IP Library Granted Patent US 9,670,236
Granted Patent B2
US 9,670,236 · App. 14/439,855 · Granted Jun 6, 2017

Class of HDAC inhibitors expands the renal progenitor cells population and improves the rate of recovery from acute kidney injury

Inventors: Neil Hukriede (Allison Park, PA); Billy W. Day (Pittsburgh, PA); Lee A. McDermott (Pittsburgh, PA)
Assignee: University of Pittsburgh—Of the Commonwealth System of Higher Education
C07F9/4841C07C317/22C07C317/44C07C321/28C07C323/16C07C323/20C07C323/47C07C323/52C07C323/60C07C323/62C07D213/75
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Quick Facts
Patent No.
US 9,670,236
App. No.
14/439,855
Granted
Jun 6, 2017
Kind
B2
Abstract

Compounds and compositions are provided that inhibit histone deacylase activity and which expand renal progenitor cell populations and improve kidney function in a damaged kidney. Methods of use of the compounds and compositions are provided.

Claims (84)

1. A compound having the formula selected from the group consisting of:

or a pharmaceutically acceptable salt thereof.

2. The compound of claim 1 , having the formula:

or a pharmaceutically acceptable salt thereof.

3. The compound of claim 1 , having the formula:

or a pharmaceutically acceptable salt thereof.

4. The compound of claim 1 , selected from the group consisting of,

or a pharmaceutically acceptable salt thereof.

5. A compound having the formula:

in which

R is O,

R1 is methoxy or —NHR4 where R4 is OH, aminophenyl, hydroxyphenyl, hydroxypyridinyl, aminopyridinyl, alkyl hydroxypyridinyl, or haloalkyl hydroxyphenyl,

R2 is phenyl, benzyl, 4-methoxybenzyl, phenylethyl, substituted phenyl having the structure

 where R5 is methylthio, methylsulfonyl, methylsulfinyl, acetyl, 2-acetato, 3-acetato, methyl carbamoyl, or methoxycarbonyl and

R3 is —CH 2 —CH 2 —CH 2 —, —CH 2 —CH 2 —CH 2 —CH 2 —, or —CH 2 —CH 2 —CH 2 —CH 2 —CH 2 —,

or a pharmaceutically acceptable salt thereof.

6. The compound of claim 5 , in which R3 is —CH 2 —CH 2 —CH 2 —or —CH 2 —CH 2 —CH 2 —CH 2 —CH 2 —.

7. The compound of claim 5 , in which R3 is —CH 2 —CH 2 —CH 2 —CH 2 —CH 2 —.

8. The compound of claim 5 , in which R1 is methoxy.

9. The compound of claim 5 , in which R2 is benzyl, 4-methoxybenzyl, or phenylethyl.

10. The compound of claim 5 , in which R2 is

where R5 is methylthio, methylsulfonyl, methylsulfinyl, acetyl, 2-acetato, 3-acetato, methyl carbamoyl, or methoxycarbonyl.

11. The compound of claim 5 , selected from the group consisting of,

or a pharmaceutically acceptable salt thereof.

12. A compound having the formula:

in which

R is S,

R1 is NHR4 where R4 is hydroxypyridinyl, aminopyridinyl, alkyl hydroxypyridinyl, or haloalkyl hydroxyphenyl, and

R2 is phenyl, benzyl, 4-methoxybenzyl, phenylethyl, or substituted phenyl having the structure

 where R5 is 3-hydroxyl, methylthio, methylsulfonyl, methylsulfinyl, acetyl, 2-acetato, 3-acetato, carbamoyl, methyl carbamoyl, or methoxycarbonyl, and

R3 is —CH 2 —CH 2 —CH 2 —, —CH 2 —CH 2 —CH 2 —CH 2 —, or —CH 2 —CH 2 —CH 2 —CH 2 —CH 2 —,

or a pharmaceutically acceptable salt thereof.

13. The compound of claim 12 , in which R3 is —CH 2 —CH 2 —CH 2 —or —CH 2 —CH 2 —CH 2 —CH 2 —CH 2 —.

14. The compound of claim 12 , in which R2 is benzyl, phenylethyl, 4-methoxybenzyl, or

 where R5 is 3-hydroxyl, acetyl, 2-acetato, 3-acetato, carbamoyl, methyl carbamoyl, or methoxycarbonyl.

15. The compound of claim 12 , selected from the group consisting of,

or a pharmaceutically acceptable salt thereof.

16. A compound having the formula:

in which

R is S,

R1 is NHR4 where R4 is hydroxyphenyl or aminophenyl, and

R2 is substituted phenyl having the structure

 where R5 4-acetato,

R3 is —CH 2 —CH 2 —CH 2 —, —CH 2 —CH 2 —CH 2 —CH 2 —, or —CH 2 —CH 2 —CH 2 —CH 2 —CH 2 —,

or a pharmaceutically acceptable salt thereof.

