IP Library Granted Patent US 8,748,464
Granted Patent B2
US 8,748,464 · App. 12/838,247 · Granted Jun 10, 2014

Use of SIRT1 activators or inhibitors to modulate an immune response

Inventors: Eric M. Verdin (San Francisco, CA); Melanie Ott (San Francisco, CA); Hye-Sook Kwon (San Mateo, CA); Hyungwook Lim (San Francisco, CA)
Assignee: The J. David Gladstone Institutes
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Quick Facts
Patent No.
US 8,748,464
App. No.
12/838,247
Granted
Jun 10, 2014
Kind
B2
Abstract

The present disclosure provides a method of increasing an immune response in an individual, the method involving administering to an individual in need thereof an inhibitor of SIRT1. The present disclosure provides a method of reducing an immune response, e.g., to treat chronic immune hyperactivity, the method generally involving administering to an individual in need thereof an activator of SIRT1. The present disclosure provides a method of modulating activation and differentiation of CD4 + T cells.

Claims (24)

1. A method of treating chronic immune hyperactivity in an individual, the method comprising administering to an individual having chronic immune hyperactivity an effective amount of a SIRT1 activator, wherein the SIRT1 activator is a compound of the formula:

or a salt thereof, wherein

R 19 is selected from:

wherein:

each Z 10 , Z 11 , Z 12 and Z 13 is independently selected from N, CR 20 or CR 1 ′; and

each Z 14 , Z 15 and Z 16 is independently selected from N, NR 1 ′, S, O, CR 20 , or CR 1 ′,

wherein:

zero to two of Z 10 , Z 11 , Z 12 or Z 13 are N;

at least one of Z 14 , Z 15 and Z 16 is N, NR 1 ′, S or O;

zero to one of Z 14 , Z 15 and Z 16 is S or O;

zero to two of Z 14 , Z 15 and Z 16 is N or NR 1 ′;

zero to one R 30 is a solubilizing group; and

zero to one R 1 ′ is an optionally substituted C 1 -C 3 straight or branched alkyl;

each R 20 is independently selected from H or a solubilizing group;

R 21 is selected from —NR 1 ′—C(O)—, —NR 1 ′—S(O) 2 —, —NR 1 ′—C(O)—NR 1 ′—, —NR 1 ′—C(S)—NR 1 ′—NR 1 ′—C(S)— NR 1 ′—CR 1 ′R 1 ′—, —NR 1 ′—C(O)—CR 1 ′R 1 ′—NR 1 ′—, —NR 1 ′—C(═NR 1 ′)—NR 1 ′—, —C(O)—NR 1 ′—C(O)—NR 1 ′—, —CR 1 ′R 1 ′—, —NR 1 ′—C(O)—C(O)—CR 1 ′═CR 1 ′—, —NR 1 ′—S(O) 2 —NR 1 ′–—NR 1 ′—C(O)—NR 1 ′—S(O) 2 —, —NR 1 ′—CR 1 ′R 1 ′—C(O)—NR 1 ′—, —CR 1 ′R 1 ′—C(O)—NR 1 ′—, —NR 1 ′—C(O)—CR 1 ′═CR 1 ′—CR 1 ′R 1 ′—, —NR 1 ′—C(═N—CN)—NR 1 ′—, —NR 1 ′—C(O)—CR 1 ′R 1 ′—O—, —NR 1 ′—C(O)—CR 1 ′R 1 —CR 1 ′R 1 ′—O—, —NR 1 ′—S(O) 2 —CR 1 ′R 1 ′—, —NR 1 ′—S(O) 2 —CR 1 ′R 1 ′—CR 1 ′R 1 ′—, —NR 1 ′— C(O)—CR 1 ′R 1 ′—; —NR 1 ′—C(O)—CR 1 ′R′ 1 —CR 1 ′R′ 1 —, —NR 1 ′—C(S)—NR 1 ′—CR 1 ′R′ 1 —CR 1 ′R′ 1 —, —NR 1 ′—C(O)—O—,

wherein each R 1 ′ is independently selected from H or optionally substituted C 1 -C 3 straight or branched alkyl; and

R 31 is selected from an optionally substituted monocyclic or bicyclic aryl, or an optionally substituted monocyclic or bicyclic heteroaryl,

wherein the chronic immune hyperactivity results from an immunodeficiency virus infection.

2. The method of claim 1 , wherein the individual is a human.

3. The method of claim 1 , wherein the immunodeficiency virus infection is a human immunodeficiency virus-1 (HIV-1) infection.

4. The method of claim 3 , further comprising administering to the individual at least one additional therapeutic agent that treats the HIV-1 infection.

5. The method of claim 1 , wherein the SIRT1 activator is a selective SIRT1 activator.

6. The method of claim 1 , wherein the SIRT1 activator is a compound of the formula:

7. The method of claim 1 , wherein the SIRT1 activator is administered orally.

Assignments (2)
CONFIRMATORY LICENSE Recorded Mar 4, 2011
From: J. DAVID GLADSTONE INSTITUTES
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 025898/0876 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 10, 2010
From: VERDIN, ERIC M.; OTT, MELANIE; KWON, HYE-SOOK; LIM, HYUNGWOOK
To: THE J. DAVID GLADSTONE INSTITUTES
Reel/Frame 024969/0574 →
Continuity (3)
Continuation In Part PCTUS2009000761 · Feb 5, 2009
Provisional Application 61026997 · Feb 7, 2008
Related Publication 20100330114A1 · Dec 30, 2010