IP Library Granted Patent US 9,938,290
Granted Patent B2
US 9,938,290 · App. 15/410,114 · Granted Apr 10, 2018

Tricyclic heterocyclic compounds as phosphoinositide 3-kinase inhibitors

Inventors: Stephen J. Shuttleworth (Oxfordshire, GB); Alexander R. Liam Cecil (Oxfordshire, GB); Thomas J. Hill (Oxfordshire, GB); Franck A. Silva (Oxfordshire, GB)
Assignee: Karus Therapeutics Limited
C07D495/14C07D491/147C07D519/00
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Quick Facts
Patent No.
US 9,938,290
App. No.
15/410,114
Granted
Apr 10, 2018
Kind
B2
Abstract

Compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein: W is O, N—H, N—(C 1 -C 10 alkyl) or S; each X is independently CH or N; R 1 is a 5 to 7-membered saturated or unsaturated, optionally substituted heterocycle containing at least 1 heteroatom selected from N or O; R 2 is (LQ) m Y; and each R 3 is independently H, C 1 -C 10 alkyl, aryl or heteroaryl, are surprisingly found to be inhibitors of PI3K-p110δ, and therefore have utility in therapy.

Claims (12)

1. A method of treating a cancer in a patient in need thereof, wherein the cancer is selected from the group consisting of: chronic myelogenous leukemia, acute myeloid leukemia, lymphoma, and solid tumor cancer, comprising administering to the patient a therapeutically effective amount of a compound represented by:

or a pharmaceutically acceptable salt thereof, wherein:

W is O;

X is CH;

R 2 is (LQ) m Y;

m is 1;

L is C 1 alkylene:

Q is a heterocyclic linker;

Y is selected from the group consisting of: H, C 1-10 alkyl, —OR 3 , and —C(O)N(R 3 ) 2 ; and

R 3 is H.

2. The method of claim 1 , wherein the cancer is a lymphoma.

3. The method of claim 1 , wherein Y is H.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 5, 2022
From: KARUS THERAPEUTICS LIMITED
To: CONVALIFE (SHANGHAI) CO. LIMITED
Reel/Frame 061315/0660 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 27, 2018
From: SHUTTLEWORTH, STEPHEN JOSEPH; CECIL, ALEXANDER RICHARD LIAM; HILL, THOMAS JAMES; SILVA, FRANCK ALEXANDRE
To: KARUS THERAPEUTICS LIMITED
Reel/Frame 045052/0293 →
Priority Claims (2)
GB 0914594.7 · Aug 20, 2009 · national
GB 1005584.6 · Apr 1, 2010 · national
Continuity (3)
Continuation 14920410 · Oct 22, 2015
Continuation 13388164
Related Publication 20180009826A1 · Jan 11, 2018