OBTAINING AND USING A TRICYCLIC PYRIMIDINONE COMPOUND AND A COMPOSITION THEREOF Russian patent published in 2025 - IPC C07D498/14 A61K31/5383 A61P9/10 A61P13/08 A61P25/28 A61P27/02 A61P27/06 

Abstract RU 2838186 C1

FIELD: chemistry.

SUBSTANCE: invention relates to a tricyclic pyrimidinone compound of formula (I) or a pharmaceutically acceptable salt thereof. In formula (I), the values of the variables are as follows: n1 and n2 are each independently equal to 0, 1 or 2; R1 is selected from -H, alkyl, deuterated alkyl, haloalkyl; R2 is selected from -H, alkyl, deuterated alkyl, haloalkyl; X1 is -O-; X2 is -O-; Ar is an arylene group, wherein the hydrogen atoms in the arylene are optionally substituted with one or more substituents and each of the substituents is independently selected from halogen; Y is -H, halogen, -OAr'; Ar' is selected from aryl or heteroaryl, where hydrogen atoms in aryl or heteroaryl are optionally substituted with one or more substitutes, each of which is independently selected from halogen, alkyl, deuterated alkyl, haloalkyl, alkoxy, haloalkoxy, deuterated alkoxy. Alkyl in "alkyl", "deuterated alkyl", "deuterated alkoxy", "haloalkyl", "haloalkoxy" and "alkoxy" each independently represents a C1-C10 linear or branched alkyl; "aryl" is 6-10 membered aryl; "arylene" is 6-10 membered arylene; "heteroaryl" is 5-10 membered heteroaryl ring containing 1-2 heteroatoms selected from N. Also disclosed is a method of producing said compound, a pharmaceutical composition based thereon and use thereof.

EFFECT: disclosed compound is a novel Lp-PLA2 inhibitor suitable for treating neurodegeneration-related diseases, such as Alzheimer's disease (AD), glaucoma and age-related macular degeneration (AMD), or cardiovascular diseases, including atherosclerosis.

13 cl, 2 tbl, 20 ex

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RU 2 838 186 C1

Authors

Gu, Chzhenkhua

Van, Duntsin

Khu, Yukhun

Dates

2025-04-11Published

2021-07-06Filed