Iloperidone metabolite for use in the treatment of psychiatric disorders

Patent metadata

Field	Value
Publication number	US-10874659-B2
Application number	US-201314384401-A
Country	US
Kind code	B2
Filing date	Mar 14, 2013
Priority date	Mar 14, 2012
Publication date	Dec 29, 2020
Grant date	Dec 29, 2020

Abstract

R-P88 is used for the treatment of disorders amenable to treatment with an atypical antipsychotic.

First claim

What is claimed is:

1. A method of treating a patient suffering from a psychiatric disorder that comprises internally administering to the patient R-P88, or a pharmaceutically acceptable salt thereof, or an ester of R-P88, or a pharmaceutically acceptable salt of such ester, once per day, titrated to a final dose in accordance with one of the following increments:
1 mg once daily, 2 mg once daily, 4 mg once daily, 6 mg once daily, 8 mg once daily, 10 mg once daily, 12 mg once daily, to reach a maximum dose of 12 mg/day; or
2 mg once daily, 4 mg once daily, 8 mg once daily, 12 mg once daily, to reach a maximum dose of 12 mg/day; or
1 mg once daily, 4 mg once daily, 8 mg once daily, and 12 mg once daily, to reach a maximum dose of 12 mg/day; or
2 mg once daily, 6 mg once daily, and 12 mg once daily, to reach a maximum dose of 12 mg/day.

2. The method of claim 1 wherein the disorder is one that is amenable to treatment with iloperidone.

3. The method of claim 1 wherein the disorder is one or more of schizophrenia, schizoaffective disorder, bipolar disorder (mania and/or depression), depression, major depression, psychotic episodes, autism, autism spectrum disorder, fragile X syndrome, and pervasive developmental disorder.

4. The method of claim 1 , wherein the R-P88, or the pharmaceutically acceptable salt thereof, or the ester of R-P88, or the pharmaceutically acceptable salt of such ester, is orally administered.

5. A method of treating a patient suffering from a psychiatric disorder that comprises internally administering to the patient R-P88, or a pharmaceutically acceptable salt thereof, or an ester of R-P88, or a pharmaceutically acceptable salt of such ester, twice per day, titrated in accordance with one of the following increments:
1 mg twice daily, 2 mg twice daily, and 3 mg twice daily, to reach a maximum dose of 6 mg/day; or
1 mg twice daily, 2 mg twice daily, 3 mg twice daily, 4 mg twice daily, 5 mg twice daily and 6 mg twice daily, to reach a maximum dose of 12 mg/day; or
1 mg twice daily, 2 mg twice daily, 4 mg twice daily, 6 mg twice daily, 8 mg twice daily, to reach a maximum dose of 16 mg/day; or
1 mg twice daily, 4 mg twice daily, and 6 mg twice daily, to reach a maximum dose of 12 mg/day; or
2 mg twice daily and 6 mg twice daily, to reach a maximum dose of 12 mg/day.

6. The method of claim 5 wherein the disorder is one that is amenable to treatment with iloperidone.

7. The method of claim 5 , wherein the R-P88, or pharmaceutically acceptable salt thereof, or ester of R-P88, or pharmaceutically acceptable salt of such ester, is titrated in accordance with the following schedule:
1 mg b.i.d. on day 1, 2 mg b.i.d. on day 2, 3 mg b.i.d. on day 3 and thereafter; or
1 mg b.i.d. on day 1, 2 mg b.i.d. on day 2, 3 mg b.i.d. on day 3, 4 mg b.i.d. on day 4, 5 mg b.i.d. on day 5, 6 mg b.i.d. on day 6 and thereafter; or
1 mg b.i.d. on day 1, 2 mg b.i.d. on day 2, 4 mg b.i.d. on day 3, 6 mg b.i.d. on day 4, 8 mg b.i.d. on day 5 and thereafter.

Assignees

• Vanda Pharmaceuticals Inc

Inventors

• Phadke Deepak
• Wolfgang Curt D
• Polymeropoulos Mihael H
• Feeney John Joseph
• Birznieks Gunther

Classifications

• A61P25/18

  Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia · CPC title

• A61K31/454 Primary

  containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone · CPC title

• C07D261/20

  condensed with carbocyclic rings or ring systems · CPC title

• A61K31/42

  Oxazoles · CPC title

• A61K31/445

  Non condensed piperidines, e.g. piperocaine · CPC title