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    Compounds for use in the treatment of infection
    21.
    发明授权
    Compounds for use in the treatment of infection 失效
    用于治疗感染的化合物

    公开(公告)号：US07700646B2

    公开(公告)日：2010-04-20

    申请号：US11455889

    申请日：2006-06-20

    申请人： James C. Anderson ,  Catherine Headley ,  Paul D. Stapleton ,  Peter W. Taylor

    发明人： James C. Anderson ,  Catherine Headley ,  Paul D. Stapleton ,  Peter W. Taylor

    IPC分类号： A61K31/353 ,  C07D311/60 ,  C07D311/62

    CPC分类号： C07D311/62 ,  C07D311/60

    摘要： There is provided a novel compound of the general formula I in which each of R8 to R10 is hydrogen, aryl, C1-6 alkyl, trialkylsilyl or acyl; R1 to R5 are individually selected from hydrogen, hydroxy, C1-6 alkoxy and acyloxy; R6 and R7 are H, C1-4 alkyl, trialkylsilyl or acyl; X is O or NR, and R is H or Me; in which any of the alkyl groups including alkyl groups in alkoxy, acyl and acyloxy groups may be substituted by aryl, C1-4 alkyl, C1-4 alkoxy, hydroxyl, trialkylsiloxy or acyloxy groups; with the proviso that R2 and R3 are not both OH when R4 is H or OH, R1 and R5 are both H, and X is O. The amide compounds (X is NR) are analogues of epigallocatechin gallate or epicatechin galate, with an amide bond in place of the natural ester bond, with resistance to hydrolysis by esterase enzymes. The ester compounds (X is O) have a different hydroxylation pattern on the B ring as compared to the natural products. The compounds may be used to modulate the resistance to β-lactam antibiotics of various infections, especially methicillin resistant Staphylococcus aureus (MRSA). Pharmaceutical compositions containing the novel compounds and combinations of the novel compounds and β-lactam antibiotics are described.

    摘要翻译： 提供了通式I的新化合物，其中R 8至R 10各自为氢，芳基，C 1-6烷基，三烷基甲硅烷基或酰基; R 1至R 5分别选自氢，羟基，C 1-6烷氧基和酰氧基; R6和R7是H，C1-4烷基，三烷基甲硅烷基或酰基; X是O或NR，R是H或Me; 其中包括烷氧基，酰基和酰氧基中的烷基的任何烷基可以被芳基，C 1-4烷基，C 1-4烷氧基，羟基，三烷基甲硅烷氧基或酰氧基取代; 条件是当R 4为H或OH时，R 2和R 3不同时为OH，R 1和R 5都为H，且X为O.酰胺化合物（X为NR）为表没食子儿茶素没食子酸没食子酸酯或表儿茶素加成酸盐的类似物，具有酰胺 键代替天然酯键，具有抗酯酶的水解作用。 与天然产物相比，酯化合物（X为O）在B环上具有不同的羟基化模式。 这些化合物可用于调节对各种感染，特别是耐甲氧西林金黄色葡萄球菌（MRSA）的β-内酰胺抗生素的抗性。 描述了含有新化合物和新化合物和β-内酰胺抗生素的组合的药物组合物。

    Dimer digallate compositions
    28.
    发明申请
    Dimer digallate compositions 审中-公开
    二聚体digallate组合物

    公开(公告)号：US20040235941A1

    公开(公告)日：2004-11-25

    申请号：US10867160

    申请日：2004-06-14

    申请人： Mars, Incorporated

    发明人： Leo J. Romanczyk JR. ,  Marc E. Lippman

    IPC分类号： C08G002/00 ,  A61K031/353 ,  C07D45/14

    CPC分类号： C07H17/06 ,  A61K31/35 ,  C07D311/32 ,  C07D311/60 ,  C07D311/62

    摘要： A process is disclosed for the production of polyphenol oligomers having n polyphenol monomeric units, n being an integer from 2-18. The process includes coupling of a protected polyphenol, having protected phenolic hydroxyl groups, with a C-4 functionalized polyphenol monomer. The protected polyphenol may be a protected polyphenol monomer or a protected polyphenol oligomer having 2-17 monomeric units. Advantageously, polyphenol monomeric units forming the polyphenol oligomers may be the same or different flavanoid compounds.

    摘要翻译： 公开了用于生产具有多酚单体单元的多酚低聚物的方法，n为2-18的整数。 该方法包括将被保护的酚羟基的被保护的多酚与C-4官能化的多酚单体的偶联。 受保护的多酚可以是受保护的多酚单体或具有2-17单体单元的被保护的多酚低聚物。 有利地，形成多酚低聚物的多酚单体单元可以是相同或不同的类黄酮化合物。

    Process for preparing procyanidin(4-6 or 4-8) oligomers and their derivatives
    30.
    发明授权
    Process for preparing procyanidin(4-6 or 4-8) oligomers and their derivatives 失效
    原花青素（4-6或4-8）寡聚体及其衍生物的制备方法

    公开(公告)号：US06207842B1

    公开(公告)日：2001-03-27

    申请号：US08948226

    申请日：1997-10-09

    申请人： Leo J. Romanczyk, Jr. ,  Alan P. Kozikowski ,  Werner Tueckmantel

    发明人： Leo J. Romanczyk, Jr. ,  Alan P. Kozikowski ,  Werner Tueckmantel

    IPC分类号： C07D31126

    CPC分类号： C07H17/06 ,  A61K31/35 ,  C07D311/32 ,  C07D311/60 ,  C07D311/62

    摘要： A process is disclosed for the production of polyphenol oligomers having n polyphenol monomers, n being an integer from 2-18. The process includes coupling of a protected polyphenol, having protected phenolic hydroxyl groups, with a C-4 functionalized polyphenol monomer. The protected polyphenol may be a protected polyphenol monomer or a protected polyphenol oligomer having 2-17 monomers. Advantageously, polyphenol monomers forming the polyphenol oligomers may be the same or different.

    摘要翻译： 公开了一种制备具有n多酚单体的多酚低聚物的方法，n是2-18的整数。 该方法包括将被保护的酚羟基的被保护的多酚与C-4官能化的多酚单体的偶联。 受保护的多酚可以是受保护的多酚单体或具有2-17个单体的被保护的多酚低聚物。 有利地，形成多酚低聚物的多酚单体可以相同或不同。