METHODS FOR TREATING ANTIPSYCHOTIC-INDUCED WEIGHT GAIN

• US 20140349999A1
• Filed: 06/05/2014
• Published: 11/27/2014
• Est. Priority Date: 08/23/2010
• Status: Active Grant

• Current Assignee: Alkermes Pharma Ireland Limited (Alkermes plc)
• Original Assignee: Alkermes Pharma Ireland Limited (Alkermes plc)
• Inventors: Deaver, Daniel, Todtenkopf, Mark
• Granted Patent: US 9,126,977 B2
• Time in Patent Office: Days
• US Class Current: 514/211.13
• CPC Class Codes: A61K 31/439 the ring forming part of a bridged ring system, e.g. quinuclidine 8-azabicyclo [3.2.1] octanes A61K31/46
• CPC Class Codes: A61K 31/485 Morphinan derivatives, e.g. morphine, codeine
• CPC Class Codes: A61K 31/496 Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
• CPC Class Codes: A61K 31/519 ortho- or peri-condensed with heterocyclic rings
• CPC Class Codes: A61K 31/551 having two nitrogen atoms, e.g. dilazep
• CPC Class Codes: A61K 31/5513 1,4-Benzodiazepines, e.g. diazepam or clozapine
• CPC Class Codes: A61K 31/554 having at least one nitrogen and one sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
• CPC Class Codes: A61K 9/20 Pills, tablets, discs, rods A61K9/0004, A61K9/0007, A61K9/0056, A61K9/0065 take precedence; for reconstitution of a drink A61K9/0095
• CPC Class Codes: A61P 3/04 Anorexiants; Antiobesity agents
• CPC Class Codes: C07D 221/28 Morphinans
• CPC Class Codes: C07D 405/06 linked by a carbon chain containing only aliphatic carbon atoms

Abstract

The present invention relates to the discovery of a novel opioid modulator effective in reducing pharmacologically induced weight gain associated with atypical antipsychotic use. The present invention provides methods of reducing antipsychotic induced weight gain, methods for suppressing food intake and reducing ghrelin levels induced by atypical antipsychotic medications in a patient.

Claims

1. A method of reducing antipsychotic induced weight gain comprising administering to the patient in need of treatment an effective amount of a compound of Formula I;

2. The method of claim 1, wherein said compound of Formula I is selected from a compound of Formula II:

6. The method according to claim 1, wherein said compound of Formula I is selected from Table A:

7. The method according to claim 1, wherein the weight gain is induced by administration of an atypical antipsychotic.

8. The method according to claim 1, wherein said compound is Compound 1:

9. The method of claim 7, wherein the atypical antipsychotic is selected from the group consisting of olanzapine, clozapine, risperidone, quetiapine, aripiprazole, ziprasidone, and pharmaceutically acceptable salts thereof.

10. The method of claim 9, wherein the atypical antipsychotic is used in the treatment of schizophrenia, bipolar disorder, dementia, acute mania, major depression and psychotic agitation.

3-5. -5. (canceled)

11-27. -27. (canceled)

28. A method of reducing Ghrelin level in the gastrointestinal tract comprising the step of administering a compound of Formula I to a patient in need thereof.

29. The method according to claim 28, wherein said compound of Formula I is Compound 1.

30. A composition comprising an atypical antipsychotic and a compound of Formula I;

31. The composition of claim 30, wherein said atypical antipsychotic is selected from olanzapine, clozapine, risperidone, quetiapine, aripiprazole, and ziprasidone.

32. The composition of claim 30, wherein said compound of Formula I is selected from Table A: