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    7-DISUBSTITUTED-PHENYL TETRACYCLINE DERIVATIVES
    4.
    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

    Applicant: Paratek Pharmaceuticals, Inc.

    Inventor： Todd Bowser ,  Paul Abato

    IPC: C07C237/34

    CPC classification number: C07C237/34 ,  C07C2603/46

    Abstract: 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.

    Abstract translation: 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。

    Epoxycarboxamide compound, azide compound, and amino alcohol compound, and process for preparing alpha-keto amide compound using them
    10.
    发明申请
    Epoxycarboxamide compound, azide compound, and amino alcohol compound, and process for preparing alpha-keto amide compound using them 失效
    环氧甲酰胺化合物，叠氮化合物和氨基醇化合物，以及使用它们制备α-酮酰胺化合物的方法

    公开(公告)号：US20030153788A1

    公开(公告)日：2003-08-14

    申请号：US10331702

    申请日：2002-12-30

    Applicant: Seikagaku Corporation

    Inventor： Nobuo Kobayashi ,  Tsuneo Koji ,  Takashi Fujita ,  Tomofumi Nishimura ,  Akihiko Hosoda

    IPC: C07C237/34 ,  C07C237/04 ,  C07C247/04 ,  C07C247/06 ,  C07D303/36

    CPC classification number: C07D295/215 ,  C07C231/12 ,  C07C231/16 ,  C07C237/22 ,  C07C247/12 ,  C07C271/22 ,  C07C2601/14 ,  C07D207/16 ,  C07D295/18 ,  C07D303/46 ,  C07D303/48 ,  C07D317/66 ,  C07D405/12 ,  C07D407/12 ,  C07D413/12

    Abstract: The present invention is to provide manufacturing intermediates which can be led to useful null-ketoamide compounds having protease-inhibiting activity extremely economically and stereoselectively, and to provide epoxycarboxamide compounds, azide compounds and amino alcohol compounds represented by the following formulae: 1 wherein R1 and R2 each represents alkyl group, alkenyl group, aromatic hydrocarbon group or heterocyclic group; R3 represents alkyl group, alkenyl group, aromatic hydrocarbon group, heterocyclic group, R6nullOnull or R7nullN(R8)null; where R6 represents alkyl group, alkenyl group, aromatic hydrocarbon group or heterocyclic group; R7 and R8 each represents hydrogen atom, alkyl group, alkenyl group, aromatic hydrocarbon group or heterocyclic group, and, R4 and R5 represent the same groups as R7 and R8, respectively, and R4 and R5 optionally form a ring together; and X represents nullOnull or nullN(R9)null, where R9 represents hydrogen atom or alkyl group, and X optionally forms a ring together with R4 or R5, and processes for preparing null-keto amide compound using the same.

    Abstract translation: 本发明提供制造中间体，其可以经济地和立体选择性地被引入具有蛋白酶抑制活性的有用的α-酮酰胺化合物，并提供由下式表示的环氧羧酰胺化合物，叠氮化合物和氨基醇化合物：其中R1和R2 各自表示烷基，烯基，芳族烃基或杂环基; R3代表烷基，烯基，芳族烃基，杂环基，R6-O-或R7-N（R8） - ; 其中R 6表示烷基，烯基，芳族烃基或杂环基; R 7和R 8各自表示氢原子，烷基，烯基，芳族烃基或杂环基，R 4和R 5分别表示与R 7和R 8相同的基团，R 4和R 5任选地形成环; 并且X表示-O-或-N（R 9） - ，其中R 9表示氢原子或烷基，X任选地与R 4或R 5一起形成环，以及使用其制备α-酮酰胺化合物的方法。

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