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US 12,767,658 B2Granted
Tetracyclic pyrimidinone compound, preparation method therefor, and composition and use thereof
AssigneeNeusco Biotech Limited
InventorsQiong Xiao, Zhenghua Gu, Youhong Hu
Life of this patent
Estimating the term…
Abstract
Disclosed is a tetracyclic pyrimidinone compound represented by formula (I) or a pharmaceutically acceptable salt thereof. The compound having a structure represented by formula (I) is a new Lp-PLA2 inhibitor usable for treatment of neurodegenerative-related diseases, such as Alzheimer's disease (AD), glaucoma and age-related macular degeneration (AMD), or of cardiovascular diseases including atherosclerosis.
Claims15
A compound represented by formula (I):
- or a pharmaceutically acceptable salt thereof,
- wherein:
- n1, n2, n3, and n4 are each independently 0, 1, or 2;
- R1 and R2 are each independently selected from:
- —H, hydroxyl, cyano, halogen, alkyl, deuteroalkyl, hydroxyalkyl, haloalkyl, cycloalkyl, and alkoxyl;
- X1, X2, and X3 are each independently selected from:
- alkylene, —O—, —S—, or —NR′—;
- R′ is selected from:
- —H, alkyl, deuteroalkyl, or cycloalkyl;
- Ar is an unsubstituted or substituted arylene or heteroarylene;
- wherein, in the substituted arylene or heteroarylene, one or more hydrogen atoms are replaced by one or more substituents that are each independently selected from:
- halogen, alkyl, haloalkyl, alkoxyl, haloalkoxyl, deuteroalkyl, deuteroalkoxyl, hydroxyl, hydroxyalkyl, cyano, amino, monoalkyl- or dialkyl-substituted amino, nitro, carboxyl, aldehyde, cycloalkyl, heterocyclyl, aryl, or heteroaryl;
- Y is —H, halogen, alkyl, haloalkyl, haloalkoxyl, cycloalkyl, alkoxyl, deuteroalkyl, deuteroalkoxyl, —OAr′, —SAr′, —NH—Ar′, —NMe—Ar′, —NR′R″, or —R′″—Ar′;
- Ar′ is an unsubstituted or substituted aryl or heteroaryl;
- wherein, in the substituted aryl or heteroaryl, one or more hydrogen atoms are replaced by one or more substituents that are each independently selected from:
- halogen, alkyl, haloalkyl, alkoxyl, hydroxyl, hydroxyalkyl, haloalkoxyl, deuteroalkyl, deuteroalkoxyl, cyano, amino, nitro, carboxyl, aldehyde, cycloalkyl, heterocyclyl, aryl, or heteroaryl;
- R″ is alkyl;
- R′″ is alkylene;
- and
- Z is O or S.
17 more elements
Dependencies are inferred from the claim text.