Compounds, Methods And Devices for Inhibiting Neoproliferative Changes in Blood Vessel Walls
    2.
    发明申请
    Compounds, Methods And Devices for Inhibiting Neoproliferative Changes in Blood Vessel Walls 有权
    用于抑制血管壁新生血管变化的化合物,方法和装置

    公开(公告)号:US20090048270A1

    公开(公告)日:2009-02-19

    申请号:US10533060

    申请日:2003-10-30

    CPC分类号: A61K31/415

    摘要: Methods, compositions and devices for inhibiting neoproliferative changes in blood vessel walls or other anatomical structures. One or more compounds of Formula I or I-A set forth herein are administered systemically and/or locally to human or veterinary patients to deter or prevent unwanted proliferative changes in blood vessels or other anatomical structures. The invention may be used to deter or prevent stenosis or restenosis of arteries following angioplasty and/or stent placement. In one embodiment, there is provided an implantable stent or stent graft from which one or more compounds of the present invention will elute or otherwise be delivered into an affected blood vessel wall.

    摘要翻译: 用于抑制血管壁或其他解剖结构中新生血管变化的方法,组合物和装置。 本文所述的一种或多种式I或I-A化合物全身和/或局部施用于人或兽医患者以阻止或预防血管或其他解剖结构中不期望的增殖性变化。 本发明可用于阻止或预防血管成形术和/或支架放置后的动脉狭窄或再狭窄。 在一个实施方案中,提供了可植入支架或支架移植物,其中一种或多种本发明化合物将从其中洗脱或以其它方式递送到受影响的血管壁。

    Non-peptide inhibition of T-lymphocyte activation and therapies related thereto

    公开(公告)号:US07235577B1

    公开(公告)日:2007-06-26

    申请号:US10402532

    申请日:2003-03-28

    IPC分类号: A61K31/415

    摘要: Compounds, preparations and methods for immunosuppressive treatment of autoimmune disorders, graft rejection and/or graft/host disease. Therapeutically effective amounts of certain substituted triarylmethane compounds, such as 1-[(2-chlorophenyl)diphenylmethyl]-1H-pyrazole, are administered to mammalian patients to selectively inhibit the calcium-activated K+ channel (IKCa1) in lymphocytes, monocytes, macrophages, platelets or endothelial cells without concomitant inhibition of P450-dependent enzyme systems, resulting in reduction of antigen-, cytokine-, or mitogen-induced calcium entry through store operated calcium channels in these cells, suppression of cytokine production by these cells, and inhibition of activation of these cells. Such inhibition of the Ca++ activated K+ channel (IKCa1) prevents the pre-Ca++ stage of cell activation and thus causes immunosuppression and an anti-inflammatory response.

    hKCa3/KCNN3 small conductance calcium activated potassium channel: a
diagnostic marker and therapeutic target
    7.
    发明授权
    hKCa3/KCNN3 small conductance calcium activated potassium channel: a diagnostic marker and therapeutic target 失效
    hKCa3 / KCNN3小电导钙激活钾通道:诊断标记和治疗靶点

    公开(公告)号:US6165719A

    公开(公告)日:2000-12-26

    申请号:US115446

    申请日:1998-07-14

    摘要: The present invention is based on the discovery and cloning of the human small conductance calcium activated potassium channel type 3 (hKCa3/KCNN3) gene, which is expressed in neuronal cells, skeletal muscle, heart, and lymphocytes. Alterations in the hKCa3/KCNN3 gene or its protein product may enhance susceptibility to schizophrenia and/or bipolar disorder. hKCa3/KCNN3 may be involved in neuropsychiatric, neurological, neuromuscular, and immunological disorders. Substantially purified hKCa3/KNN3 polypeptides and polynucleotides are provided. Antibodies which bind to hKCa3/KCNN3 polypeptides are also disclosed. A method for identifying a compound which affects hKCa3/KCNN3 polynucleotide or polypeptide is provided. A method for diagnosis and determining the prognosis and treatment regimen of a subject having or at risk of having a hKCa3/KCNN3-associated disorder is also provided. A method of treating a subject having or at risk of having an hKCa3/KCNN3-associated disorder by administering a therapeutically effective amount of a polynucleotide encoding SEQ ID NO:2 is also provided. A formulation for administration of hKCa3/KCNN3 to a patient of a therapeutically effective amount of hKCa3/KCNN3 polypeptide is provided. Kits useful for detecting the presence of hKCa3/KCNN3 polypeptide or polynucleotide in a sample from a subject having a hKCa3/KCNN3-associated disorder are provided. Transgenic nonhuman animals having a transgene encoding hKCa3/KCNN3 are also described.

