IP Library Patent Application 15113723
Patent Application
App. No. 15/113,723

KILLING SENESCENT CELLS AND TREATING SENESCENCE-ASSOCIATED CONDITIONS USING A SRC INHIBITOR AND A FLAVONOID

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Patent No.
US None
App. No.
15/113,723
Abstract

Provided herein are methods and uses for treatment or prophylaxis of a senescent cell associated disease or disorder by administering a senolytic combination comprising dasatinib and quercetin or an analog thereof to a subject in need thereof. In certain embodiments, the senescent cell associated disease or disorder is a cardiovascular disease or disorder, inflammatory disease or disorder, a pulmonary disease or disorder, a neurological disease or disorder, or a metabolic disease or disorder.

Claims (41)

1 . A method for treating a senescence associated disease or disorder in a subject comprising administering to the subject a senolytic combination,

wherein the senescence associated disease or disorder is not cancer; and

wherein the senolytic combination includes a src inhibitor and a flavonoid.

2 . The method of claim 1 , wherein the senolytic combination is administered once every 0.5-12 months; provided that if the senescence associated disease or disorder is a senescence associated metabolic disorder, the senolytic combination is administered once every 4-12 months.

3 . (canceled)

4 . The method of claim 1 , wherein the senescence associated disease or disorder is atherosclerosis.

5 . The method of claim 1 , wherein the senescence associated disease or disorder is osteoarthritis.

6 . The method of claim 1 , wherein the senescence associated disease or disorder is idiopathic pulmonary fibrosis or chronic obstructive pulmonary disease.

7 . (canceled)

8 . The method of claim 1 , wherein the senescence associated disease or disorder is selected from diabetes, metabolic syndrome, and obesity.

9 .- 10 . (canceled)

11 . A method of killing a senescent cell, comprising contacting the senescent cell with a src inhibitor and a flavonoid.

12 . The method of claim 11 , wherein the senescent cell is selected from a senescent fibroblast, a senescent pre-adipocyte, a senescent epithelial cell, a senescent chondrocyte, a senescent neuron, and a senescent endothelial cell.

13 . The method of claim 11 , wherein the senescent cell is a senescent pre-adipocyte.

14 . The method of claim 11 , wherein the src inhibitor is dasatinib.

15 . The method of claim 11 , wherein the flavonoid is a compound having a structure of the following formula (I):

or a pharmaceutically acceptable salt thereof, wherein

R 1 is —OH or —H;

R 2 is —OH or —H;

R 3 is —OH, —H, —R 6 , or —OCH 2 PO(OH) 2 ;

R 4 is —OH, —OPO(OH) 2 , —OCH 3 , —OCH 2 PO(OH) 2 , —R 6 , —H, or —OSO 3 H; and

R 5 is —OH, —H, —R 6 , or —OCH 3 ,

wherein R 6 is

16 . (canceled)

17 . The method of claim 15 wherein R 3 is —OH.

18 .- 19 . (canceled)

20 . The method of claim 15 wherein R 4 is —OH or —OSO 3 H.

21 . The method of claim 15 wherein R 5 is —OH.

22 . The method of claim 15 wherein the compound of Formula (I) is selected from the following structures and pharmaceutically acceptable salts thereof:

23 . The method of claim 1 , wherein the senolytic combination is administered during a treatment course of 1-7 days once every 0.5-12 months.

24 . The method of claim 1 , wherein the senescence associated disease or disorder is a senescence associated metabolic disorder, and the senolytic combination is administered during a treatment course of 1-7 days once every 4-12 months.

25 . The method of claim 1 , wherein the src inhibitor is dasatinib.

26 . The method of claim 1 , wherein the flavonoid is a compound having a structure of the following formula (I):

or a pharmaceutically acceptable salt thereof, wherein

R 1 is —OH or —H;

R 2 is —OH or —H;

R 3 is —OH, —H, —R 6 , or —OCH 2 PO(OH) 2 ;

R 4 is —OH, —OPO(OH) 2 , —OCH 3 , —OCH 2 PO(OH) 2 , —R 6 , —H, or —OSO 3 H; and

R 5 is —OH, —H, —R 6 , or —OCH 3 ;

wherein R 6 is

27 . The method of claim 26 , wherein the compound of Formula (I) is selected from the following structures and pharmaceutically acceptable salts thereof:

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 16, 2017
From: KIRKLAND, JAMES L.; TCHKONIA, TAMAR; ZHU, YI; PALMER, ALLYSON K.; LEBRASSEUR, NATHAN K.; MILLER, JORDAN D.
To: MAYO FOUNDATION FOR MEDICAL EDUCATION AND RESEARCH
Reel/Frame 041595/0301 →