Pyrimidinones as PI3K inhibitors

Patent metadata

Field	Value
Publication number	US-9434746-B2
Application number	US-201414146169-A
Country	US
Kind code	B2
Filing date	Jan 2, 2014
Priority date	Jun 29, 2009
Publication date	Sep 6, 2016
Grant date	Sep 6, 2016

Abstract

The present invention provides pyrimidinones that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.

First claim

What is claimed is:

1. A method of inhibiting an activity of PI3Kδ comprising contacting said PI3Kδ with a compound, which is 7-(1-(9H-purin-6-ylamino)ethyl)-6-(3-fluorophenyl)-3-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one, or a pharmaceutically acceptable salt thereof.

2. The method of claim 1 , wherein said compound is a selective inhibitor for PI3Kδ over one or more of PI3Kα, PI3Kβ, and PI3Kγ.

3. A method of treating a disease selected from B cell lymphoma, rheumatoid arthritis, myasthenia gravis, Sjoegren's syndrome, multiple sclerosis, glomerulonephritis, lupus, and inflammation related to rheumatoid arthritis, glomerulonephritis, or lupus, in a patient, comprising administering to said patient a therapeutically effective amount of a compound, which is 7-(1-(9H-purin-6-ylamino)ethyl)-6-(3-fluorophenyl)-3-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one, or a pharmaceutically acceptable salt thereof.

4. The method of claim 1 , wherein the compound is (S)-7-(1-(9H-purin-6-ylamino)ethyl)-6-(3-fluorophenyl)-3-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one, or a pharmaceutically acceptable salt thereof.

5. The method of claim 3 , wherein the disease is B cell lymphoma.

6. The method of claim 5 , wherein the B cell lymphoma is diffuse large B cell lymphoma.

7. The method of claim 3 , wherein the disease is myasthenia gravis.

8. The method of claim 3 , wherein the disease is Sjoegren's syndrome.

9. The method of claim 3 , wherein the disease is multiple sclerosis.

10. The method of claim 3 , wherein the disease is glomerulonephritis.

11. The method of claim 3 , wherein the disease is lupus.

12. The method of claim 3 , wherein the disease is inflammation related to rheumatoid arthritis.

13. The method of claim 3 , wherein the disease is inflammation related to glomerulonephritis.

14. The method of claim 3 , wherein the disease is inflammation related to lupus.

15. The method of claim 3 , wherein the compound is (S)-7-(1-(9H-purin-6-ylamino)ethyl)-6-(3-fluorophenyl)-3-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one, or a pharmaceutically acceptable salt thereof.

16. The method of claim 15 , wherein the disease is B cell lymphoma.

17. The method of claim 16 , wherein the B cell lymphoma is diffuse large B cell lymphoma.

18. The method of claim 15 , wherein the disease is myasthenia gravis.

19. The method of claim 15 , wherein the disease is Sjöegren's syndrome.

20. The method of claim 15 , wherein the disease is multiple sclerosis.

21. The method of claim 13 , wherein the disease is glomerulonephritis.

22. The method of claim 15 , wherein the disease is lupus.

23. The method of claim 15 , wherein the disease is inflammation related to rheumatoid arthritis.

24. The method of claim 15 , wherein the disease is inflammation related to glomerulonephritis.

25. The method of claim 15 , wherein the disease is inflammation related to lupus.

Assignees

• Incyte Corp
• Incyte Holdings Corp

Inventors

• Li Yun-Long
• Metcalf Brian W
• Combs Andrew P

Classifications

• A61P37/08

  Antiallergic agents (antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14) · CPC title

• A61P37/02

  Immunomodulators · CPC title

• A61P37/00

  Drugs for immunological or allergic disorders · CPC title

• A61P35/02

  specific for leukemia · CPC title

• A61P9/10

  for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis · CPC title