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    Glutamate receptor antagonists: fused cycloalkylouinoxalinediones
    1.
    发明授权
    Glutamate receptor antagonists: fused cycloalkylouinoxalinediones 失效
    谷氨酸受体拮抗剂：稠合的环烷氧基亚油酸盐

    公开(公告)号：US5721234A

    公开(公告)日：1998-02-24

    申请号：US534526

    申请日：1995-10-23

    申请人： Christopher Franklin Bigge ,  Daniel Martin Retz

    发明人： Christopher Franklin Bigge ,  Daniel Martin Retz

    IPC分类号： C07C211/60 ,  C07C215/44 ,  C07C229/50 ,  C07C233/25 ,  C07C233/41 ,  C07C233/43 ,  C07C233/54 ,  C07C247/14 ,  C07C309/66 ,  C07D241/38 ,  A61K31/495 ,  C07D401/12 ,  C07D405/12

    CPC分类号： C07D241/38 ,  C07C211/60 ,  C07C215/44 ,  C07C229/50 ,  C07C233/25 ,  C07C233/41 ,  C07C233/43 ,  C07C233/54 ,  C07C247/14 ,  C07C309/66 ,  C07C2102/10

    摘要： Novel glutamate receptor antagonists represented by the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein Z is an alicyclic fused ring having 5 to 7 carbon atoms; R.sup.1 is hydrogen, an alkyl or an arylalkyl; and A is O, CH.sub.2, NR.sup.4, CH.sub.2 NR.sup.4, CN, tetrazole or CO wherein R.sup.4 is hydrogen, alkyl, hydroxyalkyl, aminoalkyl or aralkyl, wherein (i) when A is O, CH.sub.2, NR.sup.4 or CH.sub.2 NR.sup.4 then B is hydrogen, alkyl, alkenyl, alkynyl, aryl, aralkyl, hydroxyalkyl, alkoxy, aminoalkyl, heterocyclic, alkylheterocyclic, heterocyclic-methyl, heterocyclic-ethyl, alkylcarbonyl, cycloalkylcarbonyl, arylcarbonyl, aralkylcarbonyl, heterocyclic-carbonyl, alkylheterocyclic-carbonyl, or when A is NR.sup.4 or CH.sub.2 NR.sup.4 then B is a naturally occurring .alpha.-amino acid moiety joined by an amide bond or B joins with R.sup.4 and the nitrogen to form a four to seven membered heterocyclic ring, provided that when Z is a fused cyclohexyl ring and R.sup.4 is hydrogen then B is not hydrogen; (ii) when A is CN then B is not present and Z is not a fused cyclohexyl ring; (iii) when A is tetrazole then B is hydrogen or alkyl having 1 to 6 carbon atoms; and (iv) when A is CO then B is hydroxy, alkoxy, aralkoxy, alkyl having 1 to 6 carbon atoms, aralkyl, NR.sup.7 R.sup.8.

    摘要翻译： 由式“IMAGE”表示的新型谷氨酸受体拮抗剂或其药学上可接受的盐，其中Z是具有5至7个碳原子的脂环稠合环; R1是氢，烷基或芳基烷基; 并且A是O，CH 2，NR 4，CH 2 NR 4，CN，四唑或CO，其中R 4是氢，烷基，羟基烷基，氨基烷基或芳烷基，其中（i）当A是O，CH 2，NR 4或CH 2 NR 4时，B是氢， 烯基，炔基，芳基，芳烷基，羟基烷基，烷氧基，氨基烷基，杂环，烷基杂环，杂环 - 甲基，杂环 - 乙基，烷基羰基，环烷基羰基，芳基羰基，芳烷基羰基，杂环羰基，烷基杂环羰基，或当A为NR4或CH2NR4时 B是通过酰胺键连接的天然存在的α-氨基酸部分或B与R 4和氮连接形成4至7元杂环，条件是当Z为稠合环己基环且R 4为氢时，B不为 氢; （ii）当A为CN时，B不存在，Z不为稠环己基环; （iii）当A是四唑时，B是氢或具有1至6个碳原子的烷基; 和（iv）当A是CO时，B是羟基，烷氧基，芳烷氧基，具有1至6个碳原子的烷基，芳烷基，NR 7 R 8。