17. The compound of claim 16 , in which R3 is —CH 2 —CH 2 —CH 2 —or —CH 2 —CH 2 —CH 2 —CH 2 —CH 2 —.

18. A compound having the formula:

in which

R is S,

R1 is methoxy or —NHR4 where R4 is OH, aminophenyl, hydroxyphenyl, hydroxypyridinyl, aminopyridinyl, alkyl hydroxypyridinyl, or haloalkyl hydroxyphenyl,

R2 is benzyl, phenylethyl, 4-methoxybenzyl, or

 where R5 is 3-hydroxyl, acetyl; 2-acetato, 3-acetato, carbamoyl, methyl carbamoyl, or methoxycarbonyl, and

R3 is —CH 2 —CH 2 —CH 2 —, —CH 2 —CH 2 —CH 2 —CH 2 —, or —CH 2 —CH 2 —CH 2 —CH 2 —CH 2 —,

or a pharmaceutically acceptable salt thereof.

19. The compound of claim 18 , in which R3 is —CH 2 —CH 2 —CH 2 —or —CH 2 —CH 2 —CH 2 —CH 2 —CH 2 —.

20. The compound of claim 18 , in which R1 is methoxy.

21. The compound of claim 18 , selected from the group consisting of,

or a pharmaceutically acceptable salt thereof.

22. A compound having the formula:

in which

R is S(O) or S(O) 2

R1 is methoxy or —NHR4 where R4 is OH, aminophenyl, hydroxyphenyl, hydroxypyridinyl, aminopyridinyl, alkyl hydroxypyridinyl, or haloalkyl hydroxyphenyl,

R2 is benzyl, phenylethyl, or methylsulfonylphenyl and

R3 is —CH 2 —CH 2 —CH 2 —, —CH 2 —CH 2 —CH 2 —CH 2 —, or —CH 2 —CH 2 —CH 2 —CH 2 —CH 2 —,

or a pharmaceutically acceptable salt thereof.

23. The compound of claim 22 , in which R3 is —CH 2 —CH 2 —CH 2 —or —CH 2 —CH 2 —CH 2 —CH 2 —CH 2 —.

24. The compound of claim 22 , in which R1 is methoxy.

25. The compound of claim 22 , selected from the group consisting of,

or a pharmaceutically acceptable salt thereof.

26. A compound having the formula:

in which

R is P(O)(CH 3 ) or P(O)(OCH 3 ),

R1 is methoxy or —NHR4 where R4 is OH, aminophenyl, hydroxyphenyl, hydroxypyridinyl, aminopyridinyl, alkyl hydroxypyridinyl, or haloalkyl hydroxyphenyl,

R2 is phenyl, benzyl, 4-methoxybenzyl, phenylethyl, substituted phenyl having the structure

 where R5 is 3-hydroxyl, methylthio, methylsulfonyl, methylsulfinyl, acetyl, 2-acetato, 3-acetato, carbamoyl, methyl carbamoyl, or methoxycarbonyl and

R3 is —CH 2 —CH 2 —CH 2 —, —CH 2 —CH 2 —CH 2 —CH 2 —, or —CH 2 —CH 2 —CH 2 —CH 2 —CH 2 —,

or a pharmaceutically acceptable salt thereof.

27. The compound of claim 26 , in which R3 is —CH 2 —CH 2 —CH 2 —or —CH 2 —CH 2 —CH 2 —CH 2 —CH 2 —.

28. The compound of claim 26 , in which R1 is methoxy.

29. The compound of claim 26 , in which R2 is benzyl, 4-methoxybenzyl, or phenylethyl.

30. The compound of claim 26 , in which R2 is

where R5 is 3-hydroxyl, methylthio, methylsulfonyl, methylsulfinyl, acetyl, 2-acetato, 3-acetato, carbamoyl, methyl carbamoyl, or methoxycarbonyl.

31. The compound of claim 26 , selected from the group consisting of,

or a pharmaceutically acceptable salt thereof.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 5, 2016
From: HUKRIEDE, NEIL; DAY, BILLY W.; MCDERMOTT, LEE A.
To: UNIVERSITY OF PITTSBURGH-OF THE COMMONWEALTH SYSTEM OF HIGHER EDUCATION
Reel/Frame 038479/0399 →
CONFIRMATORY LICENSE Recorded Aug 3, 2015
From: UNIVERSITY OF PITTSBURGH
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 036245/0720 →
Continuity (2)
Provisional Application 61720621 · Oct 31, 2012
Related Publication 20150246939A1 · Sep 3, 2015