申请人:Richardson-Merrell Inc.
公开号:US04017514A1
公开(公告)日:1977-04-12
Substituted thiophenecarboxylic acids and esters and pharmaceutically acceptable salts thereof of the following general structure are useful as hypolipidemic agents: ##STR1## wherein R is selected from a straight or branched saturated hydrocarbon chain containing from 10 to 20 carbon atoms and a straight or branched unsaturated hydrocarbon chain containing from 10 to 20 carbon atoms and from 1 to 4 double bonds; R.sub.1 is selected from hydrogen, a straight or branched lower alkyl chain of from 1 to 6 carbon atoms, benzyl, phenethyl, pyridyl-methyl, alkane-poly-yl containing from 3 to 6 carbon atoms, 1,2,3,4,5,6-cyclohexanehexayl, and Z; Z is selected from ##STR2## wherein n is the integer 2 or 3; R.sub.2 is selected from a straight or branched lower alkyl chain of from 1 to 4 carbon atoms, and alkylcarbonyl wherein the alkyl moiety contains from 1 to 4 carbon atoms and may be straight or branched; R.sub.3 is selected from hydrogen and a straight or branched lower alkyl chain of from 1 to 4 carbon atoms with the proviso that when R.sub.3 is hydrogen, R.sub.2 is alkylcarbonyl; or when R.sub.2 is other than alkylcarbonyl, R.sub.2 and R.sub.3 taken together with the nitrogen atom to which each is attached form a monocyclic heterocyclic group selected from pyrrolidino, piperidino, morpholino, and piperazino; or ##STR3## wherein the sum of the integers m and p is equal to from 3 to 5; and R.sub.4 is a straight or branched lower alkyl chain of from 1 to 4 carbon atoms; X is an integer of from 1 to 6 with the proviso that when R.sub.1 is alkane-poly-yl or 1,2,3,4,5,6-cyclohexanehexayl, X is equal to from 2 to 6, and when R.sub.1 is other than alkane-poly-yl or 1,2,3,4,5,6-cyclohexanehexayl, X is equal to 1.
以下一般结构的取代噻吩羧酸和酯及其药学上可接受的盐,可用作降脂药物:##STR1## 其中,R选自含有10到20个碳原子的直链或支链饱和碳氢链和含有10到20个碳原子和1到4个双键的直链或支链不饱和碳氢链; R.sub.1选自氢、1到6个碳原子的直链或支链低碳基、苯甲基、苯乙基、吡啶基-甲基、含有3到6个碳原子的烷基-聚基、1,2,3,4,5,6-环己烷基和Z; Z选自##STR2## 其中n是整数2或3; R.sub.2选自含有1到4个碳原子的直链或支链低碳基、烷基羰基,其中烷基部分含有1到4个碳原子,可以是直链或支链; R.sub.3选自氢和含有1到4个碳原子的直链或支链低碳基,但当R.sub.3是氢时,R.sub.2是烷基羰基; 或者当R.sub.2不是烷基羰基时,R.sub.2和R.sub.3与它们各自连接的氮原子共同形成单环杂环基,所选的单环杂环基选自吡咯烷基、哌啶基、吗啉基和哌嗪基; 或##STR3## 其中整数m和p的和等于3到5; R.sub.4是含有1到4个碳原子的直链或支链低碳基; X是1到6的整数,但当R.sub.1为烷基-聚基或1,2,3,4,5,6-环己烷基时,X等于2到6,当R.sub.1不是烷基-聚基或1,2,3,4,5,6-环己烷基时,X等于1。