein pipamperone is present in a dose of 10 mg.

99. The pharmaceutical composition of claim 94, wherein pipamperone is present in a dose of 15 mg.

100. The pharmaceutical composition of claim 94, wherein pipamperone is in the form of a pharmaceutically acceptable salt.

101. The pharmaceutical composition of claim 94, wherein said D2 receptor antagonist is in the form of a pharmaceutically acceptable salt.