IP Library Granted Patent US 10,201,543
Granted Patent B2
US 10,201,543 · App. 15/548,737 · Granted Feb 12, 2019

Therapeutically active compounds and their methods of use

Inventor: Stefan Kluge (Riehen, CH)
Assignee: Agios Pharmaceuticals, Inc.
A61K31/53C07D401/14C07B2200/13G01N23/20075G01N25/4866
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Quick Facts
Patent No.
US 10,201,543
App. No.
15/548,737
Granted
Feb 12, 2019
Kind
B2
Abstract

Provided are crystalline forms of 2-Methyl-1-[(4-[6-(trifluoromethyl) pyridin-2-yl]-6-{[2-(trifluoromethyl)pyridin-4-yl]amino}-1,3,5-triazin-2-yl)amino]propan-2-ol mesylate useful for treating cancer and methods of treating cancer, comprising administering to a subject in need thereof said compound.

Claims (20)

1. An isolated crystalline form of 2-methyl-1-[(4-[6-(trifluoromethyl)pyridin-2-yl]-6-{[2-(trifluoromethyl)pyridin-4-yl]amino}-1,3,5-triazin-2-yl)amino]propan-2-ol mesylate, characterized by an X-ray powder diffraction pattern substantially similar to FIG. 40 or FIG. 43 .

2. A method of treating an advanced hematologic malignancy selected from acute myelogenous leukemia (AML), myelodysplastic syndrome (MDS), chronic myelomonocytic leukemia (CMML), myeloid sarcoma, multiple myeloma, and lymphoma, each characterized by the presence of a mutant allele of IDH2, comprising administering to a subject in need thereof a therapeutically effective dose of a crystalline form of claim 1 .

3. A method of treating an advanced hematologic malignancy selected from acute myelogenous leukemia (AML), myelodysplastic syndrome (MDS), chronic myelomonocytic leukemia (CMML), myeloid sarcoma, multiple myeloma, and lymphoma, each characterized by the presence of a mutant allele of IDH2, comprising administering to subject in need thereof a pharmaceutical composition comprising a therapeutically effective dose of a crystalline form of claim 1 and one or more pharmaceutically acceptable carrier(s).

4. A method of treating an advanced hematologic malignancy selected from acute myelogenous leukemia (AML), myelodysplastic syndrome (MDS), chronic myelomonocytic leukemia (CMML), myeloid sarcoma, multiple myeloma, and lymphoma, each characterized by the presence of a mutant allele of IDH2, comprising administering to a subject in need thereof a crystalline form of claim 1 at a dose of from about 30 mg to about 300 mg free-base equivalent strength, once daily or twice daily.

5. The method of claim 4 , wherein the dose is about 75 mg, once daily or twice daily.

6. The method of claim 4 , wherein the dose is about 100 mg, once daily or twice daily.

7. The method of claim 4 , wherein the dose is about 150 mg, once daily or twice daily.

8. The method of claim 4 , wherein the dose is about 200 mg, once daily or twice daily.

9. The method of claim 4 , wherein the dosage is an oral dosage form.

10. The method of claim 9 , wherein the oral dosage form is a tablet.

11. The method of claim 4 , wherein the dose is administered once daily.

12. The method of claim 4 , wherein the dose is administered twice daily.

13. The method of claim 4 , wherein the dose is administered orally as any combination of 5, 10, 50, or 200 mg free-base equivalent strength tablets, twice daily or once daily.

14. The method of claim 4 , wherein the advanced hematologic malignancy is selected from acute myelogenous leukemia (AML), myelodysplastic syndrome (MDS), chronic myelomonocytic leukemia (CMML), and lymphoma.

15. The method of claim 14 , wherein the advanced hematologic malignancy is acute myelogenous leukemia (AML).

16. The method of claim 14 , wherein the advanced hematologic malignancy is myelodysplastic syndrome (MDS).

17. The method of claim 14 , wherein the advanced hematologic malignancy is chronic myelomonocytic leukemia (CMML).

18. The method of claim 14 , wherein the advanced hematologic malignancy is lymphoma.

19. The method of claim 6 , wherein the dose is about 100 mg, once daily.

20. The method of claim 15 , wherein the dose is about 100 mg, once daily.

Assignments (4)
CORRECTIVE ASSIGNMENT TO CORRECT THE THE ASSIGNEE NAME AND THE POSTAL CODE PREVIOUSLY RECORDED AT REEL: 056756 FRAME: 0459. ASSIGNOR(S) HEREBY CONFIRMS THE ASSIGNMENT. Recorded Mar 16, 2022
From: AGIOS PHARMACEUTICALS, INC.
To: SERVIER PHARMACEUTICALS LLC
Reel/Frame 059907/0429 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 2, 2021
From: AGIOS PHARMACEUTICALS, INC.
To: SERVIER PHARMACEUTICALS, LLC
Reel/Frame 056756/0459 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 17, 2018
From: KLUGE, STEFAN
To: SOLVIAS AG
Reel/Frame 045839/0515 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 17, 2018
From: SOLVIAS AG
To: AGIOS PHARMACEUTICALS, INC.
Reel/Frame 046183/0777 →
Continuity (2)
Provisional Application 62112127 · Feb 4, 2015
Related Publication 20180028539A1 · Feb 1, 2018
Cited By (1)
US 12,215,094