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    Tigecycline crystalline hydrate and preparation method therefor and use thereof
    5.
    发明授权
    Tigecycline crystalline hydrate and preparation method therefor and use thereof 有权
    替加环素结晶水合物及其制备方法及用途

    公开(公告)号：US09475759B2

    公开(公告)日：2016-10-25

    申请号：US14112876

    申请日：2012-04-20

    申请人： Lifang Hu

    发明人： Lifang Hu

    IPC分类号： C07C237/26 ,  A61K31/65 ,  C07C231/14

    CPC分类号： C07C237/26 ,  A61K31/65 ,  C07B2200/13 ,  C07C231/14 ,  C07C2603/46

    摘要： Provided are a Tigecycline crystalline hydrate, and a preparation method therefor and use thereof. The crystalline hydrate has high stability for storage, and is used for the manufacture of a medicament for treating or preventing the infection of respiratory system, hepatobiliary system, facial features, urogenital system, bone and joint, skin and soft tissue and endocarditis, septicemia, meningitis caused by susceptible strains of Gram-positive or Gram-negative bacteria, anaerobic bacteria, chlamydia, and mycoplasma in human or animal.

    摘要翻译： 提供替加环素结晶水合物及其制备方法及其用途。 结晶水合物具有较高的储存稳定性，用于制备治疗或预防呼吸系统，肝胆系统，面部特征，泌尿生殖系统，骨骼和关节，皮肤和软组织以及心内膜​​炎，败血病， 革兰氏阳性或革兰氏阴性菌，厌氧菌，衣原体和支原体易感菌株引起的脑膜炎。

    Process for isolating tigecycline and tigecycline made therefrom
    8.
    发明授权
    Process for isolating tigecycline and tigecycline made therefrom 有权
    用于分离替加环素和替加环素制备的方法

    公开(公告)号：US09187410B2

    公开(公告)日：2015-11-17

    申请号：US13145445

    申请日：2010-01-22

    申请人： Zita Mendes ,  Guy Villax

    发明人： Zita Mendes ,  Guy Villax

    IPC分类号： A61K31/65 ,  A61P31/00 ,  B29B9/16 ,  C07C231/24 ,  C07C237/26

    CPC分类号： C07C231/24 ,  A61K31/65 ,  C07C237/26 ,  C07C2603/46

    摘要： The present invention provides a process for isolating tigecycline which process comprises the step of spray drying a solution of tigecycline in a solvent. Preferably the solvent is water or an organic solvent. In another aspect, there is provided tigecycline obtainable by spray drying, particularly in amorphous form. In particular, the invention provides tigecycline obtainable by spray drying according to the process of the invention.

    摘要翻译： 本发明提供了一种隔离替加环素的方法，该方法包括将替加环素溶液喷雾干燥在溶剂中的步骤。 溶剂优选为水或有机溶剂。 另一方面，提供了通过喷雾干燥，特别是无定形形式获得的替加环素。 特别地，本发明提供根据本发明的方法通过喷雾干燥获得的替加环素。

    7-DISUBSTITUTED-PHENYL TETRACYCLINE DERIVATIVES
    9.
    发明申请
    7-DISUBSTITUTED-PHENYL TETRACYCLINE DERIVATIVES 审中-公开
    7-取代的苯基四环素衍生物

    公开(公告)号：US20150166470A1

    公开(公告)日：2015-06-18

    申请号：US14403616

    申请日：2013-05-30

    申请人： Paratek Pharmaceuticals, Inc.

    发明人： Todd Bowser ,  Paul Abato

    IPC分类号： C07C237/34

    CPC分类号： C07C237/34 ,  C07C2603/46

    摘要： 7-Disubstituted-phenyl tetracycline compounds are disclosed herein. Also disclosed is a method for treatment or prevention of spinal muscular atrophy using the 7-disubstituted-phenyl tetracycline compounds. This invention also relates to a method for treating or preventing a subject having spinal muscular atrophy. The method includes administering to the subject an effective amount of a tetracycline compound of formula (1), such that the spinal muscular atrophy is treated or prevented. Advantageously, the tetracycline compounds used in this method of the invention have one or more of the following characteristics: 1) potency in modulating mRNA splicing, 2) potency in modulating SMN protein levels, 3) central nervous system (CNS) and/pr brain penetration, 4) decreased phototoxic properties and 5) decreased antibacterial properties.

    摘要翻译： 7-二取代 - 苯基四环素化合物在本文中公开。 还公开了使用7-二取代 - 苯基四环素化合物治疗或预防脊髓性肌肉萎缩的方法。 本发明还涉及治疗或预防具有脊髓性肌肉萎缩的受试者的方法。 该方法包括向受试者施用有效量的式（1）的四环素化合物，使得治疗或预防脊髓性肌萎缩。 有利地，本发明方法中使用的四环素化合物具有一个或多个以下特征：1）调节mRNA剪接的效力，2）调节SMN蛋白水平的效力，3）中枢神经系统（CNS）和/ 渗透，4）光毒性降低，5）降低抗菌性能。