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    PRODRUGS OF FUMARATES AND THEIR USE IN TREATING VARIOUS DISEASES
    7.
    发明申请
    PRODRUGS OF FUMARATES AND THEIR USE IN TREATING VARIOUS DISEASES 有权
    FUMARATES的原料及其在治疗各种疾病中的应用

    公开(公告)号：US20140275205A1

    公开(公告)日：2014-09-18

    申请号：US14180687

    申请日：2014-02-14

    申请人： ALKERMES PHARMA IRELAND LIMITED

    发明人： Tarek A. Zeidan ,  Scott Duncan ,  Christopher P. Hencken ,  Thomas Andrew Wynn ,  Carlos N. Sanrame

    IPC分类号： C07D207/12

    CPC分类号： C07D491/113 ,  A61K31/4015 ,  C07C229/12 ,  C07C229/18 ,  C07C317/18 ,  C07C317/28 ,  C07D207/12 ,  C07D207/40 ,  C07D207/408 ,  C07D211/92 ,  C07D295/088

    摘要： The present invention provides compounds of formula (I), wherein: R1 is unsubstituted C1-C6 alkyl; La is substituted or unsubstituted C1-C6 alkyl linker, substituted or unsubstituted C3-C10 carbocycle, substituted or unsubstituted heterocycle comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S, or substituted or unsubstituted heteroaryl comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S; and R2 and R3 are each, independently, H, substituted or unsubstituted C1-C6 alkyl, or substituted or unsubstituted C6-C10 aryl; or alternatively, R2 and R3, together with the nitrogen atom to which they are attached, form a substituted or unsubstituted heteroaryl comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S or a substituted or unsubstituted heterocycle comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S. The invention also provides pharmaceutical compositions and methods for treating neurological diseases, such as multiple sclerosis.

    摘要翻译： 本发明提供式（I）化合物，其中：R 1为未取代的C 1 -C 6烷基; La是取代或未取代的C 1 -C 6烷基接头，取代或未取代的C 3 -C 10碳环，含有一个或两个5-或6-元环和1-4个选自N，O和S的杂原子的取代或未取代的杂环， 包含一个或两个5-或6-元环和1-4个选自N，O和S的杂原子的未取代杂芳基; 且R 2和R 3各自独立地为H，取代或未取代的C 1 -C 6烷基或取代或未取代的C 6 -C 10芳基; 或者可选地，R 2和R 3与它们所连接的氮原子一起形成取代或未取代的杂芳基，其包括一个或两个5-或6-元环和1-4个选自N，O和S的杂原子或取代的 或未取代的杂环，其包含一个或两个5-或6-元环和1-4个选自N，O和S的杂原子。本发明还提供用于治疗神经疾病如多发性硬化的药物组合物和方法。