IP Library Granted Patent US 8,642,638
Granted Patent B2
US 8,642,638 · App. 13/129,782 · Granted Feb 4, 2014

Treatment of cognitive disorders with (R)-7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide and pharmaceutically acceptable salts thereof

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Quick Facts
Patent No.
US 8,642,638
App. No.
13/129,782
Granted
Feb 4, 2014
Kind
B2
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 improve cognition.

Claims (27)

1. A method of improving cognition in a patient suffering from Schizophrenia, 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 12 , 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.

14. A method of improving cognition in a patient suffering from Alzheimer's disease, 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.

15. The method of claim 14 , 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.

16. The method of claim 15 , wherein the pharmaceutically acceptable salt of the (R)-7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide is administered to said patient.

17. The method of claim 16 , 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.

18. The method of claim 16 , 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.

19. The method of claim 18 , wherein the daily dose is in the range of between 0.3 mg to 1.5 mg.

20. The method of claim 18 , wherein the daily dose is in the range of between 0.7 mg to 1.25 mg.

21. The method of claim 18 , wherein the daily dose is in the range of between 1.0 mg to 3.0 mg.

22. The method of claim 18 , wherein the daily dose is in the range of between 1.5 mg to 2.5 mg.

23. The method of claim 18 , wherein the daily dose is in the range of between 1.75 mg to 2.25 mg.

24. The method of claim 18 , wherein the daily dose is in the range of between 2.0 mg to 3.0 mg.

25. The method of claim 14 , 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.

Assignments (3)
SECURITY INTEREST Recorded Jul 5, 2016
From: FORUM PHARMACEUTICALS INC.
To: FMR LLC
Reel/Frame 039254/0828 →
CHANGE OF NAME Recorded Apr 21, 2014
From: ENVIVO PHARMACEUTICALS, INC.
To: FORUM PHARMACEUTICALS, INC.
Reel/Frame 032722/0659 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 9, 2011
From: CHESWORTH, RICHARD; SHAPIRO, GIDEON; KOENIG, GERHARD
To: ENVIVO PHARMACEUTICALS, INC.
Reel/Frame 026721/0035 →