IP Library Granted Patent US 9,877,936
Granted Patent B2
US 9,877,936 · App. 14/921,124 · Granted Jan 30, 2018

Quinone compounds for treating Ape1 mediated diseases

Inventors: Mark R. Kelley (Zionsville, IN); James H. Wikel (Greenwood, IN)
Assignees: INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATION; APEXIAN PHARMACEUTICALS, INC.
A61K31/165A61K31/185A61K31/45A61K31/495A61K31/5375C07C235/78C07C259/06C07D211/76C07D295/185C07D295/192C07C2602/10
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Quick Facts
Patent No.
US 9,877,936
App. No.
14/921,124
Granted
Jan 30, 2018
Kind
B2
Abstract

The invention described herein pertains to compounds and compositions for treating Ape1 mediated diseases. In particular, the invention described herein pertains to quinone compounds and pharmaceutical compositions containing them for treating mediated diseases.

Claims (28)

1. A method for treating a disease responsive to Ape1 inhibition in a host animal, the method comprising administering to the host animal a composition comprising a therapeutically effective amount of a compound of the formula

or a pharmaceutically acceptable salt thereof, wherein:

R A represents a fused aryl ring that is optionally substituted;

R is hydrogen or halo, or alkyl, heteroalkyl, cycloalkyl, cycloheteroalkyl, alkoxy, heteroalkoxy cycloalkoxy, cycloheteroalkoxy, alkylthio, heteroalkylthio cycloalkylthio, or cycloheteroalkylthio, each of which is optionally substituted;

X is alkylene, alkenylene, or alkynylene, each of which is optionally substituted; and

Y is N(R 1 ) 2 , NHOR 2 , or NR 2 OR 2 , where each R 1 is independently selected from the group consisting of alkyl, heteroalkyl, cycloalkyl, and cycloheteroalkyl, each of which is optionally substituted, or both R 1 are taken together with the attached nitrogen to form an optionally substituted heterocycle; where each R 2 is independently selected from the group consisting of hydrogen, alkyl, heteroalkyl, cycloalkyl, and cycloheteroalkyl, each of which is optionally substituted, and a prodrug group, or both R 2 are taken together with the attached nitrogen and oxygen to form an optionally substituted heterocycle.

2. The method of claim 1 , wherein R A represents optionally substituted benzo.

3. The method of claim 1 , wherein R is alkyl or heteroalkyl, each of which is optionally substituted.

4. The method of claim 1 , wherein R is optionally substituted alkyl.

5. The method of claim 1 , wherein R is alkoxy.

6. The method of claim 1 , wherein R is alkylthio.

7. The method of claim 1 , wherein R is halo.

8. The method of claim 1 , wherein each R 1 is optionally substituted alkyl.

9. The method of claim 1 , wherein one R 1 is polyhydroxyalkyl.

10. The method of claim 1 , wherein both R 1 are taken together with the attached nitrogen to form an optionally substituted heterocycle selected from the group consisting of pyrrolidine, piperidine, piperazine, morpholine, pyrrolidinone, piperidinone, piperazinone, and morpholinone.

11. The method of claim 1 , wherein at least one R 2 is hydrogen.

12. The method of claim 1 , wherein at least one R 2 is alkyl.

13. The method of claim 1 , wherein both R 2 are alkyl.

14. The method of claim 1 , wherein both R 2 are taken together with the attached nitrogen and oxygen to form an optionally substituted heterocycle selected from the group consisting of oxazolidine, oxazine, oxazapine, oxazolidinone, oxazinone, and oxazapinone.

15. The method of claim 1 , wherein X is optionally substituted alkylene.

16. The method of claim 1 , wherein X is optionally substituted alkenylene.

17. The method of claim 1 , wherein X is optionally substituted alkynylene.

18. The method of claim 1 , wherein the compound has the formula

or a pharmaceutically acceptable salt thereof.

19. The method of claim 1 , wherein the compound has the formula

or a pharmaceutically acceptable salt thereof.

20. The method of claim 1 , wherein the compound has the formula

or a pharmaceutically acceptable salt thereof.

Assignments (5)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 25, 2022
From: KELLEY, MARK R.; WIKEL, JAMES H.
To: INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATION
Reel/Frame 059101/0877 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 25, 2022
From: INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATION
To: APEX THERAPEUTICS, INC.
Reel/Frame 059102/0244 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 25, 2022
From: KELLEY, MARK R; WIKEL, JAMES H.
To: INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATION
Reel/Frame 059102/0345 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 25, 2022
From: APEX THERAPEUTICS, INC.
To: APEXIAN PHARMACEUTICALS, INC.
Reel/Frame 059102/0639 →
CHANGE OF NAME Recorded Jun 28, 2017
From: APEX THERAPEUTICS, INC.
To: APEXIAN PHARMACEUTICALS, INC.
Reel/Frame 043019/0829 →
Continuity (3)
Continuation 14119949
Provisional Application 61490141 · May 26, 2011
Related Publication 20160045461A1 · Feb 18, 2016