| 摘要 |
The present invention relates to novel 3,4-dihydro-1H-pyrimido[1,6-a]pyrimidin-6(2H)-one compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease. |
| 主权项 |
1. A compound of Formula (I) or a pharmaceutically acceptable salt thereof,wherein:
R1 is selected from the group consisting of cyclopropyl, —CH2—Ar and CH2—(C═O)—N(Ra)(Rb), wherein
Ar is phenyl, optionally substituted with one or more substituents independently selected from the group consisting of halo, OCH3, and CH3, andRa and Rb are each independently H or C1-3alkyl,or Ra, Rb, together with the nitrogen atom to which they are attached, join together to form a nitrogen containing heterocyclic ring selected from the group consisting of pyrrolidinyl, morpholinyl, piperazinyl and piperidinyl, wherein the nitrogen containing heterocyclic ring is optionally substituted with one or more substituents independently selected from the group consisting of C1-3alkyl and halo; R2 is F or H, R3 is F or —O—Ar′, wherein Ar′ is phenyl substituted with one or more substituents independently selected from the group consisting of halo and CF3, and R4 is selected from the group consisting of H, F and CN. |
