2-methyl-thieno-benzodiazepine

• US 5,627,178 A
• Filed: 02/13/1995
• Issued: 05/06/1997
• Est. Priority Date: 04/23/1991
• Status: Expired due to Term

• Current Assignee: Lilly Industries Limited (Eli Lilly and Company)
• Original Assignee: Lilly Industries Limited (Eli Lilly and Company)
• Inventors: Hotten, Terrence M., Tupper, David E., Chakrabarti, Jiban K.
• Primary Examiner(s): Datlow, Philip I.
• Application Number:
  US08/387,997
• Time in Patent Office: 813 Days
• Field of Search: 514/220
• US Class Current: 514/220
• 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

Abstract

2-Methyl-4-(4-methyl-1-piperazinyl)-10H-thieno-[2,3-b][1,5]benzodiazepine, or an acid salt thereof, has pharmaceutical properties, and is of particular use in the treatment of disorders of the central nervous system. The compound has the following structure: ##STR1##

Claims

1. A method of treating a patient suffering from or susceptible to psychosis selected from the group consisting of Schizophrenia, Catatonic, Subchronic;

Schizophrenia, Catatonic, Chronic;

Schizophrenia, Catatonic, Subchronic with Acute Exacerbation;

Schizophrenia, Catatonic, Chronic with Acute Exacerbation;

Schizophrenia, Catatonic, in Remission;

Schizophrenia, Catatonic, Unspecified;

Schizophrenia, Disorganized, Subchronic;

Schizophrenia, Disorganized, Chronic;

Schizophrenia, Disorganized, Subchronic with Acute Exacerbation;

Schizophrenia, Disorganized, Chronic with Acute Exacerbation;

Schizophrenia, Disorganized, in Remission;

Schizophrenia, Disorganized, Unspecified;

Schizophrenia, Paranoid, Subchronic;

Schizophrenia, Paranoid, Chronic;

Schizophrenia, Paranoid, Subchronic with Acute Exacerbation;

Schizophrenia, Paranoid, Chronic with Acute Exacerbation;

Schizophrenia, Paranoid, in Remission;

Schizophrenia, Paranoid, Unspecified;

Schizophrenia, Undifferentiated, Subchronic;

Schizophrenia, Undifferentiated, Chronic;

Schizophrenia, Undifferentiated, Subchronic with Acute Exacerbation;

Schizophrenia, Undifferentiated, Chronic with Acute Exacerbation;

Schizophrenia, Undifferentiated, in Remission;

Schizophrenia, Undifferentiated, Unspecified;

Schizophrenia, Residual, Subchronic;

Schizophrenia, Residual, Chronic;

Schizophrenia, Residual, Subchronic with Acute Exacerbation;

Schizophrenia, Residual, Chronic with Acute Exacerbation;

Schizophrenia, Residual, in Remission;

Schizophrenia, Residual, Unspecified;

Delusional (Paranoid) Disorder;

Brief Reactive Psychosis;

Schizophreniform Disorder;

Schizoaffective Disorder;

Induced Psychotic Disorder;

Psychotic Disorder NOS (Atypical Psychosis);

Bipolar Disorder, Mixed, with Psychotic Features;

Bipolar Disorder, Manic, with Psychotic Features;

Bipolar Disorder, Depressed, with Psychotic Features; and

Major Depression, Single Episode, with Psychotic Features;

comprising administering to a patient in need thereof an effective amount of 2-methyl-4-(4-methyl-1-piperazinyl)-10H-thieno-[2,3-b][1,5]benzodiazepine, acid addition salt thereof.

2. A method of claim 1 for treating a patient suffering from or susceptible to a condition selected from the group consisting of Schizophrenia, Catatonic, Subchronic;

Schizophrenia, Catatonic, Chronic;

Schizophrenia, Catatonic, Subchronic with Acute Exacerbation;

Schizophrenia, Catatonic, Chronic with Acute Exacerbation;

Schizophrenia, Catatonic, in Remission;

Schizophrenia, Catatonic, Unspecified;

Schizophrenia, Disorganized, Subchronic;

Schizophrenia, Disorganized, Chronic;

Schizophrenia, Disorganized, Subchronic with Acute Exacerbation;

Schizophrenia, Disorganized, Chronic with Acute Exacerbation;

Schizophrenia, Disorganized, in Remission;

Schizophrenia, Disorganized, Unspecified;

Schizophrenia, Paranoid, Subchronic;

Schizophrenia, Paranoid, Chronic;

Schizophrenia, Paranoid, Subchronic with Acute Exacerbation;

Schizophrenia, Paranoid, Chronic with Acute Exacerbation;

Schizophrenia, Paranoid, in Remission;

Schizophrenia, Paranoid, Unspecified;

Schizophrenia, Undifferentiated, Subchronic;

Schizophrenia, Undifferentiated, Chronic;

Schizophrenia, Undifferentiated, Subchronic with Acute Exacerbation;

Schizophrenia, Undifferentiated, Chronic with Acute Exacerbation;

Schizophrenia, Undifferentiated, in Remission;

