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1. 发明授权

US5654468A Heteroacetic acid derivatives 失效
标题翻译：异丁酸衍生物
公开(公告)号：US5654468A
公开(公告)日：1997-08-05
申请号：US680731
申请日：1996-07-15
申请人： Naokata Yokoyama, deceased , Gordon Northrop Walker , Alan Joseph Main
发明人： Naokata Yokoyama, deceased , Gordon Northrop Walker , Alan Joseph Main
IPC分类号： A61K31/165 , A61P3/06 , C07C41/00 , C07C229/18 , C07C229/36 , C07C233/56 , C07C235/72 , C07C323/37 , C07C323/52 , C07J41/00 , C07C229/00
CPC分类号： C07C323/52 , C07C229/18 , C07C229/36 , C07C233/56 , C07J41/0055
摘要： 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.1 is halogen, trifluoromethyl, lower alkyl, aryl, aryl-lower alkyl, cycloalokyl 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 cycloalkil-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.
摘要翻译：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; R1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。

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