IP Library Granted Patent US 9,072,692
Granted Patent B2
US 9,072,692 · App. 13/866,936 · Granted Jul 7, 2015

Compositions and methods for modulating metabolic pathways

Inventors: Michael Zemel (Heiskell, TN); E. Douglas Grindstaff, II (Nashville, TN); Antje Bruckbauer (Knoxville, TN)
Assignee: NUSIRT SCIENCES, INC.
A61K31/05A61K36/87A61K31/192A61K31/353A61K45/06A61K31/015A61K31/155A61K31/19A61K31/198A61K31/426A23L1/3051A23L2/52A61K31/194A61K31/4439
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Quick Facts
Patent No.
US 9,072,692
App. No.
13/866,936
Granted
Jul 7, 2015
Kind
B2
Abstract

Compositions and methods useful for inducing an increase in fatty acid oxidation or mitochondrial biogenesis, reducing weight gain, inducing weight loss, or increasing Sirt1, Sirt3, or AMPK activity are provided herein. Such compositions can contain synergizing amounts of a sirtuin-pathway activators, including but not limited to resveratrol, in combination with beta-hydroxymethylbutyrate (HMB), keto isocaproic acid (KIC), leucine, or combinations of HMB, KIC and leucine.

Claims (36)

1. A composition comprising:

(a) at least about 500 mg of leucine and/or at least about 200 mg of one or more metabolites thereof, wherein the one or more leucine metabolites are selected from the group consisting of keto-isocaproic acid (KIC), alpha-hydroxy-isocaproic acid, and HMB; and

(b) at least about 25 mg to less than about 2000 mg of metformin;

wherein the composition is substantially free of the individual amino acids alanine, glutamic acid, glycine, isoleucine, valine, and proline;

wherein, when (a) is leucine, the molar ratio of (a) to (b) is greater than 2; and

wherein the composition is formulated as a tablet, capsule, gel capsule, beverage, snack bar or a food composition.

2. The composition of claim 1 , wherein the composition comprises at least about 50 mg of metformin.

3. The composition of claim 1 , wherein the composition comprises at least about 250 mg of metformin.

4. The composition of claim 1 , wherein the composition comprises at least about 50 mg of metformin and less than about 500 mg of metformin.

5. The composition of claim 1 , wherein the composition further comprises rosiglitazone.

6. The composition of claim 1 , wherein the composition comprises at least about 500 mg of metformin and further comprises at least about 50 mg of resveratrol.

7. The composition of claim 1 , wherein the composition is substantially free of an individual non-branched amino acid.

8. The composition of claim 1 , further comprising a sirtuin pathway activator that activates one or more of SIRT1, SIRT3, AMPK, and PGC1α.

9. The composition of claim 1 , further comprising at least one of a hydroxycinnamic acid, a stilbene, a polyphenol or a polyphenol precursor.

10. The composition of claim 1 , wherein the composition comprises a subtherapeutic amount of metformin.

11. The composition of claim 9 , wherein the polyphenol or polyphenol precursor is selected from the group consisting of chlorogenic acid, resveratrol, caffeic acid, cinnamic acid, ferulic acid, piceatannol, ellagic acid, epigallocatechin gallate, grape seed extract, and any analog thereof.

12. The composition of claim 1 , further comprising a phosphodiesterase inhibitor.

13. The composition of claim 1 , further comprising resveratrol.

14. The composition of claim 1 , wherein the composition is formulated as a unit dose.

15. The composition of claim 1 , wherein the composition comprises a therapeutic amount of metformin.

16. A method for treating diabetes in a subject in need thereof comprising:

administering to the subject the composition of claim 1 to the subject,

wherein the insulin sensitivity in the subject is increased.

17. The method of claim 16 , wherein the fat oxidation in the subject is increased or the inflammatory response in the subject is decreased.

18. The method of claim 16 , wherein the composition is substantially free of an individual non-branched amino acid.

19. The method of claim 16 , wherein the composition further comprises rosiglitazone.

20. The method of claim 16 , wherein the composition comprises at least 50 mg of metformin.

21. The method of claim 16 , wherein the composition comprises at least about 50 mg of resveratrol and at least about 500 mg of metformin.

22. The method of claim 16 , wherein the composition of claim 1 further comprises resveratrol.

23. A method for increasing irisin levels in a subject in need thereof comprising:

administering to the subject the composition of claim 1 to the subject,

wherein the irisin levels in the subject is increased.

24. The method of claim 23 , wherein the composition comprises at least about 50 mg to less than about 500 mg of metformin.

25. The method of claim 23 , wherein the composition comprises at least 50 mg of metformin.

26. The method of claim 23 , wherein the composition comprises at least about 50 mg of resveratrol and at least about 500 mg of metformin.

27. The method of claim 23 , wherein the composition of claim 1 further comprises rosiglitazone.

Assignments (2)
CHANGE OF NAME Recorded May 20, 2013
From: NUMETA SCIENCES, INC.
To: NUSIRT SCIENCES, INC.
Reel/Frame 030452/0384 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 16, 2013
From: ZEMEL, MICHAEL; GRINDSTAFF II, E. DOUGLAS; BRUCKBAUER, ANTJE
To: NUMETA SCIENCES, INC.
Reel/Frame 030432/0800 →
Continuity (9)
Continuation 13549381 · Jul 13, 2012
Provisional Application 61508139 · Jul 15, 2011
Provisional Application 61636597 · Apr 20, 2012
Provisional Application 61636598 · Apr 20, 2012
Provisional Application 61636603 · Apr 20, 2012
Provisional Application 61636605 · Apr 20, 2012
Provisional Application 61636608 · Apr 20, 2012
Provisional Application 61636610 · Apr 20, 2012
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