| 摘要 |
Substituted azetidinone hypocholesterolemic agents of formula (I) or a pharmaceutically acceptable salt thereof, wherein: Ar<1> is aryl or R<3>-aryl; Ar<2> is aryl or R<4>-aryl; R<1> is selected from the group consisting of -(CH2)q-, wherein q is 2-6; -(CH2)e-Z-(CH2)r-, wherein Z is -O-, -C(O)-, phenylene, -NR<10>- or -S(O)0-2-, e is 0-5 and r is 0-5, provided that the sum of e and r is 1-6; -(C2-C6 alkenylene)-; and -(CH2)f-V-(CH2)g-, wherein V is C3-C6 cycloalkylene, f is 1-5 and g is 0-5, provided that the sum of f and g is 1-6; R<2> is -(lower alkylene)-COR<5> or -(CH=CH)-COR<5>; R<3> and R<4> are independently 1-3 substituents selected from lower alkyl, -OR<6>, -O(CO)R<6>, -O(CO)OR<9>, -O(CH2)1-5OR<6>, -O(CO)NR<6>R<7>, -NR<6>R<7>, -NR<6>(CO)R<7>, -NR<6>(CO)OR<9>, -NR<6>(CO)NR<7>R<8>, -NR<6>SO2R<9>, -COOR<6>, -CONR<6>R<7>, -COR<6>, -SO2NR<6>R<7>, S(O)0-2R<9>, -O(CH2)1-10-COOR<6>, -O(CH2)1-10CONR<6>R<7>, -(lower alkylene)-COOR<6>, -CH=CH-COOR<6>, -CF3, -CN, -NO2 and halogen; R<5> is -OR or -NRR<12>; R, R<6>, R<7>, R<8> and R<12> are independently selected from hydrogen, lower alkyl, aryl and aryl-substituted lower alkyl; R<9> is lower alkyl, aryl or aryl-substituted lower alkyl; and R<10> is hydrogen, lower alkyl, aryl lower alkyl or -C(O)R<6>; are disclosed, as well as a method of lowering serum cholesterol by administering said compounds, alone or in combination with a cholesterol biosynthesis inhibitor, and pharmaceutical compositions containing them. |
