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US 2016/0108057 A1Published application
Tricyclic heterocyclic compounds as phosphoinositide 3-kinase inhibitors
AssigneeKarus Therapeutics Limited
InventorsStephen J. Shuttleworth, Alexander R. Liam, Thomas J. Hill, Franck A. Silva
Life of this patent
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Abstract
Compounds of formula (I) or a pharmaceutically acceptable sail thereof, wherein: W is O, N—H, N—(C1-C10 alkyl) or S; each X is independently CH or N; R1 is a 5 to 7-membered saturated or unsaturated, optionally substituted heterocycle containing at least 1 heteroatom selected from N or O; R2 is (LQ)mY; and each R3 is independently H, C1-C10 alkyl, aryl or heteroaryl, are surprisingly found to be inhibitors of PI3K-p110δ, and therefore have utility in therapy.
Claims11
A compound represented by formula I:
- or a pharmaceutically acceptable salt thereof, wherein:
- W is O;
- X is CH;
- R2 is (LQ)mY;
- m is 1;
- L is C1alkylene;
- Q is selected from the group consisting of:
- a direct bond, —NR3—, and a heterocyclic linker;
- Y is selected from the group consisting of:
- H, C1-10alkyl, heterocycle, —OR3, and C(O)N(R3)2;
- and
- R3 is independently selected for each occurrence from II or C1-C10 alkyl.
9 more elements
A compound represented by:
- or a pharmaceutically acceptable salt thereof, wherein:
- W is O;
- X is CH;
- R2 is (LQ)mY;
- m is 1 or 2;
- L is independently selected for each occurrence from C1alkylene and C2alkenylene;
- Q is independently selected for each occurrence from the group consisting of:
- —NR3—, —C(O)—, —C(O)NR3—, —NR4R5—, and —C(O)NR4R5, where R4 and R5 together with the nitrogen to which they are attached form a 5 to 7-membered heterocycle linker;
- Y is selected from the group consisting of H, C1-C10alkyl, C3-C10 cycloalkyl, —OR3, —N(R3)2, —SO2—R3, —SO2—N(R3)2, halogen, —C(halogen)bR3(3-b), and —CN;
- b is from 1 to 3;
- and
- each R3 is independently H or C1-C10alkyl.
9 more elements
Dependencies are inferred from the claim text.