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    SYNTHESIS OF TETRACYCLINES AND ANALOGUES THEREOF
    1.
    发明申请
    SYNTHESIS OF TETRACYCLINES AND ANALOGUES THEREOF 有权
    四环素及其类似物的合成

    公开(公告)号：US20100130451A1

    公开(公告)日：2010-05-27

    申请号：US12296223

    申请日：2007-04-06

    申请人： Andrew G. Myers ,  Jason D. Brubaker ,  Cuixiang Sun ,  Qiu Wang

    发明人： Andrew G. Myers ,  Jason D. Brubaker ,  Cuixiang Sun ,  Qiu Wang

    IPC分类号： A61K31/65 ,  C07C237/26 ,  A61P31/00

    CPC分类号： C07C237/26 ,  C07C323/61 ,  C07C2601/02 ,  C07C2601/08 ,  C07C2603/46 ,  C07C2603/52 ,  C07D205/04 ,  C07D213/56 ,  C07D277/30 ,  C07D277/66 ,  C07D295/155

    摘要： The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The modular synthesis of tetracyclines and tetracycline analogs described provides an efficient and enantioselective route to a variety of tetracycline analogs and polycyclines previously inaccessible via earlier tetra-cycline syntheses and semi-synthetic methods. These analogs may be used as anti-microbial agents or anti-pro liferative agents in the treatment of diseases of humans or other animals.

    摘要翻译： 四环素类抗生素在过去50年的传染病治疗中发挥了重要作用。 然而，四环素在人类和兽医药物中的使用量的增加已经导致了以前易受四环素抗生素影响的许多生物体之间的抵抗。 所描述的四环素和四环素类似物的模块合成为通过较早的四环合成和半合成方法先前无法接近的各种四环素类似物和聚环状体提供了有效和对映选择性的途径。 这些类似物可用作治疗人类或其他动物疾病的抗微生物剂或抗增效剂。

    Synthesis of tetracyclines and analogues thereof
    2.
    发明授权
    Synthesis of tetracyclines and analogues thereof 有权
    四环素及其类似物的合成

    公开(公告)号：US08486921B2

    公开(公告)日：2013-07-16

    申请号：US12296223

    申请日：2007-04-06

    申请人： Andrew G. Myers ,  Jason D. Brubaker ,  Cuixiang Sun ,  Qiu Wang

    发明人： Andrew G. Myers ,  Jason D. Brubaker ,  Cuixiang Sun ,  Qiu Wang

    IPC分类号： A61K31/65 ,  C07C237/26

    CPC分类号： C07C237/26 ,  C07C323/61 ,  C07C2601/02 ,  C07C2601/08 ,  C07C2603/46 ,  C07C2603/52 ,  C07D205/04 ,  C07D213/56 ,  C07D277/30 ,  C07D277/66 ,  C07D295/155

    摘要： The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The modular synthesis of tetracyclines and tetracycline analogs described provides an efficient and enantioselective route to a variety of tetracycline analogs and polycyclines previously inaccessible via earlier tetra-cycline syntheses and semi-synthetic methods. These analogs may be used as anti-microbial agents or anti-pro liferative agents in the treatment of diseases of humans or other animals.

    摘要翻译： 四环素类抗生素在过去50年的传染病治疗中发挥了重要作用。 然而，四环素在人类和兽医药物中的使用量的增加已经导致了以前易受四环素抗生素影响的许多生物体之间的抵抗。 所描述的四环素和四环素类似物的模块合成为通过较早的四环合成和半合成方法先前无法接近的各种四环素类似物和聚环状体提供了有效和对映选择性的途径。 这些类似物可用作治疗人类或其他动物疾病的抗微生物剂或抗增效剂。

    Synthesis of enone intermediate
    3.
    发明授权
    Synthesis of enone intermediate 有权
    烯酮中间体的合成

    公开(公告)号：US08293920B2

    公开(公告)日：2012-10-23

    申请号：US13043742

    申请日：2011-03-09

    申请人： Andrew G. Myers ,  Jason D. Brubaker

    发明人： Andrew G. Myers ,  Jason D. Brubaker

    IPC分类号： C07D261/12 ,  C07D413/06

    CPC分类号： C07D231/20 ,  C07C237/26 ,  C07D261/12 ,  C07D261/20 ,  C07D413/06 ,  C07D498/18 ,  C07F7/1804 ,  C07F7/1892

    摘要： The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides a more efficient route for preparing the enone intermediate.

