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US 2010/0144765 A1Published application
5,6-trimethylenepyrimidin-4-one compounds
OwnerDeidre Mary Bernadette HICKEY, Robert John IFE +4inventors
InventorsDeidre Mary Bernadette HICKEY, Robert John IFE, Colin Andrew LEACH, Ivan Leo PINTO, Stephen Allan SMITH, Steven James STANWAY
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Abstract
Pyrimidone compounds of formula (I): are inhibitors of the enzyme Lp-PLA2 and are of use in treating atherosclerosis.
Claims5
-19. (canceled)
A method of treating Alzheimer's disease wherein the method comprises administering to a patient in need thereof an effective amount of a compound formula (I), neat, or admixed with a pharmaceutically acceptable carrier, wherein formula (I) is:
- in which:
- Ra and Rb together with the pyrimidine ring carbon atoms to which they are attached form a fused 5-membered carbocyclic ring;
- R2CH2X is 4-fluorobenzylthio;
- R3 is C(1-3)alkyl substituted by NR8R9;
- or
- R3 is Het-C(0-2)alkyl in which Het is a 5- to 7-membered heterocyclyl ring comprising N and in which N is unsubstituted or substituted by C(1-6)alkyl;
- R4 and R5 form a 4-(4-trifluoromethylphenyl)phenyl moiety;
- R8 and R9, which may be the same or different, are selected from the group consisting of hydrogen, or C(1-6)alkyl);
- and
- X is S;
- or a pharmaceutically acceptable salt thereof.
8 more elements
Dependencies are inferred from the claim text.