11-01-2018 дата публикации
Номер: US20180009766A1
Принадлежит:
The present invention relates to pyrimidone compounds used as Lp-PLAinhibitors and pharmaceutical compositions thereof. The structure of the pyrimidone compounds is represented by general formula (I), wherein R, R, R, X, Ar, Y and n are defined as in the specification and claims. The compounds of general formula (I) in the present invention, stereoisomers and pharmaceutically acceptable salts thereof can be used as Lp-PLAinhibitors for preventing, treating and/or ameliorating diseases associated with the activity of Lp-PLAenzyme. 2. The compound of general formula I claim 1 , a stereoisomer claim 1 , deuterated form or pharmaceutically acceptable salt thereof according to claim 1 , wherein said compound of general formula I has one or more of the following features:{'sub': 1', '1', '6', '2', 'q, '(1) Ris H, C-Calkyl or —(CH)-(3-8 membered heteroaryl), wherein,'}{'sub': 1', '6', '2', 'q', '1', '4', '6', '10', '1', '4', '1', '4, 'q is 1, 2 or 3; said C-Calkyl, —(CH)-(3-8 membered heteroaryl) are optionally substituted with a group selected from the group consisting of C-Calkyl, C-Caryl, C-Calkoxy, halogen, halo-C-Calkyl;'}{'sub': 3', '1', '6', '3', '1', '4', '3, '(2) Ris H or C-Calkyl; preferably, Ris H or C-Calkyl; most preferably, Ris H;'}(3) n is 1 or 2;{'sub': 4', '4', '1', '6, '(4) X is O, S, or —N(R)—, wherein Ris H, C-Calkyl.'}3. The compound of general formula I claim 1 , a stereoisomer claim 1 , deuterated form or pharmaceutically acceptable salt thereof according to claim 1 , wherein Ris C-Calkyl claim 1 , C-Ccycloalkyl claim 1 , 3-8 membered heterocyclic radical claim 1 , C-Calkoxy claim 1 , C-Caryl claim 1 , —(CH)-(3-8 membered heteroaryl) or —NRR claim 1 , wherein claim 1 ,{'sub': 6', '10', '2', 'm', '1', '6', '6', '10', '1', '6', '3', '8', '1', '6, 'said 3-8 membered heterocyclic radical, C-Caryl, —(CH)-(3-8 membered heteroaryl) are optionally substituted with a group selected from the group consisting of: ═O, C-Calkyl, C-Caryl, C-Calkoxy, C-Ccycloalkyl, ...
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