    摘要翻译： 四环素类抗生素在过去50年的传染病治疗中发挥了重要作用。 然而，四环素在人类和兽医药物中的使用量的增加已经导致了以前易受四环素抗生素影响的许多生物体之间的抵抗。 通过手性烯酮中间体最近开发的四环素类似物的模块合成使得能够高效合成以前从未制备的新型四环素类似物。 本发明提供了制备烯酮中间体的更有效的途径。

    SYNTHESIS OF ENONE INTERMEDIATE
    8.
    发明申请
    SYNTHESIS OF ENONE INTERMEDIATE 有权
    合成中间体

    公开(公告)号：US20120029199A1

    公开(公告)日：2012-02-02

    申请号：US13043742

    申请日：2011-03-09

    申请人： Andrew G. Myers ,  Jason D. Brubaker

    发明人： Andrew G. Myers ,  Jason D. Brubaker

    IPC分类号： C07D413/06 ,  C07D261/12

    CPC分类号： C07D231/20 ,  C07C237/26 ,  C07D261/12 ,  C07D261/20 ,  C07D413/06 ,  C07D498/18 ,  C07F7/1804 ,  C07F7/1892

    摘要： The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides a more efficient route for preparing the enone intermediate.

    摘要翻译： 四环素类抗生素在过去50年的传染病治疗中发挥了重要作用。 然而，四环素在人类和兽医药物中的使用量的增加已经导致了以前易受四环素抗生素影响的许多生物体之间的抵抗。 通过手性烯酮中间体最近开发的四环素类似物的模块合成使得能够高效合成以前从未制备的新型四环素类似物。 本发明提供了制备烯酮中间体的更有效的途径。

    Synthesis of enone intermediate
    9.
    发明授权
    Synthesis of enone intermediate 有权
    烯酮中间体的合成

    公开(公告)号：US08580969B2

    公开(公告)日：2013-11-12

    申请号：US13616667

    申请日：2012-09-14

    申请人： Andrew G. Myers ,  Jason D. Brubaker

    发明人： Andrew G. Myers ,  Jason D. Brubaker

    IPC分类号： C07D261/12 ,  C07C233/57

    CPC分类号： C07D231/20 ,  C07C237/26 ,  C07D261/12 ,  C07D261/20 ,  C07D413/06 ,  C07D498/18 ,  C07F7/1804 ,  C07F7/1892

    摘要： The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides a more efficient route for preparing the enone intermediate.

    摘要翻译： 四环素类抗生素在过去50年的传染病治疗中发挥了重要作用。 然而，四环素在人类和兽医药物中的使用量的增加已经导致了以前易受四环素抗生素影响的许多生物体之间的抵抗。 通过手性烯酮中间体最近开发的四环素类似物的模块合成使得能够高效合成以前从未制备的新型四环素类似物。 本发明提供了制备烯酮中间体的更有效的途径。

    Synthesis of enone intermediate
    10.
    发明授权
    Synthesis of enone intermediate 有权
    烯酮中间体的合成

    公开(公告)号：US07960559B2

    公开(公告)日：2011-06-14

    申请号：US12833628

    申请日：2010-07-09

    申请人： Andrew G. Myers ,  Jason D. Brubaker

    发明人： Andrew G. Myers ,  Jason D. Brubaker

    IPC分类号： C07D261/20

    CPC分类号： C07D231/20 ,  C07C237/26 ,  C07D261/12 ,  C07D261/20 ,  C07D413/06 ,  C07D498/18 ,  C07F7/1804 ,  C07F7/1892

    摘要： The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides a more efficient route for preparing the enone intermediate.

    摘要翻译： 四环素类抗生素在过去50年的传染病治疗中发挥了重要作用。 然而，四环素在人类和兽医药物中的使用量的增加已经导致了以前易受四环素抗生素影响的许多生物体之间的抵抗。 通过手性烯酮中间体最近开发的四环素类似物的模块合成使得能够高效合成以前从未制备的新型四环素类似物。 本发明提供了制备烯酮中间体的更有效的途径。