5-Benzoylamino-1,3-dioxacyclanes, the method for preparing the same and their use as PKC inhibitor
    1.
    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。

    Carboline-3-carboxylic acid modified related sequences of Ala-Arg-Pro-Ala-Lys, their synthesis and use as thromobolytic agent
    2.
    发明申请
    Carboline-3-carboxylic acid modified related sequences of Ala-Arg-Pro-Ala-Lys, their synthesis and use as thromobolytic agent 有权
    羧酸修饰的Ala-Arg-Pro-Ala-Lys相关序列,它们的合成和用作溶血剂

    公开(公告)号:US20050080015A1

    公开(公告)日:2005-04-14

    申请号:US10680293

    申请日:2003-10-08

    CPC classification number: C07K14/75 A61K38/00

    Abstract: The present invention relates to the protected intermediates and the deprotected products of P6A, related to the protected pseudopeptides introducing the protected intermediateds of P6A to 3S-(2-Boc)-1,2,3,4-tetrahydro-β-carboline-3-carboxylic acid and the deprotected pseudopeptides, related to the protected pseudopeptides introducing the protected intermediateds of P6A to 3S-1,2,3,4-tetrahydro-β-carboline-3-carboxylic acid benzyl ester, related to the methods for their preparation, and related to their use as the thrombolytic agents.

    Abstract translation: 本发明涉及受保护的中间体和P6A的去保护产物,其与被保护的假肽相关,引入受保护的中间体P6A至3S-(2-Boc)-1,2,3,4-四氢-β-咔啉-3 羧酸和去保护的假肽,与保护的假肽相关,引入受保护的中间体P6A至3S-1,2,3,4-四氢-β-咔啉-3-羧酸苄酯,涉及其制备方法 ,并且与它们作为溶栓剂的用途有关。

    Carboline-3-carboxylic acid modified related sequences of Ala-Arg-Pro-Ala-Lys, their synthesis and use as thromobolytic agent
    3.
    发明授权
    Carboline-3-carboxylic acid modified related sequences of Ala-Arg-Pro-Ala-Lys, their synthesis and use as thromobolytic agent 有权
    羧酸修饰的Ala-Arg-Pro-Ala-Lys相关序列,它们的合成和用作溶血剂

    公开(公告)号:US07138491B2

    公开(公告)日:2006-11-21

    申请号:US10680293

    申请日:2003-10-08

    CPC classification number: C07K14/75 A61K38/00

    Abstract: The present invention relates to the protected intermediates and the deprotected products of P6A, related to the protected pseudopeptides introducing the protected intermediateds of P6A to 3S-(2-Boc)-1,2,3,4-tetrahydro-β-carboline-3-carboxylic acid and the deprotected pseudopeptides, related to the protected pseudopeptides introducing the protected intermediateds of P6A to 3S-1,2,3,4-tetrahydro-β-carboline-3-carboxylic acid benzyl ester, related to the methods for their preparation, and related to their use as the thrombolytic agents.

    Abstract translation: 本发明涉及受保护的中间体和P6A的去保护产物,其与被保护的假肽相关,引入受保护的中间体P6A至3S-(2-Boc)-1,2,3,4-四氢-β-咔啉-3 羧酸和去保护的假肽,与保护的假肽相关,引入受保护的中间体P6A至3S-1,2,3,4-四氢-β-咔啉-3-羧酸苄酯,涉及其制备方法 ,并且与它们作为溶栓剂的用途有关。

    Heavy metal chelating agent for oral administration, its synthesis and its uses in medicine and health protection
    4.
    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。

    Cyclic pentapeptides and their preparation
    5.
    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。

    Direct metal printing with stereolithography

    公开(公告)号:US11135649B2

    公开(公告)日:2021-10-05

    申请号:US16286006

    申请日:2019-02-26

    Abstract: An additive manufacturing process for forming a metallic layer on the surface of the substrate includes fabricating a substrate from a polymerizable composition by a stereolithographic process, and contacting the reactive surface with an aqueous solution including a metal precursor. The metal precursor includes a metal, and the polymerizable composition includes a multiplicity of multifunctional components. Each multifunctional component includes a reactive moiety extending from a surface of the substrate to form a reactive surface. An interface between the reactive surface and the aqueous solution is irradiated to form nanoparticles including the metal. The nanoparticles are chemically coupled to the reactive surface by reactive moieties, thereby forming a metallic layer on the surface of the substrate.

    DIRECT METAL PRINTING WITH STEREOLITHOGRAPHY
    10.
    发明申请

    公开(公告)号:US20190262897A1

    公开(公告)日:2019-08-29

    申请号:US16286006

    申请日:2019-02-26

    Abstract: An additive manufacturing process for forming a metallic layer on the surface of the substrate includes fabricating a substrate from a polymerizable composition by a stereolithographic process, and contacting the reactive surface with an aqueous solution including a metal precursor. The metal precursor includes a metal, and the polymerizable composition includes a multiplicity of multifunctional components. Each multifunctional component includes a reactive moiety extending from a surface of the substrate to form a reactive surface. An interface between the reactive surface and the aqueous solution is irradiated to form nanoparticles including the metal. The nanoparticles are chemically coupled to the reactive surface by reactive moieties, thereby forming a metallic layer on the surface of the substrate.

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