Synthetic drug molecules that mimic metalloenzymes
    4.
    发明授权
    Synthetic drug molecules that mimic metalloenzymes 失效
    合成药物分子,模拟金属酶

    公开(公告)号:US5217966A

    公开(公告)日:1993-06-08

    申请号:US822593

    申请日:1992-01-17

    申请人: Thomas C. Bruice

    发明人: Thomas C. Bruice

    IPC分类号: C07D487/22

    CPC分类号: C07D487/22

    摘要: Synthetic enzymes that mimic the catalytic activity of naturally occurring enzymes by providing catalytic sites enclosed in cages that protect the sites from undesirable molecules and attract and permit entry of the relevant substrates are disclosed. Molecules that mimics the catalytic activity of superoxide dismutase and catalase, pharmaceutical compositions containing these molecules, and methods for using these compositions are also disclosed.

    摘要翻译: 公开了通过提供封闭在笼中的催化位点来模拟天然存在的酶的催化活性的合成酶,其保护位点免受不期望的分子的吸引并允许相关底物进入。 还公开了模拟超氧化物歧化酶和过氧化氢酶的催化活性的分子,含有这些分子的药物组合物,以及使用这些组合物的方法。

    Synthetic drug molecules that mimic metalloenzymes
    5.
    发明授权
    Synthetic drug molecules that mimic metalloenzymes 失效
    合成药物分子的MIMIC METALLOENZYMES

    公开(公告)号:US5202317A

    公开(公告)日:1993-04-13

    申请号:US582626

    申请日:1990-09-13

    申请人: Thomas C. Bruice

    发明人: Thomas C. Bruice

    CPC分类号: C07D487/22

    摘要: Synthetic enzymes that mimic the catalytic activity of naturally occurring enzymes by providing catalytic sites enclosed in cages that protect the sites from undesirable molecules and attract and permit entry of the relevant substrates are disclosed. Molecules that mimics the catalytic activity of superoxide dismutase and catalase, pharmaceutical compositions containing these molecules, and methods for using these compositions are also disclosed.

    摘要翻译: 公开了通过提供封闭在笼中的催化位点来模拟天然存在的酶的催化活性的合成酶,其保护位点免受不期望的分子的吸引并允许相关底物进入。 还公开了模拟超氧化物歧化酶和过氧化氢酶的催化活性的分子,含有这些分子的药物组合物,以及使用这些组合物的方法。

    Triheterocyclic peptides capable of binding the minor and major grooves
of DNA
    7.
    发明授权
    Triheterocyclic peptides capable of binding the minor and major grooves of DNA 失效
    能够结合DNA的小槽和主槽的三重杂环肽

    公开(公告)号:US5698674A

    公开(公告)日:1997-12-16

    申请号:US226934

    申请日:1994-04-13

    CPC分类号: C07D207/34

    摘要: The present invention provides a triheterocyclic peptide having first, second, and third 5-member heterocyclic moieties having the following formula CR.sub.3 CONH--Q.sup.1 --CONH--Q.sup.2 --CONH--Q.sup.3 -CONH--(CR.sub.3).sub.S --B, wherein Q.sup.1 is selected from a group consisting of: ##STR1## wherein Q.sup.2 is selected from a group consisting of: ##STR2## wherein Q.sup.3 is selected from a group consisting of: ##STR3## wherein at least one of A and Z is other than C; wherein A is C, N, O, or S; wherein B is N(CR.sub.3).sub.n or C(NH.sub.2).sub.2 ; wherein n is an integer from 2 to 10; wherein P is H, a lower alkyl or a halogen; wherein Q1, Q2, and Q3 are the same or different; wherein R is H, a lower alkyl group; wherein S is an integer from 1 to 10; wherein X' represents CR.sub.3, (CR.sub.2).sub.n --NRY, or (CR.sub.2).sub.n --CR.sub.2 Y; wherein X" represents CR.sub.3, (CR.sub.2).sub.n --NRY, or (CR.sub.2).sub.n --CR.sub.2 Y; wherein X'" represents CR.sub.3, (CR.sub.2).sub.n --NRY, or (CR.sub.2).sub.n --CR.sub.2 Y; wherein Y is a polyamine group, and wherein Z is C or N; wherein at least one of X', X", or X'" is other than CR.sub.3.

    摘要翻译: 本发明提供具有具有下式CR 3 CONH-Q1-CONH-Q2-CONH-Q3-CONH-(CR 3)SB的第一,第二和第三个5元杂环部分的三杂环肽,其中Q1选自 其中Q 2选自:其中Q 3选自:其中A和Z中的至少一个不是C;其中Q 3选自: 其中A是C,N,O或S; 其中B是N(CR 3)n或C(NH 2)2; 其中n是2至10的整数; 其中P是H,低级烷基或卤素; 其中Q1,Q2和Q3相同或不同; 其中R是H,低级烷基; 其中S为1至10的整数; 其中X'代表CR3,(CR2)n-NRY或(CR2)n-CR2Y; 其中X“表示CR3,(CR2)n-NRY或(CR2)n-CR2Y; 其中X“表示CR 3,(CR 2)n-NRY或(CR 2)n-CR 2 Y; 其中Y是多胺基团,并且其中Z是C或N; 其中X',X“或X”'中的至少一个不是CR 3。