IP Library Granted Patent US 7,897,614
Granted Patent B2
US 7,897,614 · App. 11/514,905 · Granted Mar 1, 2011

Preventive agent/remedial agent for constipation predominant IBS

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Quick Facts
Patent No.
US 7,897,614
App. No.
11/514,905
Granted
Mar 1, 2011
Kind
B2
Abstract

A novel preventive and/or therapeutic medicament for a constipation predominant IBS which contains as the active ingredient a thieno[3,2-b]pyridinecarboxamide derivative represented by the formula (I): wherein R 1 and R 2 each independently represents hydrogen atom or a lower alkyl group and A represents a substituent selected from the group consisting of 1-azabicyclo[3.2.2]nonyl group 1-azabicyclo[2.2.2]octyl group, and the N-oxides thereof, a pharmaceutically acceptable salt thereof, or a solvate or hydrate thereof.

Claims (23)

1. A method of treating constipation predominant IBS comprising administering to a patient in need thereof a therapeutically effective amount of a thieno[3,2-b]pyridinecarboxamide derivative represented by the following formula (I) or a tautomer thereof:

wherein R 1 and R 2 each independently represents hydrogen atom or a lower alkyl group and A represents a substituent selected from the group consisting of a 1-azabicyclo[3.2.2]nonyl group, a 1-azabicyclo[2.2.2]octyl group, and N-oxides thereof, or a pharmaceutically acceptable salt thereof.

2. The method according to claim 1 wherein R 1 and R 2 each independently represents a hydrogen atom or a methyl group.

3. The method according to claim 1 , wherein A represents a 1-azabicyclo[2.2.2]oct-3-yl group or an N-oxide thereof.

4. The method according to claim 1 , wherein said derivative is any one of N-(1-azabicyclo[2.2.2]oct-3-yl)-4,7-dihydro-7-oxo-thieno[3,2-b]pyridine-6-carboxamide, (R)-N-(1-azabicyclo[2.2.2]oct-3-yl)-4,7-dihydro-7-oxo-thieno[3,2-b]pyridine-6-carboxamide, (S)-N-(1-azabicyclo[2.2.2]oct-3-yl)-4,7-dihydro-7-oxo-thieno[3,2-b]-pyridine-6-carboxamide, or a tautomer thereof.

5. The method according to claim 1 , wherein said derivative is in the form of a hydrochloride salt.

6. A method of treating constipation predominant IBS comprising administering to a patient in need thereof a therapeutically effective amount of (R)-N-(1-azabicyclo[2.2.2]oct-3-yl)-4,7-dihydro-7-oxo-thieno[3,2-b]pyridine-6-carboxamide or the tautomer thereof.

7. The method according to claim 2 , wherein A represents a 1-azabicyclo[2.2.2]oct-3-yl group or an N-oxide thereof.

8. The method according to claim 2 , wherein said derivative is in the form of a hydrochloride salt.

9. The method according to claim 3 , wherein said derivative is in the form of a hydrochloride salt.

10. The method according to claim 4 , wherein said derivative is in the form of a hydrochloride salt.

11. The method according to claim 6 , wherein said derivative is in the form of a hydrochloride salt.

12. The method of claim 1 , wherein the derivative of formula (I) is in the form of a pharmaceutically acceptable salt thereof.

13. A method of treating abdominal pain or discomfort associated with constipation predominant IBS, comprising administering to a patient in need thereof a therapeutically effective amount of a thieno[3,2-b]pyridinecarboxamide derivative represented by the following formula (I) or a tautomer thereof:

wherein R 1 and R 2 each independently represents a hydrogen atom or lower alkyl group and A represents a substituent selected from the group consisting of a 1-azabicyclo[3.2.2]nonyl group, a 1-azabicyclo[2.2.2]octyl group and N-oxides thereof, or a pharmaceutically acceptable salt thereof.

14. The method of claim 13 , wherein R 1 and R 2 each independently represents a hydrogen atom or a methyl group.

15. The method of claim 13 , wherein A represents a 1-azabicyclo[2.2.2]oct-3-yl group or an N-oxide thereof.

16. The method of claim 13 , wherein said derivative is any one of N-(1-azabicyclo[2.2.2]oct-3-yl)-4,7-dihydro-7-oxo-thieno[3,2-b]pyridine-6-carboxamide, (R)-N-(1-azabicyclo[2.2.2]oct-3-yl)-4,7-dihydro-7-oxo-thieno[3,2-b]pyridine-6-carboxamide, (S)-N-(1-azabicyclo[2.2.2]oct-3-yl)-4,7-dihydro-7-oxo-thieno[3,2-b]pyridine-6-carboxamide, or a tautomer thereof.

17. The method of claim 13 , wherein said derivative is in the form of a hydrochloride salt.

18. A method of treating abdominal pain or discomfort associated with constipation predominant IBS, comprising administering to a patient in need thereof a therapeutically effective amount of (R)-N-(1-azabicyclo[2.2.2]oct-3-yl)-4,7-dihydro-7-oxo-thieno[3,2-b]pyridine-6-carboxamide, or the tautomer thereof.

19. The method of claim 18 , wherein said derivative is in the form of a hydrochloride salt.

20. The method of claim 13 , wherein the administration is oral.

21. The method of claim 13 , wherein the derivative of formula (I) is in the form of a pharmaceutically acceptable salt thereof.

Assignments (1)
CHANGE OF NAME Recorded Apr 17, 2008
From: MITSUBISHI PHARMA CORPORATION
To: MITSUBISHI TANABE PHARMA CORPORATION
Reel/Frame 020838/0701 →