发明名称 TETRAHYDRO-6H-PYRAZINO[1,2-B]ISOQUINOLINE 1,4-DIONES AS APOPROTEIN B-100 INHIBITORS
摘要 The prevent invention relates to compounds of formula (I) wherein R<0> represents C3-8 cycloalkyl, optionally substituted by C1-4 alkyl; R<1> represents hydrogen, halogen, NO2, CN, CHO, NHSO2R<3>, NR<4>R<5>, NR<6>COR<7>, a 5-membered heteroaromatic ring optionally substituted by C1-4 alkyl, or a group X-Z; R<2> represents hydrogen or a prop-2-enyl group; Y represents methylene or difluoromethylene; X represents a C1-6 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 CO2R<6>, NR<4>R<5>, and NO2; 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>, NHSO2R<5>, NO2, NR<4>R<5>, NR<6>COR<8>, CO2R<6>, CONR<4>R<5>, OCF3, and a 5-membered heterocyclic group optionally substituted by C1-4 alkyl; R<3> represents C1-4 alkyl or trifluoromethyl; R<4> and R<5> independently represent hydrogen or C1-4 alkyl, or together R<4> and R<5> form a 3- to 6-membered cycloalkylamine ring; R<6> and R<8> independently represent hydrogen or C1-4 alkyl; R<7> represents C1-4 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.
申请公布号 WO9816526(A1) 申请公布日期 1998.04.23
申请号 WO1997EP05636 申请日期 1997.10.15
申请人 GLAXO GROUP LIMITED;LABAUDINIERE, RICHARD, FREDERIC;MARTRES, PAUL;DODIC, NERINA;DUMAITRE, BERNARD, ANDRE 发明人 LABAUDINIERE, RICHARD, FREDERIC;MARTRES, PAUL;DODIC, NERINA;DUMAITRE, BERNARD, ANDRE
分类号 C07D471/04;(IPC1-7):C07D471/04;A61K31/445 主分类号 C07D471/04
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