RU2013152132A - Борсодержащие малые молекулы в качестве противовоспалительных средств - Google Patents

Борсодержащие малые молекулы в качестве противовоспалительных средств Download PDF

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RU2013152132A
RU2013152132A RU2013152132/15A RU2013152132A RU2013152132A RU 2013152132 A RU2013152132 A RU 2013152132A RU 2013152132/15 A RU2013152132/15 A RU 2013152132/15A RU 2013152132 A RU2013152132 A RU 2013152132A RU 2013152132 A RU2013152132 A RU 2013152132A
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RU2642628C2 (ru
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Стефен Дж. БЕЙКЕР
Вирджиния САНДЕРЗ
Цутому АКАМА
Кэролин БЕЛЛИНГЕР-КАВАХАРА
Ивонне ФРОЙНД
Керк Р. МЕЙПЛЗ
Джейкоб Дж. Платтнер
Юн-Кан ЧЖАН
Хучэнь ЧЖОУ
Винсент С. Эрнандес
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Анакор Фармасьютикалз, Инк.
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Abstract

Способ лечения или профилактики у человека или животного заболевания, связанного с воспалением, при этом указанный способ включает введение человеку или животному терапевтически эффективного количества соединения, имеющего структуру, соответствующую формуле I:,где B представляет собой бор;Rявляется представителем, выбранным из группы, включающей отрицательный заряд, противоион соли, H, циано, замещенный или незамещенный алкил, замещенный или незамещенный гетероалкил, замещенный или незамещенный циклоалкил, замещенный или незамещенный гетероциклоалкил, замещенный или незамещенный арил и замещенный или незамещенный гетероарил;M является представителем, выбранным из кислорода, серы и NR;Rявляется представителем, выбранным из группы, включающей H, замещенный или незамещенный алкил, замещенный или незамещенный гетероалкил, замещенный или незамещенный циклоалкил, замещенный или незамещенный гетероциклоалкил, замещенный или незамещенный арил и замещенный или незамещенный гетероарил;J является представителем, выбранным из (CRR)и CR;R, Rи Rявляются представителями, независимо выбранными из группы, включающей H, циано, замещенный или незамещенный алкил, замещенный или незамещенный гетероалкил, замещенный или незамещенный циклоалкил, замещенный или незамещенный гетероциклоалкил, замещенный или незамещенный арил и замещенный или незамещенный гетероарил;n1 означает целое число, выбранное из 0-2;W является представителем, выбранным из C=O (карбонил), (CRR)и CR;R, Rи Rявляются представителями, независимо выбранными из группы, включающей H, циано, замещенный или незамещенный алкил, замещенный или незамещенный гетероалкил, замещ

Claims (1)

  1. Способ лечения или профилактики у человека или животного заболевания, связанного с воспалением, при этом указанный способ включает введение человеку или животному терапевтически эффективного количества соединения, имеющего структуру, соответствующую формуле I:
    Figure 00000001
    ,
    где B представляет собой бор;
    R1a является представителем, выбранным из группы, включающей отрицательный заряд, противоион соли, H, циано, замещенный или незамещенный алкил, замещенный или незамещенный гетероалкил, замещенный или незамещенный циклоалкил, замещенный или незамещенный гетероциклоалкил, замещенный или незамещенный арил и замещенный или незамещенный гетероарил;
    M является представителем, выбранным из кислорода, серы и NR2a;
    R2a является представителем, выбранным из группы, включающей H, замещенный или незамещенный алкил, замещенный или незамещенный гетероалкил, замещенный или незамещенный циклоалкил, замещенный или незамещенный гетероциклоалкил, замещенный или незамещенный арил и замещенный или незамещенный гетероарил;
    J является представителем, выбранным из (CR3aR4a)n1 и CR5a;
    R3a, R4a и R5a являются представителями, независимо выбранными из группы, включающей H, циано, замещенный или незамещенный алкил, замещенный или незамещенный гетероалкил, замещенный или незамещенный циклоалкил, замещенный или незамещенный гетероциклоалкил, замещенный или незамещенный арил и замещенный или незамещенный гетероарил;
    n1 означает целое число, выбранное из 0-2;
    W является представителем, выбранным из C=O (карбонил), (CR6aR7a)m1 и CR8a;
    R6a, R7a и R8a являются представителями, независимо выбранными из группы, включающей H, циано, замещенный или незамещенный алкил, замещенный или незамещенный гетероалкил, замещенный или незамещенный циклоалкил, замещенный или незамещенный гетероциклоалкил, замещенный или незамещенный арил и замещенный или незамещенный гетероарил;
    m1 означает целое число, выбранное из 0 и 1;
    A является представителем, выбранным из CR9a и N;
    D является представителем, выбранным из CR10a и N;
    E является представителем, выбранным из CR11a и N;
    G является представителем, выбранным из CR12a и N;
    R9a, R10a, R11a и R12a являются представителями, независимо выбранными из группы, включающей H, OR*, NR*R**, SR*, -S(O)2R*, -S(O)2NR*R**, -C(O)R*, -C(O)OR*, -C(О)NR*R**, нитро, галоген, циано, замещенный или незамещенный алкил, замещенный или незамещенный гетероалкил, замещенный или незамещенный циклоалкил, замещенный или незамещенный гетероциклоалкил, замещенный или незамещенный арил и замещенный или незамещенный гетероарил;
    где каждый R* и R** являются представителями, независимо выбранными из группы, включающей H, нитро, галоген, циано, замещенный или незамещенный алкил, замещенный или незамещенный гетероалкил, замещенный или незамещенный циклоалкил, замещенный или незамещенный гетероциклоалкил, замещенный или незамещенный арил и замещенный или незамещенный гетероарил;
    сочетание атомов азота (A + D + E + G) означает целое число, выбранное из 0-3;
    представитель, выбранный из R3a, R4a и R5a, и представитель, выбранный из R6a, R7a и R8a, вместе с атомами, с которыми они связаны, необязательно объединяются с образованием 4-7-членного кольца;
    R3a и R4a вместе с атомами, с которыми они связаны, необязательно объединяются с образованием 4-7-членного кольца;
    R6a и R7a вместе с атомами, с которыми они связаны, необязательно объединяются с образованием 4-7-членного кольца;
    R9a и R10a вместе с атомами, с которыми они связаны, необязательно объединяются с образованием 4-7-членного кольца;
    R10a и R11a вместе с атомами, с которыми они связаны, необязательно объединяются с образованием 4-7-членного кольца;
    R11a и R12a вместе с атомами, с которыми они связаны, необязательно объединяются с образованием 4-7-членного кольца.
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