# US 9,517,235 B2 · Methods for treating antipsychotic-induced weight gain

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- Number: US 9,517,235 B2
- Document ID: US9517235B2
- Status: Granted
- Kind: B2
- Application number: 14/813,260
- Filed: 2015-07-30
- Published: 2016-02-25
- Granted: 2016-12-13
- Earliest claimed: 2010-08-23
- Assignees: Alkermes Pharma Ireland Limited
- Applicants: Alkermes Pharma Ireland Limited
- Inventors: Daniel Deaver; Mark Todtenkopf
- Web page: https://patentgrep.com/patent/US9517235B2

## CPC

- A61K 31/485: Morphinan derivatives, e.g. morphine, codeine
- A61K 9/20: Pills, tablets, {discs, rods (A61K9/0004, A61K9/0007, A61K9/0056, A61K9/0065 take precedence; for reconstitution of a drink A61K9/0095)}
- A61K 31/439: the ring forming part of a bridged ring system, e.g. quinuclidine (8-azabicyclo [3.2.1] octanes A61K31/46)
- A61K 31/496: Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
- A61K 31/519: ortho- or peri-condensed with heterocyclic rings
- A61K 31/551: having two nitrogen atoms, e.g. dilazep
- A61K 31/5513: 1,4-Benzodiazepines, e.g. diazepam {or clozapine}
- A61K 31/554: having at least one nitrogen and one sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
- A61P 3/04: Anorexiants; Antiobesity agents
- C07D 221/28: Morphinans
- C07D 405/06: linked by a carbon chain containing only aliphatic carbon atoms
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)

## 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

### Claim 1

A method of reducing diseases or disorders associated with the adverse metabolic profile of olanzapine by administering to a patient in need 10 thereof an effective amount of a compound of the formula:
or a pharmaceutically acceptable salt thereof.

### Claim 2 (depends on 1)

The method according to claim 1, wherein said adverse metabolic effects comprise an increase in abdominal fat distribution, serum glucose levels, triglyceride levels or high density cholesterol.

### Claim 3 (depends on 1)

The method of claim 1, wherein said disease or disorder is diabetes.

### Claim 4 (depends on 1)

The method of claim 1, wherein said diseases or disorders are cardiovascular disorders.

### Claim 5 (depends on 1)

The method of claim 1, wherein the disease or disorder is obesity.

### Claim 6 (depends on 1)

The method of claim 1, wherein the disease or disorder is hypertension.

### Claim 7

A method of lowering circulating ghrelin levels in a patient in need thereof, comprising administering to said patient an effective amount of the compound of formula:
or a pharmaceutically acceptable salt thereof.

### Claim 8

A method of lowering circulating ghrelin levels in a patient in need thereof, comprising administering to said patient an effective amount of the compound of formula:
or a pharmaceutically acceptable salt thereof, wherein said ghrelin level is increased by the administration of an atypical antipsychotic.

### Claim 9 (depends on 8)

The method according to claim 8, wherein said atypical antipsychotic is olanzapine.

### Claim 10

A method of lowering ghrelin levels in gastrointestinal tracts of a patient in need thereof, comprising administering to said patient an effective amount of the compound of formula:
or a pharmaceutically acceptable salt thereof.

### Claim 11

A method of lowering ghrelin levels in gastrointestinal tracts of a patient in need thereof, comprising administering to said patient an effective amount of the compound of formula:
or a pharmaceutically acceptable salt thereof, wherein said ghrelin level is increased by the administration of an atypical antipsychotic.

### Claim 12 (depends on 11)

The method according to claim 11, wherein said atypical antipsychotic is olanzapine.