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    Hydrazide-containing CFTR inhibitor compounds and uses thereof
    1.
    发明授权
    Hydrazide-containing CFTR inhibitor compounds and uses thereof 有权
    含酰肼的CFTR抑制剂化合物及其用途

    公开(公告)号：US07888332B2

    公开(公告)日：2011-02-15

    申请号：US12175982

    申请日：2008-07-18

    申请人： Alan S. Verkman ,  Nitin D. Sonawane ,  Chatchai Muanprasat

    发明人： Alan S. Verkman ,  Nitin D. Sonawane ,  Chatchai Muanprasat

    IPC分类号： A01N43/04 ,  A61K31/715

    CPC分类号： A61K31/165 ,  A01K67/027 ,  A01K2227/105 ,  A01K2267/0306 ,  A61K31/195 ,  A61K31/47 ,  A61K31/7012 ,  C07D215/38 ,  Y02A50/471

    摘要： The invention provides compositions, pharmaceutical preparations and methods for inhibition of cystic fibrosis transmembrane conductance regulator protein (CFTR) that are useful for the study and treatment of CFTR-mediated diseases and conditions. The compositions and pharmaceutical preparations of the invention may comprise one or more hydrazide-containing compounds, and may additionally comprise one or more pharmaceutically acceptable carriers, excipients and/or adjuvants. The methods of the invention comprise, in certain embodiments, administering to a patient suffering from a CFTR-mediated disease or condition, an efficacious amount of a hydrazide-containing compound. In other embodiments the invention provides methods of inhibiting CFTR that comprise contacting cells in a subject with an effective amount of a hydrazide-containing compound. In addition, the invention features a non-human animal model of CFTR-mediated disease which model is produced by administration of a hydrazide-containing compound to a non-human animal in an amount sufficient to inhibit CFTR.

    摘要翻译： 本发明提供用于抑制囊性纤维化跨膜传导调节蛋白（CFTR）的组合物，药物制剂和方法，其可用于研究和治疗CFTR介导的疾病和病症。 本发明的组合物和药物制剂可以包含一种或多种含酰肼的化合物，并且还可以包含一种或多种药学上可接受的载体，赋形剂和/或佐剂。 在某些实施方案中，本发明的方法包括给予患有CFTR介导的疾病或病症的患者，有效量的含酰肼的化合物。 在其它实施方案中，本发明提供了抑制CFTR的方法，其包括使受试者中的细胞与有效量的含酰肼化合物接触。 此外，本发明的特征在于CFTR介导的疾病的非人动物模型，其通过以足以抑制CFTR的量向非人动物施用含酰肼的化合物来产生该模型。

    DIVALENT HYDRAZIDE COMPOUND CONJUGATES FOR INHIBITING CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR
    3.
    发明申请
    DIVALENT HYDRAZIDE COMPOUND CONJUGATES FOR INHIBITING CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR 审中-公开
    用于抑制CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR的二氯化氢复合物

    公开(公告)号：US20090253799A1

    公开(公告)日：2009-10-08

    申请号：US12418147

    申请日：2009-04-03

    申请人： Alan S. Verkman ,  Nitin D. Sonawane

    发明人： Alan S. Verkman ,  Nitin D. Sonawane

    IPC分类号： A61K31/17 ,  C07C335/00

    CPC分类号： C07C337/06 ,  C07C335/16

    摘要： Provided herein are divalent hydrazide-polyethylene glycol conjugates that inhibit the ion transport activity of a cystic fibrosis transmembrane conductance regulator (CFTR). The conjugates described herein are useful for treating diseases, disorders, and sequelae of diseases, disorders, and conditions that are associated with aberrantly increased CFTR activity, for example, secretory diarrhea.

    摘要翻译： 本文提供抑制囊性纤维化跨膜传导调节剂（CFTR）的离子迁移活性的二价酰肼 - 聚乙二醇缀合物。 本文描述的缀合物可用于治疗与异常增加的CFTR活性（例如分泌性腹泻）相关的疾病，病症和病症的疾病，病症和后遗症。

    WATER SOLUBLE SMALL MOLECULE INHIBITORS OF THE CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR
    4.
    发明申请
    WATER SOLUBLE SMALL MOLECULE INHIBITORS OF THE CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR 审中-公开
    CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR的水溶性小分子抑制剂

    公开(公告)号：US20110105565A1

    公开(公告)日：2011-05-05

    申请号：US12934621

    申请日：2009-03-25

    申请人： Alan S. Verkman ,  Nitin D. Sonawane

    发明人： Alan S. Verkman ,  Nitin D. Sonawane

    IPC分类号： A61K31/4439 ,  C07D277/08 ,  C07D417/06 ,  C07D207/456 ,  A61K31/427 ,  A61K31/426 ,  A61P13/12

    CPC分类号： C07D277/36 ,  C07D417/06 ,  C07D417/10

    摘要： Provided herein are highly water soluble, thiazolidinone derivative compounds and glycine hydrazide derivative compounds that inhibit the ion transport activity of the cystic fibrosis transmembrane conductance regulator (CFTR). The compounds, and compositions comprising the compounds, described herein are useful for treating diseases, disorders, and sequelae of diseases, disorders, and conditions that are associated with aberrantly increased CFTR activity, for example, secretory diarrhea. The compounds may also be used for inhibiting expansion or preventing formation of cysts in persons who have polycystic kidney disease.

