IP Library Granted Patent US 7,605,288
Granted Patent B2
US 7,605,288 · App. 11/728,393 · Granted Oct 20, 2009

Heat shock protein 90 inhibitors

Assignee: University of Kansas
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Quick Facts
Patent No.
US 7,605,288
App. No.
11/728,393
Granted
Oct 20, 2009
Kind
B2
Abstract

Novel compounds useful for inhibiting the 90 kDa heat shock proteins containing a quinone-like moiety and a di-hydroxy phenol like moiety, similar to geldanamycin and radicicol.

Claims (96)

1. Compounds corresponding to Formula I:

wherein A is hydrogen, halogen, lower alkyl, lower alkoxy, aryl, aralyl, or allyl;

wherein B is hydroxy, amino, halogen, lower alkoxy, or aralkoxy;

wherein C is hydroxy, amino, or lower alkoxy;

wherein D is alkyl, oxygen, amino, sulfanyl, sulfenyl, or sulfonyl;

wherein E is halogen, hydroxy, lower alkoxy, amino, or allyl amine;

wherein F is hydroxy, halogen, thiol, lower alkoxy, amino or oxidized to form a ketone;

wherein G is amino, thiol, hydroxy, lower alkoxy, or oxidized to form a ketone;

wherein I is amino;

wherein J is carbonyl;

wherein M is alkyl or cycloalkyl;

wherein K is alkyl or cycloalkyl; and

wherein R is hydrogen or alkyl.

2. The compounds according to claim 1 ,

wherein A is halogen;

wherein B and C are both hydroxy;

wherein D is oxygen;

wherein E is lower alkoxy;

wherein F and G are both oxidized to form a quinone;

wherein K is alkyl;

wherein I is amino comprising —NH—;

wherein J is carbonyl; and

wherein M is lower alkyl.

3. The compounds according to claim 1 ,

wherein A is halogen;

wherein B and C are both hydroxy;

wherein D is oxygen;

wherein E is lower alkoxy;

wherein F and G are both hydroxy;

wherein I is amino comprising —NH—;

wherein J is carbonyl;

wherein K is alkyl; and

wherein M is lower alkyl.

4. The compounds according to claim 1 ,

wherein A is halogen;

wherein B and C are both hydroxy;

wherein D is oxygen;

wherein E, F, and G are all lower alkoxy;

wherein I is amino comprising —NH—;

wherein J is carbonyl;

wherein K is alkyl; and

wherein M is lower alkyl.

5. The compounds according to claim 1 ,

wherein A is halogen;

wherein B and C are both hydroxy;

wherein D is oxygen;

wherein E is allyl amine;

wherein F and G are both oxidized to form a quinone;

wherein I is amino comprising —NH—;

wherein J is carbonyl,

wherein K is alkyl; and

wherein M is lower alkyl.

6. The compounds according to claim 1 ,

wherein A is phenyl;

wherein B and C are both hydroxy;

wherein D is oxygen;

wherein E, F, and G are all lower alkoxy;

wherein I is amino comprising —NH—;

wherein J is carbonyl;

wherein K is alkyl; and

wherein M is lower alkyl.

7. The compounds according to claim 1 ,

wherein A is halogen;

wherein B is lower alkoxy;

wherein C is hydroxy;

wherein D is oxygen;

wherein E, F, and G are all lower alkoxy;

wherein I is amino comprising —NH—;

wherein J is carbonyl;

wherein K is alkyl; and

wherein M is lower alkyl.

8. The compounds according to claim 1 ,

wherein A is halogen;

wherein B and C are both hydroxy;

wherein D is oxygen;

wherein E, F, and G are all lower alkoxy;

wherein I is amino comprising the formula —NR 1 — and wherein R 1 is alkyl;

wherein J is carbonyl;

wherein K is alkyl; and

wherein M is lower alkyl.

9. The compounds according to claim 1 ,

wherein A is halogen;

wherein B and C are both hydroxy;

wherein D is oxygen;

wherein E, F, and G are all lower alkoxy;

wherein I is amino comprising —NH—;

wherein J is carbonyl;

wherein K is lower alkyl; and

wherein M is lower alkyl.

10. The compounds according to claim 1 wherein both G and F are oxidized to form a quinone.

11. The compounds according to claim 1 wherein B and C are both hydroxy.

12. The compounds according to claim 1 wherein A is halogen.

13. The compounds according to claim 1 wherein R is hydrogen.

14. The compounds according to claim 1 wherein G and F are both hydroxy.

15. The compounds according to claim 1 wherein E, F, and G are each lower alkoxy.

16. The compounds according to claim 1 wherein F and G are oxidized to form a quinone, and E is allyl amine.

Assignments (1)
CONFIRMATORY LICENSE Recorded Sep 14, 2010
From: UNIVERSITY OF KANSAS LAWRENCE
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 024980/0065 →
Continuity (2)
Division 1097608200 · Oct 27, 2004
Related Publication 20070197787A1 · Aug 23, 2007