| 摘要 |
<p>Compounds which are inhibitors of cholesterol biosynthesis (by inhibiting de novo squalene biosynthesis), and thus are useful as hypocholesterolemic agents and antiatherosclerotic agents are provided which have the structure <CHEM> wherein m is 1, 2 or 3; n is 0, 1, 2 or 3; Y<1> and Y<2> are H or halogen; R<2>, R<3> and R<4> may be the same or different and are independently H, metal ion, C1 to C8 alkyl or C3 to C12 alkenyl; X is O, S, NH or NCH2R<1><5> wherein R<1><5> is H or C1 to C5 alkyl; and R<1> is R<5>-Q<1>-Q<2>-Q<3>- wherein Q<1>, Q<2> and Q<3> are the same or different and are independently <CHEM> a single bond, with the proviso that if Q<1> is a bond, then Q<2> and Q<3> are bonds and if Q<2> is a bond, then Q<3> is a bond, and wherein R<6> is H, alkyl, halo, or haloalkyl, R<7> is H, halo, alkyl or alkylthio; R<8> is H, halogen, trimethylsilyl or lower alkyl; R<9> is H or lower alkyl-; <CHEM> R<1><6>-C IDENTICAL C-CH2- (wherein R<1><6> is H or lower alkyl) or CH3(CH2)p where p is an integer from 2 to 7; R<1><0>, and R<1><1> are the same or different and are independently H, lower alkyl, halogen, haloalkyl or lower alkenyl or R<1><0> and R<1><1> can be taken together to form (CH2)s where s is an integer from 2 to 7; and R<1><3> an R<1><4> are the same or different and are independently lower alkyl, with the proviso that if all of Q<1>, Q<2> and Q<3> are bonds, then both R<1><0> and R<1><1> cannot be H and R<5> cannot be alkyl(CH2)p- with p</=4; including all stereoisomers thereof. New intermediates, new methods of preparation and a method for using such compounds to inhibit cholesterol biosynthesis are also provided.</p> |
