IP Library Granted Patent US 7,446,124
Granted Patent B2
US 7,446,124 · App. 11/178,553 · Granted Nov 4, 2008

Wortmannin analogs and methods of using same in combination with chemotherapeutic agents

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Quick Facts
Patent No.
US 7,446,124
App. No.
11/178,553
Granted
Nov 4, 2008
Kind
B2
Abstract

Novel wortmannin analogs and their use in inhibiting PI-3-kinase activity in mammals and the treatment or prevention of cancer and tumor formation in a subject are described herein. Preferably, the wortmannin analogs may be administered with other chemotherapeutic agents in the treatment of cancer.

Claims (32)

1. A method of treating cancer comprising administering to a subject a pharmaceutically effective amount of a compound selected from

wherein Y is a heteroatom selected from nitrogen and sulfur and R1 and R2 are independently selected from an unsaturated alkyl, non-linear alkyl, cyclic alkyl, and substituted alkyl, and a cancer chemotherapeutic agent.

2. The method of claim 1 , wherein said R1 and R2 are a disubstituted alkyl.

3. The method of claim 1 , wherein said cancer chemotherapeutic agent is selected from the group consisting of a cytotoxic agent and an anti-tumor targeting agent.

4. The method of claim 3 , wherein said cytotoxic agent is selected from the group consisting of gemeitabine, paclitaxel, and cisplatin.

5. The method of claim 3 , wherein said anti-tumor targeting agent is selected from the group consisting of gefitinib, erlotinib, trastuzumab, cetuximab and bevacizumab.

6. The method of claim 1 , wherein said compound is selected from:

7. The method of claim 1 , wherein said compound is:

8. The method of claim 1 , wherein said compound is:

9. The method of claim 1 , wherein said compound is administered orally.

10. The method of claim 1 , wherein said compound is administered intravenously.

11. The method of claim 1 , wherein said compound is

and said chemotherapeutic agent is gefitinib.

12. The method of claim 1 , wherein said compound is

and said chemotherapeutic agent is bevacizumab.

13. The method of claim 1 , wherein said compound is

and said chemotherapeutic agent is gefitinib.

14. The method of claim 1 , wherein said compound is

and said chemotherapeutic agent is bevacizumab.

15. The method of claim 1 , further comprising administering an antihyperglycemic agent.

16. A composition comprising a compound of the formula selected from

wherein Y is a heteroatom selected from nitrogen and sulfur and R1 and R2 are independently selected from an unsaturated alkyl, non-linear alkyl, cyclic alkyl, and substituted alkyl, and a cancer chemotherapeutic agent.

17. The composition of claim 16 , wherein said compound is

18. The composition of claim 16 , wherein said compound is

19. A method of treating cancer comprising administering to a subject a pharmaceutically effective amount of a compound selected from

wherein Y is a heteroatom selected from nitrogen and sulfur and R1 and R2 are indepdently selected from an unsaturated alkyl, non-linear alkyl, cyclic alkyl, and substituted alkyl, and radiation.

20. The method of claim 19 , wherein said R1 and R2 are a disubstituted alkyl.

21. The method of claim 19 , wherein said compound is selected from

22. The method of claim 19 , wherein said compound is:

23. The method of claim 19 , wherein said compound is:

24. The method of claim 19 , wherein said compound is administered orally.

25. The method of claim 19 , wherein said compound is administered intravenously.

Assignments (4)
CONFIRMATORY LICENSE Recorded Mar 11, 2009
From: UNIVERSITY OF ARIZONA
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 022368/0710 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 2, 2005
From: KIRKPATRICK, LYNN
To: PROLX PHARMACEUTICALS CORP.
Reel/Frame 016842/0429 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 2, 2005
From: WIPF, PETER
To: THE UNIVERSITY OF PITTSBURGH
Reel/Frame 016843/0090 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 2, 2005
From: POWIS, GARTH
To: ARIZONA BOARD OF REGENTS, ACTING ON BEHALF OF THE UNIVERSITY OF ARIZONA
Reel/Frame 016843/0119 →