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    FUNGICIDAL MIXTURES
    5.
    发明申请
    FUNGICIDAL MIXTURES 审中-公开
    真菌混合物

    公开(公告)号：WO2009055514A2

    公开(公告)日：2009-04-30

    申请号：PCT/US2008080850

    申请日：2008-10-23

    申请人： DU PONT ,  GREGORY VANN ,  PASTERIS ROBERT JAMES

    发明人： GREGORY VANN ,  PASTERIS ROBERT JAMES

    IPC分类号： A01P3/00 ,  A01N43/78 ,  A01N43/80 ,  C07D261/00 ,  C07D277/00

    CPC分类号： A01N43/90 ,  A01N43/40 ,  A01N43/56 ,  A01N43/653 ,  A01N43/78 ,  A01N43/80 ,  C07D413/14 ,  C07D417/14 ,  A01N37/34 ,  A01N37/36 ,  A01N37/46 ,  A01N37/50 ,  A01N43/42 ,  A01N43/50 ,  A01N43/54 ,  A01N43/76 ,  A01N47/04 ,  A01N47/12 ,  A01N47/14 ,  A01N47/24 ,  A01N47/34 ,  A01N57/12 ,  A01N59/20 ,  A01N2300/00

    摘要： Disclosed is a fungicidal composition comprising (a) at least one compound selected from the compounds of Formula 1 N-oxides, and salts thereof, wherein R1, R2, A, G, W, Z1, X, J, and n are as defined in the disclosure, and (b) at least one additional fungicidal compound. Also disclosed is a method for controlling plant diseases caused by fungal plant pathogens comprising applying to the plant or portion thereof, or to the plant seed, a fungicidally effective amount of the aforesaid composition. Also disclosed is a composition comprising component (a) of aforesaid composition and at least one insecticide. Also disclosed are compounds of Formula 1A, 1B and 1C, wherein R1, R2, A, G, W, Z1, X, J, n, Z3, M and J1are as defined in the disclosure.

    摘要翻译： 公开了一种杀真菌组合物，其包含（a）至少一种选自式1化合物的化合物及其盐的化合物，其中R 1，R 2，A，G，W，Z 1，X，J和n如所定义 在本公开中，和（b）至少一种另外的杀真菌化合物。 还公开了一种控制由真菌植物病原体引起的植物病害的方法，包括向植物或其部分或植物种子施用杀真菌有效量的上述组合物。 还公开了包含上述组合物的组分（a）和至少一种杀虫剂的组合物。 还公开了式1A，1B和1C的化合物，其中R1，R2，A，G，W，Z1，X，J，n，Z3，M和J1如本公开所定义。

    TRANSDERMAL DELIVERY SYSTEMS OF BETA-LACTAM ANTIBIOTICS
    8.
    发明申请
    TRANSDERMAL DELIVERY SYSTEMS OF BETA-LACTAM ANTIBIOTICS 审中-公开
    BETA-LACTAM抗生素的转导递送系统

    公开(公告)号：WO2008072032A1

    公开(公告)日：2008-06-19

    申请号：PCT/IB2006/054724

    申请日：2006-12-10

    申请人： YU, Chongxi

    发明人： YU, Chongxi

    IPC分类号： C07D205/12 ,  C07D277/00 ,  C07D257/00 ,  A61P31/02

    CPC分类号： C07D499/00 ,  A61P31/04

    摘要： The novel positively charged pro-drugs of beta-lactam antibiotics in the general 'Structure 4' were designed. The positively charged amino group of the pro-drug not only makes the drugs soluble in water, but also bonds to the negative charge on the phosphate head group of membranes. This bonding will disturb the membrane a little bit and may make some room for the lipophilic portion of the prodrug. When the molecules of membrane move, the membrane may 'crack' a little bit due to the bonding of the prodrug. This will let the prodrug insert into the membrane. At pH 7.4, only about 99% of amino group is protonated. When the amino group is not protonated, the bonding between the amino group of the prodrug and the phosphate head group of membrane will disassociate, and the prodrug will enter the membrane completely. When the amino group of the prodrug flips to the other side of the membrane and thus become protonated, then the prodrug is pulled into the cytosol, a semi-liquid concentrated aqueous solution or suspension. The results suggest that the pro-drugs diffuses through human skin, blood-brain, and blood-milk barriers hundreds times faster than do beta-lactam antibiotics. In plasma, more than 90% of these pro-drugs can change back to the parent drugs in a few minutes. The prodrugs can be used medicinally in treating beta-lactam antibiotics-treatable conditions in humans or animals. The prodrugs can be administered transdermally for any kind of medical treatments. Controlled transdermal administration systems of the prodrug enables beta-lactam antibiotics to reach constantly optimal therapeutic blood levels to increase effectiveness and reduce the side effects of beta-lactam antibiotics. Another great benefit of transdermal administration of these pro-drugs is that administering medication, especially to children or animals, will be much easier.

    摘要翻译： 设计了一般“结构4”中β-内酰胺抗生素新型带正电荷的前药。 前药的带正电荷的氨基不仅使药物溶于水，而且还与磷酸盐头基上的负电荷键合。 这种键合会稍微干扰膜，并且可能为前体药物的亲油部分留下一些空间。 当膜的分子移动时，由于前药的结合，膜可能会“破裂”一点。 这将使前药插入膜中。 在pH 7.4时，只有约99％的氨基被质子化。 当氨基未被质子化时，前药的氨基与膜的磷酸盐头基之间的键合将脱离，并且前药将完全进入膜。 当前药的氨基转移到膜的另一侧，从而变质子化时，将前体药物拉入胞质溶胶，半液体浓缩的水溶液或悬浮液中。 结果表明，前药通过人类皮肤，血脑和血液 - 牛奶阻滞扩散比β-内酰胺抗生素快了数百倍。 在血浆中，超过90％的这些前药可以在几分钟内改变为母体药物。 前药可以在医学上用于治疗人或动物中的β-内酰胺抗生素治疗条件。 前药可以经皮给药用于任何种类的药物治疗。 前药的受控经皮给药系统使得β-内酰胺抗生素能够达到不断优化的治疗血液水平，以增加有效性并减少β-内酰胺抗生素的副作用。 透皮给药这些前药的另一大好处是给予药物，特别是给儿童或动物服用的药物将容易得多。