Bicyclic pyrazolone or isoxazolone derivatives (I) are new. Bicyclic pyrazolone or isoxazolone derivatives of formula (I) and their tautomers and salts are new. X : CR or N, one or two being N； Y : NR6 or O； R : H, halo, A, 1-3C haloalkyl, (1-3C)alkoxy(1-3C)alkyl, aryl, heterocyclyl, OH, OA, 1-3C haloalkoxy, aryloxy, CN, NO 2, SA, SOA, SO 2A, SO 2NH 2, SF 5, NH 2, NHA, NAA, COA, COOR3, CONR4R5, OCONR4R5, OCOA'COOA, OCOA'COOH or OCOA'CONR4R5； A : 1-6C alkyl； A' : 1-6C alkylene； R1, R1' : 5-16C alkyl, 5-12C cycloalkyl, aryl(1-4C)alkyl, heteroaryl(1-4C)alkyl, (5-12C)cycloalkyl(1-4C)alkyl or bicyclic, where aryl, heteroaryl, cycloalkyl and bicyclic are optionally substituted； R2 : H； R3 : H, A or benzyl； R4, R5 : H, A, aryl, 3-12C cycloalkyl, aryl(1-4C)alkyl or (3-12C)cycloalkyl(1-3C)alkyl； R6 : H； 1-10C alkyl； or optionally substituted aryl(1-4C)alkyl, heterocyclyl(1-4C)alkyl, (3-12C)cycloalkyl(1-4C)alkyl or 8-14C bicyclic. Independent claims are also included for: (1) a medicament comprising one or more (I) and optionally other active agents； (2) two processes for preparing (I). [Image] ACTIVITY : Antilipemic； Antidiabetic； Antiarteriosclerotic. MECHANISM OF ACTION : Endothelial lipase (EL) inhibitor. N-(2-methylbenzyl)-6-chloro-1,4-dimethyl-3-oxo-1,3-dihydropyrazolo[3,4-b]pyridine-2-carboxamide had IC 50 of 0.02 microM against the phospholipid-hydrolyzing activity of EL.
