IP Library › Granted Patent US 41,253
Granted Patent E1
US 41,253 · App. 11/978,093 · Granted Apr 20, 2010

Antineoplastic combinations

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Quick Facts
Patent No.
US 41,253
App. No.
11/978,093
Granted
Apr 20, 2010
Kind
E1
Abstract

This invention provides the use of a combination of CCI-779 and EKB-569 in the treatment of neoplasms.

Claims (36)

1. A method of treating a neoplasm in a mammal in need thereof, which comprises providing to said mammal synergistically effective amount of a combination comprising CCI-779 and EKB-569.

2. The method according to claim 1 , wherein the neoplasm is renal cancer.

3. The method according to claim 1 , wherein the neoplasm is soft tissue sarcoma.

4. The method according to claim 1 , wherein the neoplasm is breast cancer.

5. The method according to claim 1 , wherein the neoplasm is a neuroendocrine tumor of the lung.

6. The method according to claim 1 , wherein the neoplasm is cervical cancer.

7. The method according to claim 1 , wherein the neoplasm is uterine cancer.

8. The method according to claim 1 , wherein the neoplasm is a head and neck cancer.

9. The method according to claim 1 , wherein the neoplasm is glioma.

10. The method according to claim 1 , wherein the neoplasm is non-small cell lung cancer.

11. The method according to claim 1 , wherein the neoplasm is prostate cancer.

12. The method according to claim 1 , wherein the neoplasm is pancreatic cancer.

13. The method according to claim 1 , wherein the neoplasm is lymphoma.

14. The method according to claim 1 , wherein the neoplasm is melanoma.

15. The method according to claim 1 , wherein the neoplasm is small cell lung cancer.

16. The method according to claim 1 , wherein the neoplasm is ovarian cancer.

17. The method according to claim 1 , wherein the neoplasm is colon cancer.

18. The method according to claim 1 , wherein the neoplasm is esophageal cancer.

19. The method according to claim 1 , wherein the neoplasm is gastric cancer.

20. The method according to claim 1 , wherein the neoplasm is leukemia.

21. The method according to claim 1 , wherein the neoplasm is colorectal cancer.

22. The method according to claim 1 , wherein the neoplasm is unknown primary cancer.

23. A method of treating a neoplasm in a mammal in need thereof, which comprises providing to said mammal an effective amount of a synergistic combination comprising CCI-779 and EKB-569, wherein either CCI-779, EKB-569, or both are provided in subtherapeutically effective amounts.

24. The method according to claim 23 in which CCI-779 is provided in a subtherapeutically effective amount.

25. The method according to claim 23 in which EKB-569 is provided in a subtherapeutically effective amount.

26. The method according to claim 23 in which both CCI-779 and EKB-569 are provided in subtherapeutically effective amounts.

27. An antineoplastic combination which comprises an antineoplastic effective amount of a synergistic combination of CCI-779 and EKB-569.

28. A process for the preparation of a compound of formula:

comprising:

( a ) reacting a trimethylsilyl - 4 - bromocrotonate or methyl 4 - bromocrotonate with dimethylamine to obtain the corresponding 4 - dimethylaminocrotonate;

( b ) hydrolyzing the 4 - dimethylaminocrotonate of step ( a ) to form the corresponding 4 - dimethylaminocrotonic acid; and

( c ) optionally chlorinating the compound of step ( b ) to form the HCl salt of the compound of step ( b ).

29. The process according to claim 28 , wherein the hydrolyzing step ( c ) comprises reacting the 4 - dimethylaminocrotonate with NaOH in the presence of MeOH.

30. The process according to claim 28 , wherein the chlorinating step ( c ) comprises reacting the 4 - dimethylaminocrotonic acid with HCl.

31. The process according to claim 28 wherein the reaction is performed with trimethylsilyl- 4 - bromocrotonate.

32. The process according to claim 28 wherein the reaction is performed with methyl 4 - bromocrotonate.