IP Library Granted Patent US 9,932,317
Granted Patent B2
US 9,932,317 · App. 14/385,268 · Granted Apr 3, 2018

Quinazoline compounds and their use in therapy

Inventors: Robert Brown (London, GB); Matthew John Fuchter (London, GB); Nadine Chapman-Rothe (London, GB); Nitipol Srimongkolpithak (London, GB); Joachim Caron (London, GB); James Snyder (Atlanta, GA); Thota Ganesh (Atlanta, GA); Jin Liu (Atlanta, GA); Aiming Sun (Atlanta, GA)
Assignees: Imperial Innovations Limited; Emory University
C07D239/95A61K31/517A61K31/519A61K31/5377A61K31/55A61K31/551C07D401/04C07D401/12C07D401/14C07D403/12C07D405/14C07D491/056
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Quick Facts
Patent No.
US 9,932,317
App. No.
14/385,268
Granted
Apr 3, 2018
Kind
B2
Abstract

This invention relates to quinazoline compounds of Formula (I) which are inhibitors of the histone lysine methyltransferase (HKMTase) EZH2, and to uses of such compounds as medicaments, in particular in the treatment of a disease or disorder in which inhibition of EZH2 provides a therapeutic or prophylactic effect.

Claims (23)

1. A compound having formula (IA)

or a pharmaceutically acceptable salt thereof;

wherein W is

R a is selected from the group consisting of hydrogen, C 1-8 alkyl, and pyridyl;

either V 1 and D 1 are both absent and E 1 is hydrogen; or

V 1 is O;

D 1 is absent or C 1-8 alkylene;

E 1 is selected from the group consisting of hydrogen and 6-membered carbocyclyl;

either V 2 and D 2 are both absent and E 2 is hydrogen; or

V 2 is O;

D 2 is absent or C 1-8 alkylene;

E 2 is selected from the group consisting of hydrogen and 6-membered carbocyclyl;

V 3 is NR e ;

R e is hydrogen;

n is 0;

R g is selected from the group consisting of hydrogen and optionally substituted 5 to 10-membered carbocyclyl-C 1-6 alkyl, said carbocyclyl being optionally substituted with up to 3 C 1-4 alkyl groups optionally substituted with up to 3 halogens; and

R h is absent.

2. A compound as claimed in claim 1 , wherein R a is selected from the group consisting of C 1-6 alkyl, and pyridyl.

3. A compound as claimed in claim 1 , wherein V 1 is O; D 1 is C 1-6 alkylene; and E 1 is hydrogen or 6-membered aryl.

4. A compound as claimed in claim 1 , wherein R g is selected from the group consisting of hydrogen and optionally substituted 6 to 10-membered aryl-C 1-2 alkyl, said aryl being optionally substituted with up to 3 C 1-4 alkyl groups optionally substituted by up to three halogens.

5. A composition comprising a compound as claimed in claim 1 and a pharmaceutically acceptable excipient.

6. A compound which is any one of the following compounds, or a pharmaceutically acceptable salt thereof:

7. A compound which is any one of the following compounds, or a pharmaceutically acceptable salt thereof:

Assignments (4)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 5, 2019
From: IMPERIAL INNOVATIONS LIMITED
To: IMPERIAL WHITE CITY INCUBATOR LIMITED
Reel/Frame 050916/0635 →
CHANGE OF NAME Recorded Nov 5, 2019
From: IMPERIAL WHITE CITY INCUBATOR LIMITED
To: IMPERIAL COLLEGE INNOVATIONS LIMITED
Reel/Frame 050916/0945 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 15, 2018
From: BROWN, ROBERT; FUCHTER, MATTHEW JOHN; CHAPMAN-ROTHE, NADINE; SRIMONGKOLPITHAK, NITIPOL; CARON, JOACHIM
To: IMPERIAL INNOVATIONS LIMITED
Reel/Frame 044943/0952 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 8, 2015
From: SNYDER, JAMES P.; GANESH, THOTA; LIU, JIN; SUN, AIMING
To: EMORY UNIVERSITY
Reel/Frame 034661/0979 →
Continuity (2)
Provisional Application 61612694 · Mar 19, 2012
Related Publication 20150057263A1 · Feb 26, 2015