IP Library Granted Patent US 11,485,705
Granted Patent B2
US 11,485,705 · App. 16/881,709 · Granted Nov 1, 2022

Salts and prodrugs of 1-methyl-d-tryptophan

Inventors: Mario Mautino (Ankeny, IA); Sanjeev Kumar (Ames, IA); Firoz Jaipuri (Ames, IA); Jesse Waldo (Huxley, IA); Hima Potturi (Ames, IA); Hong Zhuang (Ames, IA)
Assignee: LUMOS PHARMA, INC.
C07D209/20A61K31/285C07C309/04C07C309/20C07D401/12C07D405/12C07F9/65742
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Quick Facts
Patent No.
US 11,485,705
App. No.
16/881,709
Granted
Nov 1, 2022
Kind
B2
Abstract

Presently provided are indoximod prodrug and salt compounds and pharmaceutical compositions comprising salts and prodrugs of indoximod, that produce enhanced plasma concentration and exposure to indoximod compared to direct administration of indoximod, in patients in need of treatment of immunosuppression mediated by the indoleamine-2,3-dioxygenase pathway, such as patients with cancer or chronic infectious diseases.

Claims (20)

1. A prodrug of indoximod comprising ethyl N α -(L-leucyl)-1-methyl-D-tryptophanate, or a pharmaceutically acceptable salt thereof.

2. The prodrug of claim 1 , wherein the pharmaceutically acceptable salt is a phosphate, sulfate, hydrochloride, methanesulfonate, benzylsulfonate, acetate, ascorbate, aspartate, glutamate, glutarate, lactate, maleate, malonate, oxalate, succinate, fumarate, tartrate or citrate salt.

3. The prodrug of claim 1 , wherein the pharmaceutically acceptable salt is a phosphate salt.

4. The prodrug of claim 1 , wherein the pharmaceutically acceptable salt is a hydrochloride salt.

5. A pharmaceutical composition of indoximod comprising ethyl N α -(L-leucyl)-1-methyl-D-tryptophanate or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.

6. The pharmaceutical composition of claim 5 , wherein the pharmaceutically acceptable salt is a phosphate, sulfate, hydrochloride, methanesulfonate, benzylsulfonate, acetate, ascorbate, aspartate, glutamate, glutarate, lactate, maleate, malonate, oxalate, succinate, fumarate, tartrate or citrate salt.

7. The pharmaceutical composition of claim 5 , wherein the pharmaceutically acceptable salt is a phosphate salt.

8. The pharmaceutical composition of claim 5 , wherein the pharmaceutically acceptable salt is a hydrochloride salt.

9. The pharmaceutical composition of claim 5 , in the form of a solid capsule, tablet or pill.

10. The pharmaceutical composition of claim 5 , in the form of a dissolvable capsule.

11. A method of treating cancer, comprising administering to a subject in need thereof, a therapeutically effective amount of the prodrug of claim 1 , or a pharmaceutically acceptable salt thereof.

12. The method of claim 11 , wherein the pharmaceutically acceptable salt is a phosphate salt.

13. The method of claim 11 , wherein the pharmaceutically acceptable salt is a hydrochloride salt.

14. The method of claim 11 , wherein the cancer is melanoma, colon cancer, lung cancer, or breast cancer.

15. The method of claim 11 , wherein the cancer is melanoma.

16. A method of treating cancer, comprising administering to a subject in need thereof, a therapeutically effective amount of a composition comprising ethyl N α -(L-leucyl)-1-methyl-D-tryptophanate, or a pharmaceutically acceptable salt thereof.

17. The method of claim 16 , wherein the pharmaceutically acceptable salt is a phosphate salt.

18. The method of claim 16 , wherein the pharmaceutically acceptable salt is a hydrochloride salt.

19. The method of claim 16 , wherein the cancer is melanoma, colon cancer, lung cancer, or breast cancer.

20. The method of claim 16 , wherein the cancer is melanoma.

Assignments (2)
CHANGE OF NAME Recorded Jun 17, 2020
From: NEWLINK GENETICS CORPORATION
To: LUMOS PHARMA, INC.
Reel/Frame 052965/0558 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 11, 2020
From: MAUTINO, MARIO R.; KUMAR, SANJEEV; JAIPURI, FIROZ; WALDO, JESSE; POTTURI, HIMA; ZHUANG, HONG
To: NEWLINK GENETICS CORPORATION
Reel/Frame 052911/0803 →
Continuity (6)
Continuation 16277248 · Feb 15, 2019
Continuation 15634610 · Jun 27, 2017
Continuation 15171031 · Jun 2, 2016
Provisional Application 62305748 · Mar 9, 2016
Provisional Application 62196671 · Jul 24, 2015
Related Publication 20200283385A1 · Sep 10, 2020