Cyclic pentapeptides and their preparation
    131.
    发明授权
    Cyclic pentapeptides and their preparation 有权
    循环五肽及其制备方法

    公开(公告)号:US07053047B2

    公开(公告)日:2006-05-30

    申请号:US10404124

    申请日:2003-04-02

    CPC classification number: C07K7/64 A61K38/00

    Abstract: This invention relates to cyclic peptides, with the following formula (I) (SEQ ID NO: 1), cyclo(Xaa-Arg-Pro-Ala-Lys)  (I) where Xaa is Ala, Gly, Glu, Gln, Asp, Asn, Arg or Lys. The cyclic peptides have thrombolytic effects. This invention also relates to cyclic peptide preparations.

    Abstract translation: 本发明涉及具有下式(I)(SEQ ID NO:1),<?在线公式描述=“在线公式”中的环状肽end =“lead”→>环(Xaa-Arg- Pro-Ala-Lys)(I)<?in-line-formula description =“In-line Formulas”end =“tail”?>其中Xaa是Ala,Gly,Glu,Gln,Asp,Asn,Arg或Lys。 环肽具有溶栓作用。 本发明还涉及环肽制剂。

    5-Benzoylamino-1,3-dioxacyclanes, the method for preparing the same and their use as PKC inhibitor
    132.
    发明申请
    5-Benzoylamino-1,3-dioxacyclanes, the method for preparing the same and their use as PKC inhibitor 审中-公开
    5-苯甲酰氨基-1,3-二氧环己烷,其制备方法及其作为PKC抑制剂的用途

    公开(公告)号:US20050043396A1

    公开(公告)日:2005-02-24

    申请号:US10674148

    申请日:2003-09-29

    CPC classification number: C07D319/06 C07D273/06 C07D321/12

    Abstract: The present invention discloses a series of benzoylamino-1,3-dioxacyclane compounds, of which compounds 1-21 were prepared via transacetalisation reaction between N-benzoylaminoglycol and 1,1,3,3-tetramethoxypropane; while compounds 22-48 were prepared via stereospecific acetalisation reaction between N-benzoylamino glycol and aromatic aldehyde, and if necessary, the nitro groups were reduced and further be salified with propane diacid and L-Arg or L-Lys. These compounds possess the structural type of PKC inhibitor and positive anti-inflammatory effect, and can be applied in medical fields as PKC inhibitor for corresponding therapy.

    Abstract translation: 本发明公开了一系列苯甲酰基氨基-1,3-二氧杂环烷化合物,其中化合物1-21是通过N-苯甲酰氨基甘氨酸与1,1,3,3-四甲氧基丙烷之间的转化反应制备的; 而化合物22-48通过N-苯甲酰氨基二醇和芳族醛之间的立体特异性缩醛化反应制备,并且如果需要,硝基还原,并进一步用丙烷二酸和L-Arg或L-Lys进行成盐。 这些化合物具有PKC抑制剂的结构型和阳性消炎作用,可作为PKC抑制剂用于医学领域,用于相应的治疗。

    Heavy metal chelating agent for oral administration, its synthesis and its uses in medicine and health protection
    133.
    发明授权
    Heavy metal chelating agent for oral administration, its synthesis and its uses in medicine and health protection 有权
    一种用于口服给药的新型重金属螯合剂,其合成及其在医药和保健中的应用

    公开(公告)号:US06306837B1

    公开(公告)日:2001-10-23

    申请号:US09473737

    申请日:1999-12-28

    CPC classification number: C07H15/12 Y10S514/836

    Abstract: The present invention relates to a new kind of heavy metal chelating agents and a preparation process and uses thereof. The said heavy metal chelating agents are expressed in &agr;-[D(+)glucose-1-yl-amino]-&bgr;3-mercapto-(S)-propanoic acid (abbreviated to NGP,I) and/or N,N′-di[D(+)glucose-1-yl]-L-cystine (abbreviated to NGCD,II). In the process of preparation, glucose and cysteine are reacted with a base, with a reducing agent, and the obtained products are acidified to give NGP,I, which can be used in and/or as drugs, health foods and food additives for accelerating the excretion of heavy metals including Pb, Cd, Hg, Al, Sb, As, etc. The structural feature of the compounds of the present invention is that they contain glucose and cysteirie in their molecules. Compared with the heavy metal-excreting drugs of prior art, the compounds of the present invention have four advantages, namely suitability for oral administration, high ability to accelerate the excretion of heavy metals, high selectivity and less toxicity.

    Abstract translation: 本发明涉及一种新型的重金属螯合剂及其制备方法和用途。 所述重金属螯合剂在α-[D(+)葡萄糖-1-基 - 氨基]-β-巯基 - (S) - 丙酸(缩写为NGP,I)和/或N, 二[D(+)葡萄糖-1-基] -L-胱氨酸(缩写为NGCD,II)。 在制备过程中,葡萄糖和半胱氨酸与碱反应,还原剂,将所得产物酸化,得到NGP,I,可用于和/或作为药物的保健食品和食品添加剂加速 重金属的排泄,包括Pb,Cd,Hg,Al,Sb,As等。本发明化合物的结构特征是它们在其分子中含有葡萄糖和半胱氨酸。 与现有技术的重金属排泄物相比,本发明的化合物具有四个优点,即口服适用性,加速重金属排泄能力高,选择性低,毒性小。

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