TREATMENT OF COGNITIVE DISORDERS WITH (R)-7-CHLORO-N-(QUINUCLIDIN-3-YL)BENZO[B]THIOPHENE-2-CARBOXAMIDE AND PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF

• US 20140155430A1
• Filed: 02/07/2014
• Published: 06/05/2014
• Est. Priority Date: 11/19/2008
• Status: Active Grant

• Current Assignee: Forum Pharmaceuticals Inc.
• Original Assignee: Envivo Pharmaceuticals, Inc.
• Inventors: Chesworth, Richard, Shapiro, Gideon, Koenig, Gerhard
• Granted Patent: US 8,815,933 B2
• Time in Patent Office: Days
• US Class Current: 514/305
• CPC Class Codes: A61K 31/439 the ring forming part of a bridged ring system, e.g. quinuclidine 8-azabicyclo [3.2.1] octanes A61K31/46
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system

Abstract

(R)-7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide has been found to have procognitive effects in humans at unexpectedly low doses. Thus, (R)-7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide and pharmaceutically acceptable salts thereof can be used at unexpectedly low doses to improve cognition.

Claims

1. A method of treating negative symptoms associated with Schizophrenia in a patient in need thereof, comprising:

administering to said patient a daily dose in the range of between 0.1 mg to 3.0 mg of (R)-7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide, or a pharmaceutically acceptable salt thereof.

2. The method of claim 1, wherein the pharmaceutically acceptable salt of the (R)-7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide is:

(R)-7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide hydrochloride;

(R)-7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide hydrochloride monohydrate;

or (R)-7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide hydrochloride solvate.

3. The method of claim 2, wherein the pharmaceutically acceptable salt of the (R)-7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide is administered to the patient.

4. The method of claim 3, wherein the pharmaceutically acceptable salt of the (R)-7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide is (R)-7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide hydrochloride.

5. The method of claim 3, wherein the pharmaceutically acceptable salt of the (R)-7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide is (R)-7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide hydrochloride monohydrate.

6. The method of claim 5, wherein the daily dose is in the range of between 0.3 mg to 1.5 mg.

7. The method of claim 5, wherein the daily dose is in the range of between 0.7 mg to 1.25 mg.

8. The method of claim 5, wherein the daily dose is in the range of between 1.0 mg to 3.0 mg.

9. The method of claim 5, wherein the daily dose is in the range of between 1.5 mg to 2.5 mg.

10. The method of claim 5, wherein the daily dose is in the range of between 1.75 mg to 2.25 mg.

11. The method of claim 5, wherein the daily dose is in the range of between 2.0 mg to 3.0 mg.

12. The method of claim 1, wherein the schizophrenia comprises a paranoid type, a disorganized type, catatonic type, or an undifferentiated type.

13. The method of claim 1, wherein the (R)-7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide, or pharmaceutically acceptable salt thereof, is administered as a pharmaceutical composition.