IP Library Granted Patent US 10,189,861
Granted Patent B2
US 10,189,861 · App. 15/581,702 · Granted Jan 29, 2019

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.
C07D513/04C07D471/18C07D487/04C07D487/12C07D487/14C07D487/16C07D487/18C07D495/14C07D498/04C07D498/18C07F5/022
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Quick Facts
Patent No.
US 10,189,861
App. No.
15/581,702
Granted
Jan 29, 2019
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 (16)

1. A compound having the formula:

or a pharmaceutically acceptable salt thereof,

wherein,

R′ is H or methyl;

L is absent, SO 2 , or CO;

X is H, methyl, fluoro, chloro, phenyl, pyridinyl, thiophenyl, —NH—CO—CH═CH—CH 2 —N(CH 3 ) 2 , —S(O) 2 —N(CH 3 ) 2 , or

Z is NH or N—C1-C3 alkyl;

R 2 is hydrogen or methyl;

R 6 is hydrogen; and

R 1 is H, C═O(CH 3 ),

2. The compound of claim 1 , wherein the compound is selected from the group consisting of:

3. A compound selected from the group consisting of:

4. The compound

or a pharmaceutically acceptable salt thereof.

5. The compound

or a pharmaceutically acceptable salt thereof.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 8, 2017
From: GRAY, NATHANAEL S.; WALLER, DAVID; CHOI, HWAN GUEN; WANG, JINHUA; DENG, XIANMING
To: DANA-FARBER CANCER INSTITUTE, INC.
Reel/Frame 043227/0334 →
Continuity (3)
Division 14775897
Provisional Application 61802075 · Mar 15, 2013
Related Publication 20170283422A1 · Oct 5, 2017