IP Library Granted Patent US 8,263,634
Granted Patent B2
US 8,263,634 · App. 12/942,297 · Granted Sep 11, 2012

Heteroaryl-ureas and their use as glucokinase activators

Assignee: Novo Nordisk A/S
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Quick Facts
Patent No.
US 8,263,634
App. No.
12/942,297
Granted
Sep 11, 2012
Kind
B2
Abstract

This invention relates to compounds of formula (I) which are activators of glucokinase and thus may be useful for the management, treatment, control, or adjunct treatment of diseases, where increasing glucokinase activity is beneficial.

Claims (18)

1. A method of alleviating or relieving a symptom or complication of diabetes in a human suffering from type 2 diabetes comprising administering to said human a compound or pharmaceutical composition which comprises {2-[3-Cyclohexyl-3-(trans-4-propoxy-cyclohexyl)-ureido]-thiazol-5-ylsulfanyl)-acetic acid or a salt thereof with a pharmaceutically acceptable acid or base.

2. The method of claim 1 , wherein the compound is {2-[3-cyclohexyl-3-(trans-4-propoxy-cyclohexyl)-ureido]-thiazol-5-ylsulfanyl)-acetic acid.

3. A method of alleviating or relieving a symptom or complication of diabetes in a human suffering from type 2 diabetes comprising administering to said human a compound or pharmaceutical composition which comprises 3-{2-[3-Cyclohexyl-3-(trans-4-propoxy-cyclohexyl)-ureido]-thiazol-5-ylsulfanyl)-propionic acid or a salt thereof with a pharmaceutically acceptable acid or base.

4. The method of claim 3 , wherein the compound is 3-{2-[3-cyclohexyl-3-(trans-4-propoxy-cyclohexyl)-ureido]-thiazol-5-ylsulfanyl}-propionic acid.

5. A method of alleviating or relieving a symptom or complication of diabetes in a human suffering from type 2 diabetes comprising administering to said human a compound or pharmaceutical composition which comprises 3-{2-[3-Cyclohexyl-3-(trans-4-methyl-cyclohexyl)-ureido]-thiazol-5-ylsulfanyl}-propionic acid or a salt thereof with a pharmaceutically acceptable acid or base.

6. The method of claim 5 , wherein the compound is 3-{2-[3-cyclohexyl-3-(trans-4-methyl-cyclohexyl)-ureido]-thiazol-5-ylsulfanyl}-propionic acid.

7. A method of alleviating or relieving a symptom or complication of diabetes in a human suffering from type 2 diabetes comprising administering to said human a compound or pharmaceutical composition which comprises {2-[3-Cyclohexyl-3-(trans-4-methoxy-cyclohexyl)-ureido]-thiazol-5-ylsulfanyl}-acetic acid or a salt thereof with a pharmaceutically acceptable acid or base.

8. The method of claim 7 , wherein the compound is {2-[3-cyclohexyl-3-(trans-4-methoxy-cyclohexyl)-ureido]-thiazol-5-ylsulfanyl}-acetic acid.

9. A method of alleviating or relieving a symptom or complication of diabetes in a human suffering from type 2 diabetes comprising administering to said human a compound or pharmaceutical composition which comprises 2-{2-[3-Cyclohexyl-3-(trans-4-methyl-cyclohexyl)-ureido]-thiazol-5-ylsulfanyl}-2-methyl-propionic acid or a salt thereof with a pharmaceutically acceptable acid or base.

10. The method of claim 9 , wherein the compound is 2-{2-[3-cyclohexyl-3-(trans-4-methyl-cyclohexyl)-ureido]-thiazol-5-ylsulfanyl}-2-methyl-propionic acid.

11. A method for lowering blood glucose levels in a human comprising administering to said human a compound selected from the group consisting of:

{2-[3-Cyclohexyl-3-(trans-4-propoxy-cyclohexyl)-ureido]-thiazol-5-ylsulfanyl}-acetic acid;

3-{2-[3-Cyclohexyl-3-(trans-4-propoxy-cyclohexyl)-ureido]-thiazol-5-ylsulfanyl}propionic acid;

3-{2-[3-Cyclohexyl-3-(trans-4-methyl-cyclohexyl)-ureido]-thiazol-5-ylsulfanyl}-propionic acid;

{2-[3-Cyclohexyl-3-(trans-4-methoxy-cyclohexyl)-ureido]-thiazol-5-ylsulfanyl}-acetic acid; and

2-{2-[3-Cyclohexyl-3-(trans-4-methyl-cyclohexyl)-ureido]-thiazol-5-ylsulfanyl}-2-methyl-propionic acid;

or a salt of any of the above with a pharmaceutically acceptable acid or base.

12. The method of claim 11 , wherein the human suffers from type 2 diabetes.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 14, 2021
From: NOVO NORDISK A/S
To: VTV THERAPEUTICS LLC
Reel/Frame 055584/0833 →
Priority Claims (3)
DK 2004 00013 · Jan 6, 2004 · national
DK 2004 01272 · Aug 23, 2004 · national
DK 2004 01897 · Dec 7, 2004 · national
Continuity (5)
Continuation 12757217 · Apr 9, 2010
Continuation 12188402 · Aug 8, 2008
Continuation 11453330 · Jun 14, 2006
Continuation PCTDK2005000002 · Jan 6, 2005
Related Publication 20110060019A1 · Mar 10, 2011