Schizophrenia, Undifferentiated, Unspecified;

Schizophrenia, Residual, Subchronic;

Schizophrenia, Residual, Chronic;

Schizophrenia, Residual, Subchronic with Acute Exacerbation;

Schizophrenia, Residual, Chronic with Acute Exacerbation;

Schizophrenia, Residual, in Remission;

Schizophrenia, Residual, Unspecified;

Delusional (Paranoid) Disorder;

Brief Reactive Psychosis;

Schizophreniform Disorder;

Schizoaffective Disorder;

Induced Psychotic Disorder;

Psychotic Disorder NOS (Atypical Psychosis);

Bipolar Disorder, Mixed, with Psychotic Features;

Bipolar Disorder, Manic, with Psychotic Features;

Bipolar Disorder, Depressed, with Psychotic Features; and

Major Depression, Single Episode, with Psychotic Features.

3. A method of claim 2 for treating a patient suffering from or susceptible to a condition selected from the group consisting of Schizophrenia, Catatonic, Subchronic;

Schizophrenia, Catatonic, Chronic;

Schizophrenia, Catatonic, Subchronic with Acute Exacerbation;

Schizophrenia, Catatonic, Chronic with Acute Exacerbation;

Schizophrenia, Catatonic, in Remission;

Schizophrenia, Catatonic, Unspecified;

Schizophrenia, Disorganized, Subchronic;

Schizophrenia, Disorganized, Chronic;

Schizophrenia, Disorganized, Subchronic with Acute Exacerbation;

Schizophrenia, Disorganized, Chronic with Acute Exacerbation;

Schizophrenia, Disorganized, in Remission;

Schizophrenia, Disorganized, Unspecified;

Schizophrenia, Paranoid, Subchronic;

Schizophrenia, Paranoid, Chronic;

Schizophrenia, Paranoid, Subchronic with Acute Exacerbation;

Schizophrenia, Paranoid, Chronic with Acute Exacerbation;

Schizophrenia, Paranoid, in Remission;

Schizophrenia, Paranoid, Unspecified;

Schizophrenia, Undifferentiated, Subchronic;

Schizophrenia, Undifferentiated, Chronic;

Schizophrenia, Undifferentiated, Subchronic with Acute Exacerbation;

Schizophrenia, Undifferentiated, Chronic with Acute Exacerbation;

Schizophrenia, Undifferentiated, in Remission;

Schizophrenia, Undifferentiated, Unspecified;

Schizophrenia, Residual, Subchronic;

Schizophrenia, Residual, Chronic;

Schizophrenia, Residual, Subchronic with Acute Exacerbation;

Schizophrenia, Residual, Chronic with Acute Exacerbation;

Schizophrenia, Residual, in Remission;

Schizophrenia, Residual, Unspecified;

Delusional (Paranoid) Disorder;

Brief Reactive Psychosis;

Schizophreniform Disorder; and

Schizoaffective Disorder.

4. A method of claim 1 wherein the effective amount is from 1 to 20 mg per day of 2-methyl-4-(4- methyl-1-piperazinyl)-10H-thieno-[2,3-b][1,5]benzodiazepine, or an acid addition salt thereof.

5. A method of treating a patient suffering from or susceptible to an anxiety disorder selected from the group consisting of Psychoactive Substance Anxiety Disorder;

Organic Anxiety Disorder;

Obsessive Compulsive Disorder;

Post-traumatic Stress Disorder;

Generalized Anxiety Disorder; and

Anxiety Disorder NOS;

comprising administering to a patient in need thereof an effective amount of 2-methyl-4-(4-methyl-1-piperazinyl)-10H-thieno[2,3-b][1,5]benzodiazepine, or an acid addition salt thereof.

6. A method of claim 5 wherein the effective amount is from 1 to 20 mg per day of 2-methyl-4-(4- methyl-1-piperazinyl)-10H-thieno-[2,3-b][1,5]benzodiazepine, or an acid addition salt thereof.

7. A method of claim 5 for treating an animal, including a human, suffering from or susceptible to an anxiety disorder selected from the group consisting of Organic Anxiety Disorder;

Obsessive Compulsive Disorder;

Post-traumatic Stress Disorder;

Generalized Anxiety Disorder; and

Anxiety Disorder NOS.

8. A method of treating a patient suffering from or susceptible to a pathologic psychological condition wherein delusions, hallucinations, disorganized behavior, or anxiety are a consistent manifestation of the pathologic condition, comprising administering to a patient in need thereof an effective amount of 2-methyl-4-(4-methyl-1-piperazinyl)-10H-thieno[2,3-b][1,5]benzodiazepine, or an acid addition salt thereof.

9. A method of claim 8 wherein delusions, hallucinations, or disorganized behavior are a consistent manifestation of the pathologic condition.

10. A method of claim 8 wherein the effective amount is from 1 to 20 mg per day of 2-methyl-4-(4-methyl-1-piperazinyl)-10H-thieno-[2,3b][1,5]benzodiazepine, or an acid addition salt thereof.