IP Library Granted Patent US 9,227,985
Granted Patent B2
US 9,227,985 · App. 14/212,721 · Granted Jan 5, 2016

Tricyclic heterocycles as bet protein inhibitors

Inventors: Andrew P. Combs (Kennett Square, PA); Richard B. Sparks (Wilmington, DE); Thomas P. Maduskuie (Wilmington, DE); James D. Rodgers (Landenberg, PA)
Assignees: Incyte Corporation; Incyte Holdings Corporation
C07D498/16C07D471/06C07D498/06
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Quick Facts
Patent No.
US 9,227,985
App. No.
14/212,721
Granted
Jan 5, 2016
Kind
B2
Abstract

The present invention relates to tricyclic heterocycles of Formula (I): which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer.

Claims (16)

1. A compound having the structure:

or a pharmaceutically acceptable salt thereof.

2. A pharmaceutical composition comprising the compound of claim 1 , or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable carrier or excipient.

3. A compound which is (4S)-7-(3,5-dimethylisoxazol-4-yl)-4-pyridin-2-yl-4,5-dihydroimidazo[1,5,4-de][1,4]benzoxazin-2(1H)-one, or a pharmaceutically acceptable salt thereof.

4. A pharmaceutical composition comprising the compound of claim 3 , or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable carrier or excipient.

5. A compound which is (4R)-7-(3,5-dimethylisoxazol-4-yl)-4-pyridin-2-yl-4,5-dihydroimidazo[1,5,4-de][1,4]benzoxazin-2(1H)-one, or a pharmaceutically acceptable salt thereof.

6. A pharmaceutical composition comprising the compound of claim 5 , or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable carrier or excipient.

7. The compound of claim 1 which is:

8. A pharmaceutical composition comprising the compound of claim 7 and at least one pharmaceutically acceptable carrier or excipient.

9. A compound which is (4S)-7-(3,5-dimethylisoxazol-4-yl)-4-pyridin-2-yl-4,5-dihydroimidazo[1,5,4-de][1,4]benzoxazin-2(1H)-one.

10. A pharmaceutical composition comprising the compound of claim 9 and at least one pharmaceutically acceptable carrier or excipient.

11. A compound having the structure:

or a pharmaceutically acceptable salt thereof.

12. A pharmaceutically composition comprising the compound of claim 11 , or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable carrier or excipient.

13. A compound having the structure:

14. A pharmaceutical composition comprising the compound of claim 13 and at least one pharmaceutically acceptable carrier or excipient.

Assignments (3)
CORRECTIVE ASSIGNMENT TO CORRECT THE RECEIVING PARTY INFORMATION PREVIOUSLY RECORDED ON REEL 035920 FRAME 0576. ASSIGNOR(S) HEREBY CONFIRMS THE RECEIVING PARTY NAME SHOULD BE RECORDED AS TWO PARTIES. Recorded Jul 2, 2015
From: INCYTE CORPORATION
To: INCYTE HOLDINGS CORPORATION; INCYTE CORPORATION
Reel/Frame 036054/0740 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 16, 2015
From: INCYTE CORPORATION
To: INCYTE HOLDINGS CORPORATION AND INCYTE CORPORATION
Reel/Frame 035920/0576 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 9, 2014
From: COMBS, ANDREW P.; SPARKS, RICHARD B.; MADUSKUIE, THOMAS P.; RODGERS, JAMES D.
To: INCYTE CORPORATION
Reel/Frame 032636/0425 →
Continuity (2)
Provisional Application 61794812 · Mar 15, 2013
Related Publication 20140275030A1 · Sep 18, 2014