IP Library Granted Patent US 10,751,310
Granted Patent B2
US 10,751,310 · App. 16/081,791 · Granted Aug 25, 2020

Prevention, treatment and reversal of disease using therapeutically effective amounts of dicarboxylic acid compounds

Inventors: Bruce A. Freeman (Pittsburgh, PA); Francisco J. Schopfer (Pittsburgh, PA)
Assignee: University of Pittsburgh—Of the Commonwealth System of Higher Education
A61K31/194A61K9/0073C07C323/52A61K9/0019A61K9/0034A61K9/0053A61K31/225
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Quick Facts
Patent No.
US 10,751,310
App. No.
16/081,791
Granted
Aug 25, 2020
Kind
B2
Abstract

Various embodiments of this invention are directed to pharmaceutical compositions and methods for treating disease. The compositions of such embodiments include dicarboxylic acid compounds containing electron withdrawing groups, alkyl esters of dicarboxylic acids containing electron withdrawing groups, or compounds of Formulae I to X. The methods of various embodiments include administering an effective amount of any of these pharmaceutical compositions to a patient in need of treatment.

Claims (61)

1. A compound comprising a dicarboxylic acid having the structure:

wherein X is acyl, carboxylic acid, an ester, a halogen, fluoromethyl, —CN, sulfonyl, sulfone, sulfonic acid, primary ammonium, secondary ammonium, tertiary ammonium, or −NO 2 ,

m is from 1 to 10; and

n is from 1 to 10.

2. A compound comprising a dicarboxylic acid having the structure:

wherein X is acyl, carboxylic acid, an ester, a halogen, fluoromethyl, —CN, sulfonyl, sulfone, sulfonic acid, primary ammonium, secondary ammonium, tertiary ammonium, or —NO 2 ;

Y and Z are each, independently, hydrogen or a C 1 to C 10 alkyl;

m is from 1 to 10; and

n is from 1 to 10.

3. A compound comprising a dicarboxylic acid having the structure:

wherein X is an electron withdrawing group;

Y and Z are each, independently, hydrogen or C 1 to C 10 alkyl;

p and t are each, independently, 1 to 10;

s is absent or 1 to 10, and

r is 1.

4. A pharmaceutical composition comprising a therapeutically effective amount of a compound selected from a compound of Formulae III, VII or IX, and a pharmaceutically acceptable excipient, wherein Formulae III, VII or IX are:

wherein X is an electron withdrawing group,

m is from 1 to 10; and

n is from 1 to 10;

wherein X is an electron withdrawing group;

Y and Z are each, independently, hydrogen or a C 1 to C 10 alkyl;

m is from 1 to 10; and

n is from 1 to 10;

wherein X is an electron withdrawing group;

Y and Z are each, independently, hydrogen or C 1 to C 10 alkyl;

p and t are each, independently, 1 to 10;

s is absent or 1 to 10, and

r is 1 to 5.

5. The composition of claim 4 , wherein said therapeutically effective amount is from about 25 milligrams to less than 450 milligrams.

6. The composition of claim 4 , wherein said therapeutically effective amount is from about 100 milligrams to about 300 milligrams.

7. The composition of claim 4 , wherein said therapeutically effective amount is from about 100 milligrams to about 200 milligrams.

8. The composition of claim 4 , wherein said therapeutically effective amount is about 150 milligrams.

9. The compound of claim 1 , wherein X is NO 2 .

10. The compound of claim 2 , wherein X is NO 2 .

11. The compound of claim 3 , wherein X is NO 2 .

12. The compound of claim 1 , wherein m is 2 and n is 1.

13. The compound of claim 2 , wherein m is 2 and n is 1.

14. The compound of claim 2 , wherein Y is a C 1 -C 3 alkyl and Z is a C 1 -C 3 alkyl.

15. The compound of claim 10 , wherein Y is a C 1 -C 3 alkyl and Z is a C 1 -C 3 alkyl.

16. The compound of claim 2 , wherein Y is ethyl or methyl and Z is ethyl or methyl.

17. The compound of claim 10 , wherein Y is ethyl or methyl and Z is ethyl or methyl.

18. The compound of claim 1 , wherein X is CN.

19. The compound of claim 2 , wherein X is CN.

20. The compound of claim 3 , wherein X is CN.

21. The compound of claim 1 , wherein X is Cl, Br or F.

22. The compound of claim 1 , wherein X is Cl, Br or F.

23. The compound of claim 3 , wherein X is Cl, Br or F.

24. The compound of claim 12 , wherein X is NO 2 .

25. The composition of claim 4 , wherein X is NO 2 in Formulae III, VII or IX.

26. The composition of claim 4 , wherein X is CN in Formulae III, VII or IX.

27. The composition of claim 4 , wherein X is Cl, Br or F in Formulae III, VII or IX.

28. The composition of claim 4 , wherein m is 2 and n is 1 in Formulae III or VII.

29. The composition of claim 4 , wherein Y is a C 1 -C 3 alkyl and Z is a C 1 -C 3 alkyl in Formulae VII or IX.

30. The composition of claim 4 , wherein Y is ethyl or methyl and Z is ethyl or methyl in Formulae VII or IX.

31. The composition of claim 4 , wherein the compound is a compound of Formulae III.

32. The composition of claim 4 , wherein the compound is a compound of Formulae VII.

33. The composition of claim 4 , wherein the compound is a compound of Formulae IX.

34. The composition of claim 4 , wherein X is acyl, carboxylic acid, an ester, a halogen, fluoromethyl, —CN, sulfonyl, sulfone, sulfonic acid, primary ammonium, secondary ammonium, tertiary ammonium, or —NO 2 in Formulae III, VII or IX.

35. The composition of claim 25 , wherein the compound is a compound of Formulae III.

36. The composition of claim 25 , wherein the compound is a compound of Formulae VII.

37. The composition of claim 25 , wherein the compound is a compound of Formulae IX.

Assignments (2)
CONFIRMATORY LICENSE Recorded Dec 13, 2018
From: UNIVERSITY OF PITTSBURGH
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 047818/0671 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 7, 2018
From: FREEMAN, BRUCE A.; SCHOPFER, FRANCISCO J.
To: UNIVERSITY OF PITTSBURGH - OF THE COMMONWEALTH SYSTEM OF HIGHER EDUCATION
Reel/Frame 046816/0364 →
Continuity (2)
Provisional Application 62303960 · Mar 4, 2016
Related Publication 20190091186A1 · Mar 28, 2019
Cited By (2)
US 12,390,435 US 12,728,111