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    Fungicidal compositions and methods of making thereof
    2.
    发明授权
    Fungicidal compositions and methods of making thereof 有权
    杀真菌组合物及其制备方法

    公开(公告)号：US06291513B1

    公开(公告)日：2001-09-18

    申请号：US09609211

    申请日：2000-07-05

    申请人： Wendell G. Phillips ,  Michael K. Mao ,  Chun Ma ,  Thomas L. Fevig

    发明人： Wendell G. Phillips ,  Michael K. Mao ,  Chun Ma ,  Thomas L. Fevig

    IPC分类号： A01N4306

    CPC分类号： C07F7/083 ,  C07D333/38 ,  C07F7/0814

    摘要： The fungicidal compound 4,5-dimethyl-N-2-propenyl-2-(trimethylsilyl)-3-thiophenecarboxamide (Formula (I)) has shown superior and unexpected control of the growth of the soil-borne fungus Gaeumannomyces graminis (Gg). The present invention provides a novel compound for synthesizing the compound of Formula (I) which uses the compound 4-hydroxy-4,5-dimethyl-2-trimethylsilanyl-dihydrothiophene-3-carboxylic acid allylamide (Formula (II)) as well as novel compounds of synthesizing the allylamide. In addition, Formula (II) itself has unexpectedly been found to provide control of Gg. Therefore, the compounds having Formula (III): or an agronomic salts and compositions thereof are expected to provide such control as well; wherein: Q is —NH, S, or O; W is O, or S; X is —OH, —OAc, —OR, where R is lower alkyl; Y is S, O, or —NH; Z is —Si(R)3, —C(R)3, where R is lower alkyl; R1 is a lower alkyl, allyl, or propargyl; R2 is a lower alkyl or aryl; and R3 and R4 are independently chosen from hydrogen, a lower alkyl and aryl; optionally, R2 and R3 together form a 5- or 6-membered ring.

    摘要翻译： 杀真菌化合物4,5-二甲基-N-2-丙烯基-2-（三甲基甲硅烷基）-3-噻吩甲酰胺（式（I））显示出对土壤真菌Gaeumannomyces graminis（Gg）生长的优异和意想不到的控制， 。 本发明提供用于合成式（I）的化合物的新型化合物，其使用化合物4-羟基-4,5-二甲基-2-三甲基硅烷基 - 二氢噻吩-3-甲酸烯丙基酰胺（式（II））以及 合成烯丙基酰胺的新型化合物。 此外，公式（II）本身意外地被发现提供了GG的控制。 因此，具有式（III）的化合物或其农艺盐及其组合物预期也提供这种控制; 其中：Q是-NH，S或O; W是O或S; X是-OH，-OAc，-OR，其中R是低级烷基; Y是S，O或-NH; Z是-Si （R）3，-C（R）3，其中R是低级烷基; R 1是低级烷基，烯丙基或炔丙基; R 2是低级烷基或芳基; R 3和R 4独立地选自氢，低级烷基和芳基;任选地，R 2和R 3一起形成5-或6-元环。

    Compounds and methods for the treatment of cardiovascular, inflammatory and immune disorders
    5.
    发明授权
    Compounds and methods for the treatment of cardiovascular, inflammatory and immune disorders 失效
    用于治疗心血管，炎症和免疫疾病的化合物和方法

    公开(公告)号：US06420392B1

    公开(公告)日：2002-07-16

    申请号：US08669371

    申请日：1996-10-09

    申请人： Tesfaye Biftu ,  Xiong Cai ,  Sajjat Hussoin ,  Gurmit Grewal ,  T Y Shen

    发明人： Tesfaye Biftu ,  Xiong Cai ,  Sajjat Hussoin ,  Gurmit Grewal ,  T Y Shen

    IPC分类号： A01N4306

    CPC分类号： C07D405/04 ,  C07D207/09 ,  C07D307/12 ,  C07D307/14 ,  C07D333/16 ,  C07D333/18 ,  C07D333/20 ,  C07D405/12 ,  C07D407/12 ,  C07D409/12 ,  Y10S514/825 ,  Y10S514/826 ,  Y10S514/863 ,  Y10S514/912 ,  Y10S514/914 ,  Y10S514/921 ,  Y10S514/925

    摘要： 2,5-Diaryl tetrahydrofurans, 2,5-diaryl tetrahydrothiophenes, 1,3-diaryl cyclopentanes are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i.e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase. Also disclosed is a method to treat disorders mediated by PAF and/or leukotrienes that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier, to a patient in need of such therapy.

    摘要翻译： 公开了2,5-二芳基四氢呋喃，2,5-二芳基四氢噻吩，1,3-二芳基环戊烷，其减少趋化性和呼吸道爆发，导致在炎性或免疫反应期间形成多形核白细胞的有害氧自由基。 该化合物通过作为PAF受体拮抗剂，通过抑制酶5-脂氧合酶，或通过显示双重活性，即作为PAF受体拮抗剂和5-脂肪氧合酶抑制剂两者而表现出该生物学活性。 还公开了一种治疗由PAF和/或白三烯介导的病症的方法，其包括向有需要的患者施用有效量的一种或多种上述化合物或其药学上可接受的盐，任选地在药学上可接受的载体中 的这种疗法。