IP Library Granted Patent US 8,946,264
Granted Patent B2
US 8,946,264 · App. 13/656,664 · Granted Feb 3, 2015

Pyridine derivative

Inventors: Tsuyoshi Shinozuka (Tokyo, JP); Tomoharu Tsukada (Tokyo, JP); Kunihiko Fujii (Tokyo, JP); Makoto Mori (Tokyo, JP)
Assignee: Daiichi Sankyo Company, Limited
C07D401/12
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Quick Facts
Patent No.
US 8,946,264
App. No.
13/656,664
Filed
Oct 20, 2012
Granted
Feb 3, 2015
Kind
B2
Art Unit
1625
USPC
546/273.4
Abstract

The present invention relates to a novel pyridine derivative or a pharmacologically acceptable ester thereof, or a pharmacologically acceptable salt of the derivative or ester, which has an excellent hypoglycemic effect or treats and/or prevents the onset of a disorder of carbohydrate or lipid metabolism or a disease mediated by peroxisome proliferator-activated receptor (PPAR) γ. A compound represented by the general formula (I): [wherein R represents a pyridyl group substituted with 1 to 3 group(s) independently selected from Substituent Group A, and Substituent Group A represents a halogen atom, a C 1 -C 6 alkyl group and a C 1 -C 6 alkoxy group] or a pharmacologically acceptable ester thereof, or a pharmacologically acceptable salt of the compound or ester.

Claims (22)

1. A compound having a formula (I):

or a pharmacologically acceptable C 1 to C 4 alkyl ester of the compound, or a pharmacologically acceptable salt of the compound or the ester.

2. The compound according to claim 1 that is: 3-({6-[(3,5-dimethylpyridin-2-yl)oxy]-1-methyl-1H-benzimidazol-2-yl}methoxy)benzoic acid.

3. The compound according to claim 1 that is: a pharmacologically acceptable salt of 3-({6-[(3,5-dimethylpyridin-2-yl)oxy]-1-methyl-1H-benzimidazol-2-yl}methoxy)benzoic acid.

4. The compound according to claim 1 that is: a calcium salt of 3-({6-[(3,5-dimethylpyridin-2-yl)oxy]-1-methyl-1H-benzimidazol-2-yl}methoxy)benzoic acid.

5. The compound according to claim 1 that is: a sodium salt of 3-({6-[(3,5-dimethylpyridin-2-yl)oxy]-1-methyl-1H-benzimidazol-2-yl}methoxy)benzoic acid.

6. The compound according to claim 1 that is: a hydrochloride salt of 3-({6-[(3,5-dimethylpyridin-2-yl)oxy]-1-methyl-1H-benzimidazol-2-yl}methoxy)benzoic acid.

7. A composition comprising the compound, or the pharmacologically acceptable C 1 to C 4 alkyl ester of the compound, or the pharmacologically acceptable salt of the compound or the ester of claim 1 and an inert carrier or diluent.

8. The composition according to claim 7 , further comprising an additive.

9. The composition according to claim 8 , wherein the additive is selected from the group consisting of: excipients, lubricants, binders, disintegrants, stabilizers, corrigents, diluents, and a combination thereof.

10. The composition according to claim 7 , wherein the composition is for oral administration.

11. A method for the treatment of a disease selected from the group consisting of: diabetes, type II diabetes, impaired glucose tolerance, and gestational diabetes mellitus, the method comprising

administering a pharmacologically effective amount of the compound, or the pharmacologically acceptable ester of the compound, or the pharmacologically acceptable salt of the compound or the ester of claim 1 to a warm-blooded animal.

12. The method according to claim 11 , wherein the warm-blooded animal is a human.

13. The method according to claim 12 , wherein the disease is diabetes.

14. The method according to claim 12 , wherein the disease is type II diabetes.

15. A method for lowering blood glucose levels in a human comprising

administering a pharmacologically effective amount of the compound, or the pharmacologically acceptable ester of the compound, or the pharmacologically acceptable salt of the compound or the ester of claim 1 to the human.

16. A method for improving insulin resistance in a human comprising

administering a pharmacologically effective amount of the compound, or the pharmacologically acceptable ester of the compound, or the pharmacologically acceptable salt of the compound or the ester of claim 1 to the human.

17. A method for activating peroxisome proliferator-activated receptor (PPAR) γ in a human, comprising

administering a pharmacologically effective amount of the compound, or the pharmacologically acceptable ester of the compound, or the pharmacologically acceptable salt of the compound or the ester of claim 1 to the human.

Priority Claims (1)
JP 2009-051820 · Mar 5, 2009 · national
Continuity (3)
Continuation 13088103 · Apr 15, 2011
Continuation PCTJP2010053384 · Mar 3, 2010
Related Publication 20130045994A1 · Feb 21, 2013