Use of metformin in combination with a glucokinase activator and compositions comprising metformin and a glucokinase activator

Patent metadata

Field	Value
Publication number	US-10064846-B2
Application number	US-201715687824-A
Country	US
Kind code	B2
Filing date	Aug 28, 2017
Priority date	May 26, 2010
Publication date	Sep 4, 2018
Grant date	Sep 4, 2018

Abstract

The present invention provides uses of a glucokinase activator in combination with metformin. Uses include treating type 2 diabetes, lowering blood glucose, improving insulin sensitivity, enhancing phosphorylation of glucose, and improving the therapeutic effectiveness of metformin. The invention also provides pharmaceutical compositions that comprise a GK activator and metformin. The invention also provides a salt formed between metformin and a GK activator.

First claim

What is claimed is:

1. A method of improving insulin sensitivity in a subject comprising:
administering to the subject {2-[3-cyclohexyl-3-(trans-4-propoxy-cyclohexyl)-ureido]-thiazol-5-ylsulfanyl}-acetic acid or a pharmaceutically acceptable salt thereof in combination with metformin, wherein the metformin is administered in an amount of less than 1000 mg/day.

2. The method of claim 1 , wherein the metformin is administered in an amount between 0.01 mg/day and less than 1000 mg/day.

3. The method of claim 1 , wherein metformin is administered in an amount between 10 mg/day and 850 mg/day.

4. The method of claim 1 , wherein the metformin is administered in an amount between 10 mg/day and less than 1000 mg/day.

5. The method of claim 1 , wherein {2-[3-cyclohexyl-3-(trans-4-propoxy-cyclohexyl)-ureido]-thiazol-5-ylsulfanyl}-acetic acid is administered in an amount of less than 1000 mg/day.

6. The method of claim 1 , wherein the metformin is 1,1-dimethylbiguanide monohydrochloride.

7. The method of claim 2 , wherein the metformin is 1,1-dimethylbiguanide monohydrochloride.

8. The method of claim 3 , wherein the metformin is 1,1-dimethylbiguanide monohydrochloride.

9. The method of claim 4 , wherein the metformin is 1,1-dimethylbiguanide monohydrochloride.

10. The method of claim 5 , wherein the metformin is 1,1-dimethylbiguanide monohydrochloride.

11. The method of claim 1 , wherein the subject is a human.

12. The method of claim 11 , wherein the subject is suffering from type 2 diabetes.

13. The method of claim 1 , wherein the {2-[3-cyclohexyl-3-(trans-4-propoxy-cyclohexyl)-ureido]-thiazol-5-ylsulfanyl}-acetic acid or a pharmaceutically acceptable salt thereof and the metformin are administered in the same dosage form.

14. The method of claim 1 , wherein the {2-[3-cyclohexyl-3-(trans-4-propoxy-cyclohexyl)-ureido]-thiazol-5-ylsulfanyl}-acetic acid or a pharmaceutically acceptable salt thereof and the metformin are administered in separate dosage forms.

15. The method of claim 1 , wherein the {2-[3-cyclohexyl-3-(trans-4-propoxy-cyclohexyl)-ureido]-thiazol-5-ylsulfanyl}-acetic acid or a pharmaceutically acceptable salt thereof and the metformin are administered simultaneously.

16. The method of claim 1 , wherein the {2-[3-cyclohexyl-3-(trans-4-propoxy-cyclohexyl)-ureido]-thiazol-5-ylsulfanyl}-acetic acid or a pharmaceutically acceptable salt thereof and the metformin are administered in sequence.

Assignees

• Vtv Therapeutics Llc

Inventors

• Mjalli Adnan M M
• Valcarce Lopez Maria Carmen

Classifications

• A61P3/08

  for glucose homeostasis (pancreatic hormones A61P5/48) · CPC title

• A61P3/10

  for hyperglycaemia, e.g. antidiabetics · CPC title

• A61P43/00

  Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title

• A61P3/00

  Drugs for disorders of the metabolism (of the blood or the extracellular fluid A61P7/00) · CPC title

• C07C279/26

  X and Y being nitrogen atoms, i.e. biguanides · CPC title