发明名称 TETRAHYDRO-6H-PYRAZINO[1,2-B]ISOQUINOLINE 1,4-DIONES AS APOPROTEIN B-100 INHIBITORS
摘要 <p>The prevent invention relates to compounds of formula (I) wherein R0 represents C¿3-8? cycloalkyl, optionally substituted by C1-4 alkyl; R?1¿ represents hydrogen, halogen, NO¿2?, CN, CHO, NHSO2R?3, NR4R5, NR6COR7¿, a 5-membered heteroaromatic ring optionally substituted by C¿1-4? alkyl, or a group X-Z; R?2¿ represents hydrogen or a prop-2-enyl group; Y represents methylene or difluoromethylene; X represents a C¿1-6? alkylene, C2-6 alkenylene, C3-6 alkynylene or an N-linked imine group; Z represents hydrogen, C1-4alkoxy, CO2R?6¿, or an optionally substituted 5- or 6-membered heteroaromatic or phenyl group, where optional substitution is selected from a group consisting of CO¿2?R?6, NR4R5¿, and NO¿2?; Ar represents a phenyl or 5- or 6-membered heteroaromatic group optionally substituted by one or more groups selected from halogen, cyano, C1-4 alkyl, C1-4 alkoxy, CF3, S(O)nR?5¿, NHSO¿2R?5, NO2, NR?4R5, NR6COR8, CO¿2R?6, CONR4R5, OCF¿3, and a 5-membered heterocyclic group optionally substituted by C1-4 alkyl; R3 represents C¿1-4? alkyl or trifluoromethyl; R?4 and R5¿ independently represent hydrogen or C¿1-4? alkyl, or together R?4 and R5¿ form a 3- to 6-membered cycloalkylamine ring; R?6 and R8¿ independently represent hydrogen or C¿1-4? alkyl; R?7¿ represents C¿1-4? alkyl or (CH2)mE, where m is 0 or 1 and E is a 5- or 6-membered heteroaromatic group; n is an integer from 0-3; and pharmaceutically acceptable derivatives thereof, to processes for their preparation; and their use in the treatment of conditions mediated by ApoB-100 regulation.</p>
申请公布号 WO1998016526(A1) 申请公布日期 1998.04.23
申请号 EP1997005636 申请日期 1997.10.15
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