    摘要翻译： 本文提供了高度水溶性的，阻止囊性纤维化跨膜传导调节剂（CFTR）的离子迁移活性的噻唑烷酮衍生物化合物和甘氨酰肼衍生物化合物。 包含本文所述的化合物的化合物和组合物可用于治疗与异常增加的CFTR活性（例如分泌性腹泻）相关的疾病，病症和病症的疾病，障碍和后遗症。 这些化合物也可用于抑制扩张或阻止患有多囊肾病的人的囊肿形成。

    Methods for identifying inhibitors of solute transporters
    7.
    发明授权
    Methods for identifying inhibitors of solute transporters 有权
    鉴定溶质转运蛋白抑制剂的方法

    公开(公告)号：US09316633B2

    公开(公告)日：2016-04-19

    申请号：US12514992

    申请日：2007-11-16

    申请人： Alan S. Verkman ,  Marc Harris Levin

    发明人： Alan S. Verkman ,  Marc Harris Levin

    IPC分类号： G01N33/50 ,  G01N33/62 ,  G01N33/68 ,  G01N33/80

    CPC分类号： G01N33/5026 ,  G01N33/62 ,  G01N33/6872 ,  G01N33/80 ,  G01N2500/10

    摘要： Provided herein are methods for identifying and characterizing agents that alter the volume of a cell. Methods are provided for rapid screening and identification of an agent that alters the capability of a small, neutrally charged solute transporter to transport the solute across a cell membrane. The methods described herein may be used to identify and characterize inhibitors of urea transporters, to identify and characterize inhibitors of aquaporins, and to identify and characterize inhibitors of other small, neutrally charged solutes such as glucose.

    摘要翻译： 本文提供了用于鉴定和表征改变细胞体积的试剂的方法。 提供了用于快速筛选和鉴定改变小的中性带电溶质转运蛋白将细胞穿过细胞膜输送溶质的能力的方法。 本文描述的方法可用于鉴定和表征尿素转运蛋白的抑制剂，以鉴定和表征水通道蛋白的抑制剂，以及鉴定和表征其它小的，中性电荷的溶质如葡萄糖的抑制剂。

    PYRIMIDO-PYRROLO-QUINOXALINEDIONE INHIBITORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR PROTEIN AND USES THEREFOR
    8.
    发明申请
    PYRIMIDO-PYRROLO-QUINOXALINEDIONE INHIBITORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR PROTEIN AND USES THEREFOR 有权
    环糊精转铁蛋白导管调节蛋白的吡哆醇 - 吡喃半乳糖苷酶抑制剂及其用途

    公开(公告)号：US20120208822A1

    公开(公告)日：2012-08-16

    申请号：US13389898

    申请日：2010-08-10

    申请人： Alan S. Verkman ,  Lukmanee Tradtrantip

    发明人： Alan S. Verkman ,  Lukmanee Tradtrantip

    IPC分类号： A61K31/519 ,  A61P1/00 ,  A61P1/12 ,  A61P13/12

    CPC分类号： A61K31/407 ,  A61K31/495 ,  C07D487/14

    摘要： Provided herein are pyrimido-pyrrolo-quinoxalinedione (PPQ) compounds, and compositions comprising these compounds, that inhibit cystic fibrosis transmembrane conductance regulator (CFTR) mediated ion transport and that are useful for treating diseases and disorders associated with aberrantly increased CFTR chloride channel activity. The compounds, and compositions comprising the compounds, described herein are useful for treating diseases, disorders, and sequelae of diseases, disorders, and conditions that are associated with aberrantly increased CFTR activity, for example, polycystic kidney disease. The compounds may be used for inhibiting expansion or preventing formation of cysts in persons who have polycystic kidney disease.

    摘要翻译： 本文提供嘧啶 - 吡咯并喹喔啉酮（PPQ）化合物和包含这些化合物的组合物，其抑制囊性纤维化跨膜传导调节物（CFTR）介导的离子转运并且可用于治疗与异常增加的CFTR氯离子通道活性相关的疾病和病症。 包含本文所述的化合物的化合物和组合物可用于治疗与异常增加的CFTR活性例如多囊肾病相关的疾病，病症和病症的疾病，病症和病症的后遗症。 该化合物可用于抑制扩张或阻止患有多囊肾病的人的囊肿形成。