IP Library Granted Patent US 10,098,955
Granted Patent B2
US 10,098,955 · App. 15/662,612 · Granted Oct 16, 2018

Pharmaceutical formulations containing lipoic acid derivatives

Inventors: Robert G. L. Shorr (Edison, NJ); Robert J. Rodriguez (West Windsor, NJ); Rajinder Bhasin (Coram, NY)
Assignee: Rafael Pharmaceuticals, Inc.
A61K47/18A61K31/19A61K31/20A61K31/381A61K45/06A61K47/183A61K47/22A61K47/36A61K47/541Y02A50/409Y02A50/475Y02A50/479
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Quick Facts
Patent No.
US 10,098,955
App. No.
15/662,612
Granted
Oct 16, 2018
Kind
B2
Abstract

Pharmaceutical formulations containing lipoic acid derivatives and ion pairs thereof are described. The pharmaceutical formulations are useful in the treatment of medical disorders, such as cancer.

Claims (28)

1. A method of treating a cancer selected from the group consisting of carcinoma, sarcoma, myeloma, lymphoma, leukemia and cancer of the pancreas, comprising the step of intravenously administering to a human patient in need thereof a pharmaceutical formulation comprising:

a) therapeutically effective amount of a compound of Formula I:

and

b) at least one ion pairing agent.

2. The method of claim 1 , wherein the at least one ion pairing agent comprises a tertiary amine.

3. The method of claim 1 , wherein the at least one ion pairing agent comprises triethanolamine, polyethyleneimine, diethanolamine, monoethanolamine, mefenamic acid, tromethamine, or a combination thereof.

4. The method of claim 1 , wherein the at least one ion pairing agent comprises triethanolamine.

5. The method of claim 1 , wherein the at least one ion pairing agent and the compound of Formula I are present in a molar ratio of 20:1 to 1:20.

6. The method of claim 1 , wherein the cancer is a carcinoma, sarcoma, myeloma, lymphoma, or leukemia.

7. The method of claim 6 , wherein the cancer is a lymphoma.

8. The method of claim 6 , wherein the cancer is a leukemia.

9. The method of claim 6 , wherein the cancer is a carcinoma.

10. The method of claim 6 , wherein the cancer is a sarcoma.

11. The method of claim 6 , wherein the cancer is a myeloma.

12. The method of claim 1 , wherein the cancer is a cancer of the pancreas.

13. The method of claim 1 , wherein the compound of Formula I is administered at a dose of 0.001 mg/m 2 to 10 g/m 2 .

14. The method of claim 13 , wherein the compound of Formula I is administered at a dose of 0.01 mg/m 2 to 5 g/m 2 .

15. The method of claim 14 , wherein the compound of Formula I is administered at a dose of 0.25 mg/m 2 to 3 g/m 2 .

16. The method of claim 7 , wherein the compound of Formula I is administered at a dose of 0.25 mg/m to 3 g/m 2 .

17. The method of claim 8 , wherein the compound of Formula I is administered at a dose of 0.25 mg/m 2 to 3 g/m 2 .

18. The method of claim 12 , wherein the compound of Formula I is administered at a dose of 0.25 mg/m 2 to 3 g/m 2 .

19. A method of treating a cancer selected from the group consisting of carcinoma, sarcoma, myeloma, lymphoma, leukemia and cancer of the pancreas, comprising the step of intravenously administering to a human patient in need thereof a pharmaceutical formulation comprising:

a) a therapeutically effective amount of a compound of Formula I:

or a salt thereof; and

b) at least one ion pairing agent.

20. The method of claim 19 , wherein the cancer is a lymphoma and the compound of Formula I or salt thereof is administered at a dose of 0.25 mg/m 2 to 3 g/m 2 .

21. The method of claim 19 , wherein the cancer is a leukemia and the compound of Formula I or salt thereof is administered at a dose of 0.25 mg/m 2 to 3 g/m 2 .

22. The method of claim 19 , wherein the cancer is a cancer of the pancreas and the compound of Formula I or salt thereof is administered at a dose of 0.25 mg/m 2 to 3 g/m 2 .

Assignments (3)
CHANGE OF NAME Recorded Aug 7, 2018
From: CORNERSTONE PHARMACEUTICALS, INC.
To: RAFAEL PHARMACEUTICALS, INC.
Reel/Frame 046734/0195 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 30, 2018
From: SHORR, ROBERT G. L.; RODRIGUEZ, ROBERT J.; BHASIN, RAJINDER
To: CORNERSTONE PHARMACEUTICALS, INC.
Reel/Frame 046503/0940 →
CHANGE OF NAME Recorded Jul 30, 2018
From: CORNERSTONE PHARMACEUTICALS, INC.
To: RAFAEL PHARMACEUTICALS, INC.
Reel/Frame 046660/0859 →
Continuity (6)
Continuation 14857192 · Sep 17, 2015
Continuation 13569654 · Aug 8, 2012
Continuation 12604763 · Oct 23, 2009
Continuation In Part 12105100 · Apr 17, 2008
Provisional Application 60912605 · Apr 18, 2007
Related Publication 20180104341A1 · Apr 19, 2018