IP Library Granted Patent US 9,676,792
Granted Patent B2
US 9,676,792 · App. 14/775,897 · Granted Jun 13, 2017

Pyrimido-diazepinone compounds and methods of treating disorders

Inventors: Nathanael S. Gray (Boston, MA); David Waller (Somerville, MA); Hwan Guen Choi (Boston, MA); Jinhua Wang (Boston, MA); Xianming Deng (Brookline, MA)
Assignee: Dana-Farber Cancer Institute, Inc.
C07D513/04C07D471/18C07D487/04C07D487/14C07D487/16C07D495/14C07D498/04C07D498/18C07F5/022
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Quick Facts
Patent No.
US 9,676,792
App. No.
14/775,897
Granted
Jun 13, 2017
Kind
B2
Abstract

The present invention relates to novel pyrimido-diazepinone compounds, methods of modulating protein kinases, including MPS1 (TTK), ERK5 (BMK1, MAPK7), LRKK2, EphA2, polo kinase 1, 2, 3, or 4, Ack1, Ack2, Abl, DCAMKL1, ABL1, Abl mutants, DCAMKL2, ARK5, BRK, MKNK2, FGFR4, TNK1, PLK1, ULK2, PLK4, PRKD1, PRKD2, PRKD3, ROS1, RPS6KA6, TAOK1, TAOK3, TNK2, Bcr-Abl, GAK, cSrc, TPR-Met, Tie2, MET, FGFR3, Aurora, Axl, Bmx, BTK, c-kit, CHK2, Flt3, MST2, p70S6K, PDGFR, PKB, PKC, Raf, ROCK-H, Rsk1, SGK, TrkA, TrkB and TrkC, and the use of such compounds in the treatment of various diseases, disorders or conditions.

Claims (14)

1. A compound of formula V:

or a pharmaceutically acceptable salt thereof,

wherein,

X is hydrogen;

R 2 is hydrogen or alkyl;

R 3 is —OH or O-(alkyl);

R 4 is hydrogen or alkyl;

R 6 is hydrogen or alkyl; and

R′ is hydrogen.

2. The compound of claim 1 , wherein R 2 is H, methyl, or ethyl.

3. The compound of claim 1 , wherein R 6 is H.

4. The compound of claim 1 , wherein R 3 is —OCH 3 or —OCH 2 CH 3 .

5. The compound of claim 1 , wherein R 4 is methyl or ethyl.

6. A pharmaceutical composition comprising a compound of claim 1 , or a pharmaceutically acceptable salt thereof, together with a pharmaceutically acceptable carrier.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 17, 2017
From: GRAY, NATHANAEL S.; WALLER, DAVID; CHOI, HWAN GUEN; WANG, JINHUA; DENG, XIANMING
To: DANA-FARBER CANCER INSTITUTE, INC.
Reel/Frame 040985/0804 →
CONFIRMATORY LICENSE Recorded Jul 1, 2016
From: DANA-FARBER CANCER INST
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 039239/0397 →
Continuity (2)
Provisional Application 61802075 · Mar 15, 2013
Related Publication 20160024115A1 · Jan 28, 2016