IP Library Granted Patent US 8,729,286
Granted Patent B2
US 8,729,286 · App. 13/468,477 · Granted May 20, 2014

Platinum compounds as treatment for cancers, and related methods, kits, and compositions

Inventors: Stephen J. Lippard (Cambridge, MA); Justin J. Wilson (Cambridge, MA)
Assignee: Massachusetts Institute of Technology
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Quick Facts
Patent No.
US 8,729,286
App. No.
13/468,477
Granted
May 20, 2014
Kind
B2
Abstract

The present invention is a platinum(II) compound comprising a beta-diketonate ligand represented by the following general formula: Or general formula: wherein R 1 and R 2 are independently selected from the group consisting of alkyl optionally substituted, heteroalkyl optionally substituted, and aryl optionally substituted; R 3 and R 4 are independently selected from the group consisting of ammonia, an optionally substituted heterocycle including at least one nitrogen, and an optionally substituted amine, or R 3 and R 4 can be joined together to form a bidentate ligand Z and Y are independently selected from the group consisting of O and S, provided at least one of Z and Y is S; and X— is a counterion. These compounds are useful in the treatment of cancer.

Claims (39)

1. A compound having the structure:

wherein X − is a counterion.

2. A compound having the structure:

wherein:

R 1 and R 2 are independently selected from the group consisting of alkyl optionally substituted, heteroalkyl optionally substituted, and aryl optionally substituted, provided at least one of R 1 or R 2 is not alkyl or haloalkyl;

R 3 and R 4 are independently selected from the group consisting of ammonia, an optionally substituted heterocycle including at least one nitrogen, and an optionally substituted amine, or R 3 and R 4 can be joined together to form a bidentate ligand;

and

X − is a counterion.

3. A compound having the structure:

wherein:

R 1 and R 2 are independently selected from the group consisting of alkyl optionally substituted, heteroalkyl optionally substituted, and aryl optionally substituted, provided at least one of R 1 or R 2 is aryl optionally substituted;

R 3 and R 4 are independently selected from the group consisting of ammonia, an optionally substituted heterocycle including at least one nitrogen, and an optionally substituted amine, or R 3 and R 4 can be joined together to form a bidentate ligand;

and

X − is a counterion.

4. A compound having the structure:

wherein:

R 1 and R 2 are independently selected from the group consisting of alkyl optionally substituted, heteroalkyl optionally substituted, and aryl optionally substituted; and

R 3 and R 4 are independently selected from the group consisting of ammonia an optionally substituted heterocycle including at least one nitrogen, and an optionally substituted amine;

X − is a counterion.

5. A compound having the structure:

wherein:

R 1 and R 2 are independently selected from the group consisting of alkyl optionally substituted, heteroalkyl optionally substituted, and aryl optionally substituted;

R 3 and R 4 are independently selected from the group consisting of ammonia, an optionally substituted heterocycle including at least one nitrogen, and an optionally substituted amine, or R 3 and R 4 can be joined together to form a bidentate ligand;

Z and Y are independently selected from the group consisting of O and S, provided at least one of Z and Y is S; and

X − is a counterion.

6. The compound of claim 2 , wherein at least one of R 1 or R 2 is not alkyl or haloalkyl.

7. The compound of claim 2 , wherein at least one of R 3 and R 4 is NH 3 .

8. The compound of claim 2 , wherein each of R 3 and R 4 is NH 3 .

9. The compound of claim 2 , wherein R 3 and R 4 are independently selected from the group consisting of ammonia and an optionally substituted amine, and are not joined together to form a bidentate ligand.

10. The compound of claim 2 , wherein at least one of R 1 or R 2 is aryl optionally substituted.

11. The compound of claim 2 , wherein at least one of R 1 or R 2 is not methyl or —CF 3 .

12. The compound of claim 2 , wherein at least one of R 1 is —CH 3 or —CF 3 and R 2 is aryl, optionally substituted.

13. The compound of claim 2 , wherein each of R 1 and R 2 is aryl, optionally substituted.

14. The compound of claim 5 , wherein Z is O and Y is S.

15. The compound of claim 5 , wherein Z is S and Y is O.

16. The compound of claim 5 , wherein each of Z and Y is S.

17. A pharmaceutical composition, comprising:

a compound as in claim 5 ; and

one or more pharmaceutically acceptable carriers, additives, and/or diluents.

Assignments (2)
CONFIRMATORY LICENSE Recorded May 3, 2013
From: MASSACHUSETTS INSTITUTE OF TECHNOLOGY
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 030342/0579 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 3, 2012
From: LIPPARD, STEPHEN J.; WILSON, JUSTIN J.
To: MASSACHUSETTS INSTITUTE OF TECHNOLOGY
Reel/Frame 029067/0297 →
Continuity (1)
Related Publication 20130303606A1 · Nov 14, 2013