IP Library Granted Patent US 9,624,241
Granted Patent B2
US 9,624,241 · App. 14/923,105 · Granted Apr 18, 2017

Tricyclic heterocycles as BET protein inhibitors

Inventors: Andrew P. Combs (Wilmington, DE); Richard B. Sparks (Wilmington, DE); Thomas P. Maduskuie, Jr. (Wilmington, DE)
Assignees: Incyte Corporation; Incyte Holdings Corporation
C07D498/06C07D471/06C07D498/16C07D519/00
View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 9,624,241
App. No.
14/923,105
Granted
Apr 18, 2017
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 (8)

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

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

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

4. A compound which is (4S)-2-(4-acetylpiperazin-1-yl)-7-(3,5-dimethylisoxazol-4-yl)-4-pyridin-2-yl-4,5-dihydroimidazo[1,5,4-de][1,4]benzoxazine.

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

6. A pharmaceutical composition comprising the compound of claim 2 and at least one pharmaceutically acceptable carrier.

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

8. A pharmaceutical composition comprising the compound of claim 4 and at least one pharmaceutically acceptable carrier.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 10, 2015
From: COMBS, ANDREW P.; SPARKS, RICHARD B.; MADUSKUIE, THOMAS P., JR.; RODGERS, JAMES D.
To: INCYTE CORPORATION
Reel/Frame 037000/0169 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 10, 2015
From: INCYTE CORPORATION
To: INCYTE HOLDINGS CORPORATION; INCYTE CORPORATION
Reel/Frame 037000/0257 →
Continuity (3)
Continuation 14212721 · Mar 14, 2014
Provisional Application 61794812 · Mar 15, 2013
Related Publication 20160046650A1 · Feb 18, 2016