AGENT FOR TREATMENT OF SCHIZOPHRENIA

• US 20140371236A1
• Filed: 08/28/2014
• Published: 12/18/2014
• Est. Priority Date: 08/22/2002
• Status: Active Grant

• Current Assignee: Sumitomo Pharmaceuticals Company Limited (Sumitomo Chemical Company Limited)
• Original Assignee: Sumitomo Dainippon Pharma Company Limited (Sumitomo Chemical Company Limited)
• Inventors: Ogasa, Masaaki, Sami, Shunsuke, Nakamura, Mitsutaka
• Granted Patent: US 9,815,827 B2
• Time in Patent Office: Days
• US Class Current: 514/254.04
• CPC Class Codes: A61K 31/496 Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
• 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
• CPC Class Codes: C07D 417/12 linked by a chain containing hetero atoms as chain links

Abstract

The present invention provides a novel method for treatment of schizophrenia which can improve wide-ranging symptoms of schizophrenia, especially positive symptoms and negative symptoms without being accompanied by extrapyramidal symptoms, which comprises orally administering as an active compound (1R,23,3R,4S)-N-[(1R,2R)-2-[4-(1,2-benzoisothiazol-3-yl)-1-piperazinylmethyl]-1-cyclohexylmethyl]-2,3-bicyclo[2.2.1]heptanedicarboxyimide or a pharmaceutically acceptable salt thereof (e.g., hydrochloride) at a daily dose of 5 mg to 120 mg once a day to a patient with schizophrenia, and a therapeutic agent to be used in said method.

Claims

1-19. -19. (canceled)

20. A method for treating schizophrenia in a patient, without causing clinically significant body weight gain in the patient, the method comprising administering to the patient a dose of 5 mg to 120 mg of the active compound:

(1R,2S,3R,4S)N-[(1R,2R)-2-[4-(1,2-benzoisothiazol-3-yl)-1-piperazinylmethyl]-1-cyclohexylmethyl]-2,3-bicyclo[2.2.1]heptanedicarboximide or a pharmaceutically acceptable salt thereof.

21. The method of claim 20, wherein said active compound is (1R,2S,3R,4S)N-[(1R,2R)-2-[4-(1,2-benzoisothiazol-3-yl)-1-piperazinylmethyl]-1 -cyclohexylmethyl]-2,3-bicyclo[2.2.1]heptanedicarboximide hydrochloride.

22. The method of claim 20, wherein 20 mg to 120 mg of said active compound is administered to said patient.

23. The method of claim 20, wherein said active compound is administered to said patient orally.

24. The method of claim 20, wherein said active compound is administered to said patient without concurrently administering another antipsychotic medication.

25. The method of claim 20, wherein said active compound is administered to said patient for a period of at least six weeks.

26. The method of claim 20, wherein said patient has a BPRS score of at least 42 and wherein the patient'"'"'s BPRS score is significantly reduced from a baseline measurement prior to the administering of said active compound.

27. The method of claim 20, wherein said active compound is administered once daily.