Back to results
US 2005/0033052 A1Published application
Novel compounds
OwnerColin Leach, Ivan Pinto +2inventors
InventorsColin Leach, Ivan Pinto, Stephen Smith, Steven Stanway
Life of this patent
Estimating the term…
Abstract
Pyrimidone and pyridone compounds of the formula: are inhibitors of the enzyme Lp-PLA2 and are of use in therapy, in particular for treating atherosclerosis.
Claims14
A compound of formula (I):
- in which:
- R1 is an aryl group, optionally substituted by 1, 2, 3 or 4 substituents which may be the same or different selected from the group consisting of C(1-6)alkyl, C(1-6)alkoxy, C(1-6)alkylthio, hydroxy, halogen, CN, and mono to perfluoro-C(1-4)alkyl;
- R2 and R3 together with the ring carbon atoms to which they are attached form a fused 5- or 6-membered non-aromatic heterocyclyl ring containing 1 or 2 heteroatoms which may be the same or different selected from N, O and S, optionally substituted by 1, 2 or 3 substituents which may be the same or different selected from the group consisting of oxo, hydroxy, halogen, OR7, COR7, COOR7, CONR9R10, SR7, NR7COR8, SO2NR9R10, NR7SO2R8, and C(1-6)alkyl optionally substituted by 1, 2 or 3 substituents selected from the group consisting of hydroxy, halogen, OR7, COR7, carboxy, COOR7, CONR9R10 and NR9R10;
- R4 is hydrogen, C(1-6)alkyl which may be unsubstituted or substituted by 1, 2 or 3 substituents selected from the group consisting of hydroxy, halogen, OR7, COR7, carboxy, COOR7, CONR9R10, NR9R10, NR7COR8, mono- or di-(hydroxyC(1-6)alkyl)amino and N-hydroxyC(1-6)alkyl-N—C(1-6)alkylamino;
- or
- R4 is Het-C(0-4)alkyl in which Het is a 5- to 7-membered heterocyclyl ring comprising N and optionally O or S, and in which N may be substituted by COR7, COOR7, CONR9R10, or C(1-6)alkyl optionally substituted by 1, 2 or 3 substituents selected from the group consisting of hydroxy, halogen, OR7, COR7, carboxy, COOR7, CONR9R10 and NR9R10;
- R5 is an aryl or a heteroaryl ring optionally substituted by 1, 2, 3 or 4 substituents which may be the same or different selected from the group consisting of C(1-6)alkyl, C(1-6)alkoxy, C(1-6)alkylthio, arylC(1-6)alkoxy, hydroxy, halogen, CN, COR7, carboxy, COOR7, NR7COR8, CONR9R10, SO2NR9R10, NR7SO2R8, NR9R10, mono to perfluoro-C(1-4)alkyl and mono to perfluoro-C(1-4)alkoxy;
- R6 is an aryl or a heteroaryl ring which is further optionally substituted by 1, 2, 3 or 4 substituents which may be the same or different selected from the group consisting of C(1-18)alkyl, C(1-18)alkoxy, C(1-6)alkylthio, C(1-6)alkylsulfonyl, arylC(1-6)alkoxy, hydroxy, halogen, CN, COR7, carboxy, COOR7, CONR9R10, NR7COR8, SO2NR9R10, NR7SO2R8, NR9R10, mono to perfluoro-C(1-4)alkyl and mono to perfluoro-C(1-4)alkoxy, or C(5-10)alkyl;
- R7 and R8 are independently hydrogen or C(1-12)alkyl;
- R9 and R10 which may be the same or different is each selected from the group consisting of hydrogen, or C(1-12)alkyl, or R9 and R10 together with the nitrogen to which they are attached form a 5- to 7 membered ring optionally containing one or more further heteroatoms selected from the group consisting of oxygen, nitrogen and sulphur, and optionally substituted by one or two substituents selected from hydroxy, oxo, C(1-4)alkyl, C(1-4)alkylcarboxy, aryl, e.g. phenyl, or aralkyl;
- X is C(2-4)alkylene, optionally substituted by 1, 2 or 3 substituents selected from the group consisting of methyl and ethyl, CH═CH or (CH2)nS where n is 1, 2 or 3;
- and
- Y is CH or N;
- and
- pharmaceutically acceptable salts thereof.
12 more elements
(Deleted)
(Deleted)
Dependencies are inferred from the claim text.