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    • 3. 发明授权
    • Heteroacetic acid derivatives
    • 异丁酸衍生物
    • US5569674A
    • 1996-10-29
    • US358130
    • 1994-12-16
    • Naokato Yokoyama, deceasedGordon N. WalkerAlan J. Main
    • Naokato Yokoyama, deceasedGordon N. WalkerAlan J. Main
    • A61K31/165A61P3/06C07C41/00C07C229/18C07C229/36C07C233/56C07C235/72C07C323/37C07C323/52C07J41/00A61K31/24
    • C07C323/52C07C229/18C07C229/36C07C233/56C07J41/0055
    • Disclosed are compounds of formula ##STR1## wherein R is hydroxy, esterified hydroxy or etherified hydroxy;R.sub.1 is halogen, trifluoromethyl or lower alkyl;R.sub.2 is halogen, trifluoromethyl or lower alkyl;R.sub.3 is halogen, trifluoromethyl, lower alkyl, aryl, aryl-lower alkyl, cycloalkyl or cycloalkyl-lower alkyl; orR.sub.3 is the radical ##STR2## wherein R.sub.8 is hydrogen, lower alkyl, aryl, cycloalkyl, aryl-lower alkyl or cycloalkyl-lower alkyl; R.sub.9 is hydroxy or acyloxy; R.sub.10 represents hydrogen or lower alkyl; or R.sub.9 and R.sub.10 together represent oxo;R.sub.4 is hydrogen, halogen, trifluoromethyl or lower alkyl;X is --NR.sub.7, S or O;W is O or S;R.sub.5 represents hydrogen, lower alkyl or aryl-lower alkyl; andR.sub.6 represents hydrogen; orR.sub.5 and R.sub.6 together represent oxo provided that X represents --NR.sub.7 ;R.sub.7 represents hydrogen or lower alkyl;Z represents carboxyl, carboxyl derivatized as a pharmaceutically acceptable ester or as a pharmaceutically acceptable amide; and pharmaceutically acceptable salts thereof; which are useful as hypocholesteremic agents.
    • 公开了式(I)的化合物,其中R是羟基,酯化的羟基或醚化的羟基; R1是卤素,三氟甲基或低级烷基; R2是卤素,三氟甲基或低级烷基; R3是卤素,三氟甲基,低级烷基,芳基,芳基 - 低级烷基,环烷基或环烷基 - 低级烷基; 或R3是基团,其中R8是氢,低级烷基,芳基,环烷基,芳基 - 低级烷基或环烷基 - 低级烷基; R9是羟基或酰氧基; R 10表示氢或低级烷基; 或R 9和R 10一起代表氧代; R4是氢,卤素,三氟甲基或低级烷基; X是-NR 7,S或O; W为O或S; R5代表氢,低级烷基或芳基 - 低级烷基; R6代表氢; 或者R 5和R 6一起代表氧代,条件是X代表-NR7; R7代表氢或低级烷基; Z表示羧基,羧基衍生化为药学上可接受的酯或作为药学上可接受的酰胺; 及其药学上可接受的盐; 其可用作低胆固醇剂。