IP Library Granted Patent US 10,508,092
Granted Patent B2
US 10,508,092 · App. 15/689,378 · Granted Dec 17, 2019

Synthesis of novel analogs of diptoindonesin G, compounds formed thereby, and pharmaceutical compositions containing them

Inventors: Wei Xu (Middleton, WI); Weiping Tang (Middleton, WI); Jitian Liu (Madison, WI); Jill Kolesar (Middleton, WI)
Assignee: Wisconsin Alumni Research Foundation
C07D307/79C07D307/77
View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 10,508,092
App. No.
15/689,378
Granted
Dec 17, 2019
Kind
B2
Abstract

Disclosed are unnatural analogs of Diptoindonesin G, methods to make the analogs, pharmaceutical compositions containing the analogs, and methods of using the analogs to inhibit neoplastic cell growth.

Claims (43)

1. A compound selected from the group consisting of:

wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , and R 8 are independently selected from the group consisting of —H, —OH, —OR 10 , —NH 2 , —NHR 10 , and —NR 10 R 11 , wherein R 10 and R 11 are independently selected from the group consisting of C 1 -C 6 -alkyl, provided that R 1 , R 2 , and R 4 are not simultaneously —OH or —OR 10 ; and further provided that at least one of R 6 , R 7 , or R 8 is —OH;

R 9 is —O—, —NH—, or —S—; and

salts thereof.

2. The compound of claim 1 , wherein the salts are pharmaceutically suitable salts.

3. A compound selected from the group consisting of:

wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , and R 8 are independently selected from the group consisting of —H, —OH, —OR 10 , —NH 2 , —NHR 10 , and —NR 10 R 11 , wherein R 10 and R 11 are independently selected from the group consisting of C 1 -C 6 -alkyl, provided that R 1 , R 2 , and R 4 are not simultaneously —OH or —OR 10 , and further provided that at least one of R 1 , R 3 , R 4 , or R 5 is —OH, and at least one of R 6 , R 7 , or R 8 is —OH; and

wherein R 9 is —O—; and

salts thereof.

4. The compound of claim 3 , wherein R 1 is —OH.

5. The compound of claim 3 , wherein R 2 is —OH.

6. The compound of claim 3 , wherein R 3 is —OH.

7. The compound of claim 3 , wherein R 4 is —OH.

8. The compound of claim 3 , wherein R 5 is —OH.

9. The compound of claim 3 , wherein R 6 is —OH.

10. The compound of claim 3 , wherein R 7 is —OH.

11. The compound of claim 3 , wherein R 8 is —OH.

12. A compound selected from the group consisting of:

wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , and R 8 are independently selected from the group consisting of —H, —OH, —OR 10 , —NH 2 , —NHR 10 , and —NR 10 R 11 , provided that at least one of R 1 , R 2 , R 3 , R 4 , R 5 is —OH, and at least one of R 6 , R 7 , and R 8 is —OH, wherein R 10 and R 11 are independently selected from the group consisting of C 1 -C 6 -alkyl, and provided that R 1 , R 2 , R 4 , and R 6 are not simultaneously —OH;

wherein R 9 is —NH—; and

salts thereof.

13. The compound of claim 12 , wherein R 1 is —OH.

14. The compound of claim 12 , wherein R 2 is —OH.

15. The compound of claim 12 , wherein R 3 is —OH.

16. The compound of claim 12 , wherein R 4 is —OH.

17. The compound of claim 12 , wherein R 5 is —OH.

18. The compound of claim 12 , wherein R 6 is —OH.

19. The compound of claim 12 , wherein R 7 is —OH.

20. The compound of claim 12 , wherein R 8 is —OH.

21. A compound selected from the group consisting of:

wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , and R 8 are independently selected from the group consisting of —H, —OH, —OR 10 , —NH 2 , —NHR 10 , and —NR 10 R 11 , wherein R 10 and R 11 are independently selected from the group consisting of C 1 -C 6 -alkyl, provided that R 1 , R 2 , R 4 , and R 6 are not simultaneously —OH; and

wherein R 9 is —S—; and

salts thereof.

22. The compound of claim 21 , wherein R 1 is —OH.

23. The compound of claim 21 , wherein R 2 is —OH.

24. The compound of claim 21 , wherein R 3 is —OH.

25. The compound of claim 21 , wherein R 4 is —OH.

26. The compound of claim 21 , wherein R 5 is —OH.

27. The compound of claim 21 , wherein R 6 is —OH.

28. The compound of claim 21 , wherein R 7 is —OH.

29. The compound of claim 21 , wherein R 8 is —OH.

30. A pharmaceutical composition comprising a compound as recited in claim 1 , in combination with a pharmaceutically suitable delivery vehicle.

31. A method of inhibiting neoplastic cell growth, the method comprising contacting a neoplastic cell or a cell suspected of being neoplastic with a growth inhibiting-effective amount of a compound as in claim 1 .

Assignments (2)
CONFIRMATORY LICENSE Recorded Nov 15, 2019
From: WISCONSIN ALUMNI RESEARCH FOUNDATION
To: THE GOVERNMENT OF THE UNITED STATES, AS REPRESENTED BY THE SECRETARY OF THE ARMY
Reel/Frame 051035/0865 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 18, 2017
From: XU, WEI; KOLESAR, JILL; LIU, JITIAN; TANG, WEIPING
To: WISCONSIN ALUMNI RESEARCH FOUNDATION
Reel/Frame 043611/0203 →
Continuity (2)
Provisional Application 62382987 · Sep 2, 2016
Related Publication 20180065945A1 · Mar 8, 2018