Substituted tricyclic compounds as FGFR inhibitors

Patent metadata

Field	Value
Publication number	US-11840534-B2
Application number	US-202117337027-A
Country	US
Kind code	B2
Filing date	Jun 2, 2021
Priority date	Jun 13, 2012
Publication date	Dec 12, 2023
Grant date	Dec 12, 2023

Abstract

The present invention relates to tricyclic compounds, and pharmaceutical compositions of the same, that are inhibitors of one or more FGFR enzymes and are useful in the treatment of FGFR-associated diseases such as cancer.

First claim

What is claimed is:

1. A method of treating cancer in a patient comprising administering to said patient a therapeutically effective amount of 3-(2,6-difluoro-3,5-dimethoxyphenyl)-1-ethyl-8-(morpholin-4-ylmethyl)-1,3,4,7-tetrahydro-2H-pyrrolo[3′,2′:5,6]pyrido[4,3-d]pyrimidin-2-one, or a pharmaceutically acceptable salt thereof, wherein said cancer is selected from leukemia, chronic lymphocytic lymphoma, B-cell lymphoma, Hodgkin's lymphoma, non-Hodgkin's lymphoma, polycythemia vera, essential thrombocythemia, primary myelofibrosis, Waldenstrom's Macroglobulinemia, hairy cell lymphoma, and Burkett's lymphoma.

2. The method of claim 1 , wherein said cancer is leukemia.

3. The method of claim 1 , wherein said leukemia is adult T cell leukemia.

4. The method of claim 1 , wherein said leukemia is acute myelogenous leukemia.

5. The method of claim 1 , wherein said cancer is chronic lymphocytic lymphoma.

6. The method of claim 1 , wherein said cancer is B-cell lymphoma.

7. The method of claim 1 , wherein said cancer is Hodgkin's lymphoma.

8. The method of claim 1 , wherein said cancer is non-Hodgkin's lymphoma.

9. The method of claim 1 , wherein said cancer is polycythemia vera.

10. The method of claim 1 , wherein said cancer is essential thrombocythemia.

11. The method of claim 1 , wherein said cancer is primary myelofibrosis.

12. The method of claim 1 , wherein said cancer is Waldenstrom's Macroglobulinemia.

13. The method of claim 1 , wherein said cancer is hairy cell lymphoma.

14. The method of claim 1 , wherein said cancer is Burkett's lymphoma.

15. The method of claim 1 , the method comprising administering to said patient a therapeutically effective amount of 3-(2,6-difluoro-3,5-dimethoxyphenyl)-1-ethyl-8-(morpholin-4-ylmethyl)-1,3,4,7-tetrahydro-2H-pyrrolo[3′,2′:5,6]pyrido[4,3-d]pyrimidin-2-one.

Assignees

• Incyte Corp
• Incyte Holdings Corp

Inventors

• Wu Liangxing
• Zhang Colin
• He Chunhong
• Lu Liang
• Yao Wenqing

Classifications

• C07D471/04

  Ortho-condensed systems · CPC title

• C07D471/14 Primary

  Ortho-condensed systems · CPC title

• A61P1/16

  for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics · CPC title

• A61P11/00

  Drugs for disorders of the respiratory system · CPC title

• A61P19/02

  for joint disorders, e.g. arthritis, arthrosis · CPC title