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US 12,630,551 B2Granted
Endocyclic pyrimidinone compounds, and preparation methods, compositions and use thereof
AssigneeNeusco Biotech Limited
InventorsZhenghua Gu, Dongqin Wang
Life of this patent
Estimating the term…
Abstract
Disclosed is an endocyclic pyrimidinone compound of Formula (I) or a pharmaceutically acceptable salt thereof, which is an entirely new Lp-PLA2 inhibitor useful in treating neurodegeneration-related diseases such as Alzheimer's disease (AD), glaucoma and age-related macular degeneration (AMD), or cardiovascular diseases including atherosclerosis.
Claims10
A compound of Formula (I) or a pharmaceutically acceptable salt thereof,
- wherein
- n1, n2, and n3 are each independently 0, 1, or 2;
- R1 and R2 are each independently selected from the group consisting of —H, hydroxyl, cyano, halogen, alkyl, deuterated alkyl, deuterated alkoxy, hydroxyalkyl, haloalkyl, haloalkoxy, cycloalkyl, alkoxy, arylene, or heteroarylene;
- X1 and X2 are each independently selected from the group consisting of alkylene, —O—, —S—, or —NR′—,
- R′ is selected from the group consisting of —H, alkyl, deuterated alkyl, or cycloalkyl;
- Ar is arylene or heteroarylene, wherein hydrogens in the arylene or heteroarylene are each optionally substituted with one or more substituents, and the substituents are each independently selected from the group consisting of halogen, alkyl, deuteroalkyl, haloalkyl, alkoxy, deuteroalkoxy, haloalkoxy, hydroxy, hydroxyalkyl, cyano, amino, monoalkyl- or dialkyl-substituted amino, nitro, carboxy, formyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl;
- Y is selected from the group consisting of —H, halogen, alkyl, haloalkyl, haloalkoxy, cycloalkyl, alkoxy, deuterated alkyl, deuterated alkoxy, hydroxy, hydroxyalkyl, cyano, arylene, heteroarylene, —OAr′, —SAr′, —NR″—Ar′, —NR″R″, or —R′″—Ar′;
- Ar′ is aryl or heteroaryl, wherein hydrogens in the aryl or heteroaryl are optionally substituted with one or more substituents, the substituents are each independently selected from the group consisting of halogen, alkyl, haloalkyl, alkoxy, hydroxy, hydroxyalkyl, haloalkoxy, deuterated alkyl, deuterated alkoxy, cyano, amino, nitro, carboxy, formyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl;
- R″ is H—, alkyl, or cycloalkyl;
- R′″ is alkylene;
- Z is O or S.
8 more elements
Dependencies are inferred from the claim text.