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345 条记录 (耗时 0.034 秒)

    Metformin-Cysteine Prodrug
    81.
    发明申请
    Metformin-Cysteine Prodrug 有权
    二甲双胍半胱氨酸前药

    公开(公告)号：US20110257432A1

    公开(公告)日：2011-10-20

    申请号：US13087673

    申请日：2011-04-15

    申请人： Thomas M. DiMauro

    发明人： Thomas M. DiMauro

    IPC分类号： C07C323/58 ,  C07C323/59

    CPC分类号： C07C323/58 ,  C07C323/59 ,  C07C381/00

    摘要： A metformin-cysteine prodrug. It is believed that the prodrug of the present invention will transport in the LAT1 and LAT2 transporter system. Because the LAT1 and LAT2 transporters are important and effective transporters of amino acids in both the small intestine and colon, it is believed that the LAT-transportable prodrugs of the present invention will be effectively absorbed both in small intestine and in the colon. The increased absorption window provided by the present invention should result in highly sustained plasma concentrations of metformin, thereby increasing the effectiveness of the medication and allowing for a single daily dose.

    摘要翻译： 二甲双胍半胱氨酸前药。 据信本发明的前药将在LAT1和LAT2转运体系中运输。 因为LAT1和LAT2转运蛋白是小肠和结肠中氨基酸的重要且有效的转运蛋白，所以相信本发明的LAT可转运前体药物将被有效地吸收在小肠和结肠中。 由本发明提供的增加的吸收窗口应该导致二甲双胍的高度持续的血浆浓度，从而增加药物的有效性并允许单次日剂量。

    Nucleophile-stable thioester generating compounds, methods of production and use
    82.
    发明授权
    Nucleophile-stable thioester generating compounds, methods of production and use 失效
    亲核稳定硫酯生成化合物，生产和使用方法

    公开(公告)号：US06977292B2

    公开(公告)日：2005-12-20

    申请号：US10332454

    申请日：2001-08-30

    申请人： Paolo Botti ,  James A. Bradburne ,  Stephen B. H. Kent

    发明人： Paolo Botti ,  James A. Bradburne ,  Stephen B. H. Kent

    IPC分类号： C07D317/32 ,  C07C323/52 ,  C07C323/59 ,  C07D317/34 ,  C07D319/06 ,  C07K1/00 ,  C07K1/02 ,  C07K1/04 ,  C07K7/00

    CPC分类号： C07K1/023 ,  C07C323/52 ,  C07K1/006 ,  C07K1/026 ,  C07K1/04

    摘要： The invention is directed to nucleophile-stable thioester generating compounds comprising a carboxyester thiol. The compounds have wide applicability in organic synthesis, including the generation of peptide-, polypeptide- and other polymer-thioesters. The invention is particularly useful for generating activated-thioesters from precursors that are made under conditions in which strong nucleophiles are employed, such as peptides or polypeptides made using Fmoc SPPS, as well as multi-step ligation or conjugation schemes that require (or benefit from the use of) compatible selective approaches for directing a specific ligation or conjugation reaction of interest.

    摘要翻译： 本发明涉及包含羧基酯硫醇的产生亲核试剂的硫代酯化合物。 这些化合物在有机合成中具有广泛的应用，包括产生肽，多肽和其他聚合物 - 硫酯。 本发明特别可用于从在其中使用强亲核试剂的条件下制备的前体产生活化硫酯，例如使用Fmoc SPPS制备的肽或多肽，以及需要（或从中获益）的多步连接或缀合方案 用于引导感兴趣的特异性连接或缀合反应的相容性选择性方法。

    Anti-inflammatory and immunomodulatory amino acid derivatives, their preparation and use
    84.
    发明授权
    Anti-inflammatory and immunomodulatory amino acid derivatives, their preparation and use 失效
    抗炎和免疫调节氨基酸衍生物，其制备和用途

    公开(公告)号：US06956059B2

    公开(公告)日：2005-10-18

    申请号：US10478819

    申请日：2002-05-20

    申请人： Keith Coupland

    发明人： Keith Coupland

    IPC分类号： A61K31/201 ,  A61K31/231 ,  A61P29/00 ,  A61P37/02 ,  C07C231/10 ,  C07C233/49 ,  C07C319/20 ,  C07C323/59 ,  A01M37/18

    CPC分类号： C07C233/49 ,  C07C323/59 ,  Y10S514/885 ,  Y10S514/886

    摘要： The present invention ralates to compounds of formula (I): wherein R is hydrogen (H) or C1-6 alkyl; and X is defined such that —NH—(X)—COOH is the residue of an amino acid, which amino acid may itself optionally be substituted at any pendant amino group thereof by a residue of a carboxylic acid or a derivative thereof; or a salt thereof. The use of these compounds, in particular as potential anti-inflammatory and immunomodulatory drugs, and their preparation are described

    摘要翻译： 本发明涉及式（I）化合物：其中R是氢（H）或C 1-6烷基; 并且X定义为使得-NH-（X）-COOH是氨基酸的残基，该氨基酸本身可以任意地被其任何侧氨基被羧酸或其衍生物的残基取代; 或其盐。 描述了这些化合物，特别是作为潜在的抗炎和免疫调节药物的用途及其制备