IP Library Granted Patent US 9,913,827
Granted Patent B2
US 9,913,827 · App. 15/456,439 · Granted Mar 13, 2018

Bendamustine derivatives and methods of using same

Inventors: Roger P. Bakale (Malvern, PA); Peter D. Brown (West Chester, PA); Jian Chen (West Chester, PA); Anthony S. Drager (Thorndale, PA); Rachel Y. LaBell (Coatesville, PA); Robert E. McKean (Chester Springs, PA); Piyush R. Patel (Wallingford, PA); Renee C. Roemmele (Maple Glen, PA)
Assignee: IGNYTA, INC.
A61K31/4184A61K9/14A61K47/42C07D235/16
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Quick Facts
Patent No.
US 9,913,827
App. No.
15/456,439
Granted
Mar 13, 2018
Kind
B2
Abstract

The present invention is directed to bendamustine esters and bendamustine amides and their use for the treatment of cancer.

Claims (26)

1. A method of treating cancer in a patient comprising administering to said patient a pharmaceutical composition, wherein said pharmaceutical composition comprises:

(a) a compound of formula (I)

wherein R 1 is C 8 -C 24 alkyl, or a pharmaceutically acceptable salt thereof; and

(b) a means for increasing the circulation time of the compound of formula (I), or a pharmaceutically acceptable salt thereof, in an aqueous environment.

2. The method according to claim 1 , wherein said cancer is in the form of a solid tumor or a liquid tumor.

3. The method according to claim 2 , wherein said cancer is in the form of a solid tumor.

4. The method according to claim 3 , wherein said cancer is sarcoma, bladder cancer, cervical cancer, testicular cancer, melanoma, glioblastoma, colon cancer, head and neck cancer, ovarian cancer, prostate cancer, breast cancer, or lung cancer.

5. The method according to claim 1 , wherein said cancer is in the form of a liquid tumor.

6. The method according to claim 5 , wherein said cancer is lymphocytic leukemia, Hodgkin's disease, non-Hodgkin's lymphoma, multiple myeloma, or acute lymphocytic leukemia.

7. The method according to claim 1 , wherein in the compound of formula (I) R 1 is C 10 -C 24 alkyl.

8. The method according to claim 1 , wherein in the compound of formula (I) R 1 is C 12 -C 24 alkyl.

9. The method according to claim 1 , wherein in the compound of formula (I) R 1 is C 14 -C 24 alkyl.

10. The method according to claim 1 , wherein in the compound of formula (I) R 1 is C 10 alkyl.

11. The method according to claim 1 , wherein in the compound of formula (I) R 1 is C 12 alkyl.

12. The method according to claim 1 , wherein in the compound of formula (I) R 1 is C 14 alkyl.

13. The method according to claim 1 , wherein in the compound of formula (I) R 1 is C 15 alkyl.

14. The method according to claim 1 , wherein in the compound of formula (I) R 1 is C 16 alkyl.

15. A method of treating cancer in a patient comprising administering to said patient a pharmaceutical composition, wherein said pharmaceutical composition comprises:

(a) a compound of the formula

or a pharmaceutically acceptable salt thereof; and

(b) a means for increasing the circulation time of the compound, or a pharmaceutically acceptable salt thereof, in an aqueous environment.

16. The method according to claim 15 , wherein said cancer is in the form of a solid tumor or a liquid tumor.

17. The method according to claim 16 , wherein said cancer is in the form of a solid tumor.

18. The method according to claim 17 , wherein said cancer is sarcoma, bladder cancer, cervical cancer, testicular cancer, melanoma, glioblastoma, colon cancer, head and neck cancer, ovarian cancer, prostate cancer, breast cancer, or lung cancer.

19. The method according to claim 16 , wherein said cancer is in the form of a liquid tumor.

20. The method according to claim 19 , wherein said cancer is lymphocytic leukemia, Hodgkin's disease, non-Hodgkin's lymphoma, multiple myeloma, or acute lymphocytic leukemia.

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 22, 2018
From: BAKALE, ROGER P.; BROWN, PETER D.; CHEN, JIAN; DRAGER, ANTHONY S.; LABELL, RACHEL Y.; MCKEAN, ROBERT E.; PATEL, PIYUSH R.; ROEMMELE, RENEE C.
To: CEPHALON, INC.
Reel/Frame 044687/0217 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 22, 2018
From: BAKALE, ROGER P.; CHEN, JIAN; DRAGER, ANTHONY S.; LABELL, RACHEL Y.; MCKEAN, ROBERT E.; PATEL, PIYUSH R.; ROEMMELE, RENEE C
To: CEPHALON, INC.
Reel/Frame 044687/0429 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 22, 2018
From: CEPHALON, INC.
To: IGNYTA, INC.
Reel/Frame 044687/0557 →
Continuity (7)
Continuation 15184968 · Jun 16, 2016
Continuation 14868278 · Sep 28, 2015
Continuation 14699965 · Apr 29, 2015
Continuation PCTUS2013069550 · Nov 12, 2013
Provisional Application 61725213 · Nov 12, 2012
Provisional Application 61776951 · Mar 12, 2013
Related Publication 20170182008A1 · Jun 29, 2017