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Last Updated: August 13, 2020

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Claims for Patent: 9,944,651

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Summary for Patent: 9,944,651
Title:Compositions useful for treating disorders related to kit
Abstract: Compounds and compositions useful for treating disorders related to mutant KIT are described herein.
Inventor(s): Hodous; Brian L. (Cambridge, MA), Kim; Joseph L. (Wayland, MA), Wilson; Kevin J. (Boston, MA), Wilson; Douglas (Ayer, MA), Zhang; Yulian (Acton, MA)
Assignee: BLUEPRINT MEDICINES CORPORATION (Cambridge, MA)
Application Number:15/479,145
Patent Claims: 1. A compound which is: ##STR00233##

2. A compound which is: ##STR00234## or a pharmaceutically acceptable salt thereof.

3. A pharmaceutical composition comprising a compound which is: ##STR00235## or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.

4. A method of treating a condition selected from gastrointestinal stromal tumor (GIST), mastocytosis, and acute myeloid leukemia (AML) in a patient in need thereof, wherein the method comprises administering to the patient a therapeutically effective amount of a compound which is ##STR00236## or a pharmaceutically acceptable salt thereof.

5. The method of claim 4, wherein the condition is GIST.

6. The method of claim 5, wherein the patient has a D842V mutation in PDFGR.alpha. in Exon 18.

7. The method of claim 5, wherein the patient has a mutation in Exon 17 in KIT.

8. The method of claim 5, wherein the patient is refractory to treatment with imatinib, sunitinib, and/or regorafenib.

9. The method of claim 7, wherein the patient has a D816 mutation in KIT in Exon 17.

10. The method of claim 9, wherein the D816 mutation is D816V.

11. The method of claim 5, wherein the patient has unresectable GIST.

12. The method of claim 4, wherein the condition is mastocytosis.

13. The method of claim 12, wherein the mastocytosis is systemic mastocytosis (SM) or cutaneous mastocytosis (CM).

14. The method of claim 13, wherein the systemic mastocytosis (SM) is selected from indolent (ISM), smoldering (SSM), aggressive (ASM), SM with associated hematologic non-mast cell lineage disease (SM-AHNMD), and mast cell leukemia (MCL).

15. The method of claim 13, wherein the systemic mastocytosis is aggressive (ASM).

16. The method of claim 13, wherein the systemic mastocytosis is systemic mastocytosis-associated hematologic non-mast cell disease (SM-AHNMD).

17. The method of claim 13, wherein the systemic mastocytosis is mast cell leukemia (MCL).

18. The method of claim 12, wherein the patient has a mutation in Exon 17 in KIT.

19. The method of claim 18, wherein the patient has a D816 mutation in KIT in Exon 17.

20. The method of claim 19, wherein the D816 mutation is D816V.

21. The method of claim 4, wherein the condition is acute myeloid leukemia (AML).

22. The method of claim 21, wherein the patient has a mutation in Exon 17 in KIT.

23. The method of claim 22, wherein the patient has a D816 mutation in KIT in Exon 17.

24. The method of claim 23, wherein the D816 mutation is D816V.

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Serving leading biopharmaceutical companies globally:

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