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    Compositions and methods for treating amyloidosis
    1.
    发明申请
    Compositions and methods for treating amyloidosis 审中-公开
    治疗淀粉样变性的组合物和方法

    公开(公告)号：US20110281951A1

    公开(公告)日：2011-11-17

    申请号：US13066451

    申请日：2011-04-14

    申请人： Walter Szarek ,  Donald Weaver ,  Xianqi Kong ,  Heather Gordon

    发明人： Walter Szarek ,  Donald Weaver ,  Xianqi Kong ,  Heather Gordon

    IPC分类号： A61K31/185 ,  A61P3/10 ,  A61P25/00 ,  A61P25/28

    CPC分类号： A61K31/404 ,  A61K31/00 ,  A61K31/185 ,  A61K31/192 ,  A61K31/194 ,  A61K31/198 ,  A61K31/205 ,  A61K31/4015 ,  A61K31/403 ,  A61K31/4035 ,  A61K31/4152 ,  A61K31/428 ,  A61K31/437 ,  A61K31/44 ,  A61K31/4409 ,  A61K31/4418 ,  A61K31/4439 ,  A61K31/445 ,  A61K31/4453 ,  A61K31/465 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/472 ,  A61K31/4725 ,  A61K31/473 ,  A61K31/4741 ,  A61K31/675 ,  A61K31/706

    摘要： Therapeutic compounds and methods for modulating amyloid aggregation in a subject, whatever its clinical setting, are described. Amyloid aggregation is modulated by the administration to a subject of an effective amount of a therapeutic compound of the formula or a pharmaceutically acceptable salt or ester, such that modulation of amyloid aggregation occurs. R1 and R2 are each independently a hydrogen atom or a substituted or unsubstituted aliphatic or aryl group. Z and Q are each independently a carbonyl (C═O), thiocarbonyl (C═S), sulfonyl (SO2), or sulfoxide (S═O) group. “k” and “m” are 0 or 1, provided when k is 1, R1 is not a hydrogen atom, and when m is 1, R2 is not a hydrogen atom. In an embodiment, at least one of k or m must equal 1. “p” and “s” are each independently positive integers selected such that the biodistribution of the therapeutic compound for an intended target site is not prevented while maintaining activity of the therapeutic compound. T is a linking group and Y is a group of the formula -A X wherein A is an anionic group at physiological pH, and X is a cationic group.

    摘要翻译： 描述了治疗化合物和调节受试者淀粉样蛋白聚集的方法，无论其临床情况如何。 淀粉样蛋白聚集通过施用有效量的下式的治疗化合物或药学上可接受的盐或酯来调节，使得发生淀粉样蛋白聚集的调节。 R 1和R 2各自独立地为氢原子或取代或未取代的脂族基或芳基。 Z和Q各自独立地为羰基（C = O），硫代羰基（C = S），磺酰基（SO 2）或亚砜（S = O）。 当k为1时，“k”和“m”为0或1，R1不是氢原子，当m为1时，R2不为氢原子。 在一个实施方案中，k或m中的至少一个必须等​​于1.“p”和“s”各自独立地为正整数，使得治疗化合物对于预期靶位点的生物分布不被预防，同时维持治疗 复合。 T是连接基团，Y是式-AX的基团，其中A是生理pH下的阴离子基团，X是阳离子基团。

    Compositions and methods for treating amyloidosis
    2.
    发明申请
    Compositions and methods for treating amyloidosis 审中-公开
    治疗淀粉样变性的组合物和方法

    公开(公告)号：US20090099100A1

    公开(公告)日：2009-04-16

    申请号：US12217580

    申请日：2008-07-07

    申请人： Walter Szarek ,  Donald Weaver ,  Xianqi Kong ,  Heather Gordon

    发明人： Walter Szarek ,  Donald Weaver ,  Xianqi Kong ,  Heather Gordon

    IPC分类号： A61K31/185 ,  A61K31/7008 ,  A61P3/00

    CPC分类号： A61K31/404 ,  A61K31/00 ,  A61K31/185 ,  A61K31/192 ,  A61K31/194 ,  A61K31/198 ,  A61K31/205 ,  A61K31/4015 ,  A61K31/403 ,  A61K31/4035 ,  A61K31/4152 ,  A61K31/428 ,  A61K31/437 ,  A61K31/44 ,  A61K31/4409 ,  A61K31/4418 ,  A61K31/4439 ,  A61K31/445 ,  A61K31/4453 ,  A61K31/465 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/472 ,  A61K31/4725 ,  A61K31/473 ,  A61K31/4741 ,  A61K31/675 ,  A61K31/706

