DIHYDROIMIDAZO[1,5-B]ISOQUINOLINE-1,3-DIONES AS APOPROTEIN B-100 INHIBITORS

摘要

The present invention relates to compounds of formula (I), wherein R<0> represents C3-8cycloalkyl, optionally substituted by C1-4alkyl; 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 C1-4alkyl, or a group X-Z; R<2> represents hydrogen or C1-6alkyl; Y represents methylene or difluoromethylene; X represents a C1-6alkylene, C2-6alkenylene, C3-6alkynylene 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, C1-4alkyl, C1-4alkoxy, 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 C1-4alkyl; R<3> represents C1-4alkyl or trifluoromethyl; R<4> and R<5> independently represent hydrogen or C1-4alkyl, or together R<4> and R<5> form a 3- to 6-membered cycloalkylamine ring; R<6> and R<8> independently represent hydrogen or C1-4alkyl; R<7> represents C1-4alkyl 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.