IP Library Granted Patent US 8,940,752
Granted Patent B2
US 8,940,752 · App. 12/824,924 · Granted Jan 27, 2015

Pyrimidinones as PI3K inhibitors

Inventors: Yun-Long Li (Chadds Ford, PA); Brian W. Metcalf (Moraga, CA)
Assignee: Incyte Corporation
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Quick Facts
Patent No.
US 8,940,752
App. No.
12/824,924
Granted
Jan 27, 2015
Kind
B2
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.

Claims (16)

1. A compound, which 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.

2. The compound of claim 1 , which is (S)-7-(1-(9H-purin-6-ylamino)ethyl)-6-(3-fluorophenyl)-3-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one.

3. A compound, which is 6-(3-fluorophenyl)-3-methyl-7-[1-(9H-purin-6-ylamino)ethyl]-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one, or a pharmaceutically acceptable salt thereof.

4. The compound of claim 3 , which is 6-(3-fluorophenyl)-3-methyl-7-[1-(9H-purin-6-ylamino)ethyl]-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one.

5. A composition comprising a compound according to claim 1 , or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable carrier.

6. A composition comprising a compound according to claim 3 , or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable carrier.

7. A composition comprising a compound according to claim 2 and at least one pharmaceutically acceptable carrier.

8. A composition comprising a compound according to claim 4 and at least one pharmaceutically acceptable carrier.

9. A method of treating arthritis in a patient, comprising administering to said patient a therapeutically effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt thereof.

10. A method of treating arthritis in a patient, comprising administering to said patient a therapeutically effect amount of a compound of claim 3 , or a pharmaceutically acceptable salt thereof.

11. A method of treating arthritis in a patient, comprising administering to said patient a therapeutically effective amount of a compound of claim 2 .

12. A method of treating arthritis in a patient, comprising administering to said patient a therapeutically effective amount of a compound of claim 4 .

13. A method of treating rheumatoid arthritis in a patient, comprising administering to said patient a therapeutically effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt thereof.

14. A method of treating rheumatoid arthritis in a patient, comprising administering to said patient a therapeutically effect amount of a compound of claim 3 , or a pharmaceutically acceptable salt thereof.

15. A method of treating rheumatoid arthritis in a patient, comprising administering to said patient a therapeutically effective amount of a compound of claim 2 .

16. A method of treating rheumatoid arthritis in a patient, comprising administering to said patient a therapeutically effective amount of a compound of claim 4 .

Assignments (3)
CORRECTIVE ASSIGNMENT TO CORRECT THE OMMISSION OF SECOND RECEIVING PARTY NAME PREVIOUSLY RECORDED AT REEL: 035292 FRAME: 0004. ASSIGNOR(S) HEREBY CONFIRMS THE ASSIGNMENT. Recorded Jul 2, 2015
From: INCYTE CORPORATION
To: INCYTE HOLDINGS CORPORATION; INCYTE CORPORATION
Reel/Frame 036054/0696 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 16, 2015
From: INCYTE CORPORATION
To: INCYTE HOLDINGS CORPORATION AND INCYTE CORPORATION
Reel/Frame 035924/0004 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 29, 2010
From: LI, YUN-LONG; METCALF, BRIAN W.; COMBS, ANDREW P.
To: INCYTE CORPORATION
Reel/Frame 025059/0267 →
Continuity (3)
Provisional Application 61221160 · Jun 29, 2009
Provisional Application 61259765 · Nov 10, 2009
Related Publication 20110015212A1 · Jan 20, 2011