    摘要： Therapeutic compounds and methods for modulating amyloid aggregation in a subject, whatever its clinical setting, are described. Amyloid aggregation is modulated by the administration to a subject of an effective amount of a therapeutic compound of the formula or a pharmaceutically acceptable salt or ester, such that modulation of amyloid aggregation occurs. R1 and R2 are each independently a hydrogen atom or a substituted or unsubstituted aliphatic or aryl group. Z and Q are each independently a carbonyl (C═O), thiocarbonyl (C═S), sulfonyl (SO2), or sulfoxide (S═O) group. “k” and “m” are 0 or 1, provided when k is 1, R1 is not a hydrogen atom, and when m is 1, R2 is not a hydrogen atom. In an embodiment, at least one of k or m must equal 1. “p” and “s” are each independently positive integers selected such that the biodistribution of the therapeutic compound for an intended target site is not prevented while maintaining activity of the therapeutic compound. T is a linking group and Y is a group of the formula -A X wherein A is an anionic group at physiological pH, and X is a cationic group.

    摘要翻译： 描述了治疗化合物和调节受试者淀粉样蛋白聚集的方法，无论其临床情况如何。 淀粉样蛋白聚集通过施用有效量的下式的治疗化合物或药学上可接受的盐或酯来调节，使得发生淀粉样蛋白聚集的调节。 R 1和R 2各自独立地为氢原子或取代或未取代的脂族基或芳基。 Z和Q各自独立地为羰基（C-O），硫代羰基（C-S），磺酰基（SO2）或亚砜（S-O）基团。 当k为1时，“k”和“m”为0或1，R1不是氢原子，当m为1时，R2不为氢原子。 在一个实施方案中，k或m中的至少一个必须等​​于1.“p”和“s”各自独立地为正整数，使得治疗化合物对于预期靶位点的生物分布不被预防，同时维持治疗 复合。 T是连接基团，Y是式-AX的基团，其中A是生理pH下的阴离子基团，X是阳离子基团。

    Phosphono-carboxylate compounds for treating amyloidosis
    4.
    发明申请
    Phosphono-carboxylate compounds for treating amyloidosis 审中-公开
    用于治疗淀粉样变性的膦酰羧酸盐化合物

    公开(公告)号：US20080004244A1

    公开(公告)日：2008-01-03

    申请号：US11888989

    申请日：2007-08-02

    申请人： Walter Szarek ,  Xianqi Kong ,  Gregory Thatcher ,  Boris Gorine

    发明人： Walter Szarek ,  Xianqi Kong ,  Gregory Thatcher ,  Boris Gorine

    IPC分类号： A61K31/662 ,  A61P25/00

    CPC分类号： A61K31/662 ,  A61K31/66 ,  A61K31/675

    摘要： Therapeutic compounds and methods for modulating amyloid deposition in a subject, whatever its clinical setting, are described. Amyloid deposition is modulated by the administration to a subject of an effective amount of a therapeutic compound comprising a phosphonate group and a carboxylate group, a congener thereof, or a pharmaceutically acceptable salt or ester thereof. In preferred embodiments, an interaction between an amyloidogenic protein and a basement membrane constituent is modulated.

    摘要翻译： 描述了治疗化合物和调节受试者淀粉样蛋白沉积的方法，无论其临床情况如何。 通过施用有效量的包含膦酸酯基和羧酸酯基的治疗化合物，其同类物或其药学上可接受的盐或酯来调节淀粉样蛋白沉积。 在优选的实施方案中，调节淀粉样蛋白形成蛋白质与基底膜成分之间的相互作用。

    Pharmaceutical drug candidates and methods for preparation thereof
    9.
    发明授权
    Pharmaceutical drug candidates and methods for preparation thereof 有权
    药物候选药物及其制备方法

    公开(公告)号：US07253306B2

    公开(公告)日：2007-08-07

    申请号：US10871543

    申请日：2004-06-18

    申请人： Xianqi Kong ,  David Migneault ,  Xinfu Wu

    发明人： Xianqi Kong ,  David Migneault ,  Xinfu Wu

    IPC分类号： C07C309/00

    CPC分类号： A61K31/185

    摘要： The present invention is directed to methods of preparation of sulfonate derivatized compounds, e.g., 3-amino-1-propanesulfonic acid and 1,3-propanedisulfonic acid disodium salt with increased purity, with reduced potential for toxic by-products, and that are pharmaceutically useful, e.g., for the treatment of amyloidosis.

    摘要翻译： 本发明涉及制备磺酸衍生化合物的方法，例如3-氨基-1-丙磺酸和1,3-丙烷二磺酸二钠盐，其纯度提高，有毒副产物的潜力降低，且为药学上 有用的，例如用于治疗淀粉样变性。