2-Hydroxymethylolanzapine compositions and methods

• US 6,346,528 B1
• Filed: 10/17/2000
• Issued: 02/12/2002
• Est. Priority Date: 11/23/1998
• Status: Expired due to Fees

• Current Assignee: Sepracor Incorporated
• Original Assignee: Sepracor Incorporated
• Inventors: Yelle, William E.
• Primary Examiner(s): Rose, Shep K.
• Application Number:
  US09/690,357
• Time in Patent Office: 483 Days
• Field of Search: 514/220
• US Class Current: 514/220
• 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 31/551 having two nitrogen atoms, e.g. dilazep
• CPC Class Codes: A61K 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• CPC Class Codes: A61P 1/00 Drugs for disorders of the alimentary tract or the digestive system
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system
• CPC Class Codes: A61P 25/14 for treating abnormal movements, e.g. chorea, dyskinesia
• 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 25/30 for treating abuse or dependence
• CPC Class Codes: A61P 31/10 Antimycotics
• CPC Class Codes: C07D 495/04 Ortho-condensed systems

Abstract

Methods and compositions are disclosed utilizing 2-hydroxymethylolanzapine for the treatment of psychosis in humans. 2-Hydroxymethylolanzapine exhibits a lessened liability toward drug-drug interactions than olanzapine and a more predictable dosing regimen than olanzapine. 2-Hydroxymethylolanzapine is also useful for the treatment of acute mania, mild anxiety states, anxiety disorders, schizophrenia, bipolar disorder, attention deficit hyperactivity disorder, autistic disorder, excessive aggression, substance abuse, depressive signs and symptoms, tic disorder, functional bowel disorder and fungal dermatitis.

Claims

1. A pharmaceutical composition comprising an amount of 2-hydroxymethylolanzapine, or a pharmaceutically acceptable salt thereof, ranging from 1 mg to 150 mg, and one or more pharmaceutically acceptable carriers for oral therapy, wherein the pharmaceutical composition is in the form of a tablet or capsule.