Thiazolopyrimidinone derivatives as PI3 kinase inhibitors
AssigneeGlaxoSmithKline LLC
InventorsHong Lin, Juan I. Luengo, Ralph A. Rivero, Mark James Schulz, Ren Xie, Jin Zeng
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Abstract
This invention relates to novel compounds of formula (I): and derivatives thereof useful for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3′ OH kinase family (hereinafter PI3 kinases), suitably, PI3Kα, PI3Kδ, PI3Kβ, and/or PI3Kγ.
Claims10
A compound of formula (I)
- wherein
- R1 is selected from the group consisting of:
- H, C1-3alkyl, —SC1-6alkyl, —OC1-6alkyl, NRaRb, hydroxy, —SH, NH—NH2, C3-6cycloalkyl, C4-6heterocycloalkyl, —SO2Ph, —OPh, —SPh, —SO2(C1-3alkyl), —O(arylalkyl), and phenyl;
- R2 is H or C1-3alkyl;
- R3 is selected from the group consisting of:
- C1-6alkyl, C3-7cycloalkyl, C4-6heterocycloalkyl, alkylcarboxy, aryl, arylalkyl, and heteroaryl;
- each R4 is independently selected from the group consisting of:
- C1-3alkyl, alkoxy, amide, and ester;
- n is 0-2;
- m is 0-3;
- and
- Ra and Rb are each independently H, or C1-3alkyl;
- or a pharmaceutically acceptable salt thereof.
A compound which is 5-methyl-4-{[2-methyl-3-(trifluoromethyl)phenyl]methyl}-2-(4-morpholinyl)[1,3]thiazolo[4,5-d]pyrimidin-7(4H)-one, or a pharmaceutically acceptable salt thereof.
A compound which is 4-[(3-chloro-2-methylphenyl)methyl]-5-ethyl-2-(4-morpholinyl)[1,3]thiazolo[4,5-d]pyrimidin-7(4H)-one, or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.