    摘要翻译: 本发明是基于在神经细胞,骨骼肌,心脏和淋巴细胞中表达的人小电导钙激活钾通道3型(hKCa3 / KCNN3)基因的发现和克隆。 hKCa3 / KCNN3基因或其蛋白质产物的改变可能增加对精神分裂症和/或双相情感障碍的易感性。 hKCa3 / KCNN3可能参与神经精神,神经,神经肌肉和免疫疾病。 提供了大量纯化的hKCa3 / KNN3多肽和多核苷酸。 还公开了与hKCa3 / KCNN3多肽结合的抗体。 提供了鉴定影响hKCa3 / KCNN3多核苷酸或多肽的化合物的方法。 还提供了用于诊断和确定具有hKCa3 / KCNN3相关病症或具有hKCa3 / KCNN3相关病症风险的受试者的预后和治疗方案的方法。 还提供了通过施用治疗有效量的编码SEQ ID NO:2的多核苷酸治疗患有或具有hKCa3 / KCNN3相关病症风险的受试者的方法。 提供了将hKCa3 / KCNN3给予治疗有效量的hKCa3 / KCNN3多肽的患者的制剂。 提供了可用于检测来自具有hKCa3 / KCNN3相关病症的受试者的样品中hKCa3 / KCNN3多肽或多核苷酸的存在的试剂盒。 还描述了具有编码hKCa3 / KCNN3的转基因的转基因非人动物。

    Methods for inhibiting neoproliferative changes in blood vessel walls
    8.
    发明授权
    Methods for inhibiting neoproliferative changes in blood vessel walls 有权
    抑制血管壁新生血管变化的方法

    公开(公告)号:US08026263B2

    公开(公告)日:2011-09-27

    申请号:US10533060

    申请日:2003-10-30

    IPC分类号: A61K31/425

    CPC分类号: A61K31/415

    摘要: Methods, compositions and devices for inhibiting neoproliferative changes in blood vessel walls or other anatomical structures. One or more compounds of Formula I or I-A set forth herein are administered systemically and/or locally to human or veterinary patients to deter or prevent unwanted proliferative changes in blood vessels or other anatomical structures. The invention may be used to deter or prevent stenosis or restenosis of arteries following angioplasty and/or stent placement. In one embodiment, there is provided an implantable stent or stent graft from which one or more compounds of the present invention will elute or otherwise be delivered into an affected blood vessel wall.

    摘要翻译: 用于抑制血管壁或其他解剖结构中新生血管变化的方法,组合物和装置。 本文所述的一种或多种式I或I-A化合物全身和/或局部施用于人或兽医患者以阻止或预防血管或其他解剖结构中不期望的增殖性变化。 本发明可用于阻止或预防血管成形术和/或支架放置后的动脉狭窄或再狭窄。 在一个实施方案中,提供了可植入支架或支架移植物,其中一种或多种本发明化合物将从其中洗脱或以其它方式递送到受影响的血管壁。

    Exons of the hSKCa3/KCNN3 gene
    10.
    发明授权
    Exons of the hSKCa3/KCNN3 gene 失效
    hSKCa3 / KCNN3基因的外显子

    公开(公告)号:US07022480B1

    公开(公告)日:2006-04-04

    申请号:US10269503

    申请日:2002-10-11

    IPC分类号: C12Q1/68 C12N15/867 C12N5/02

    CPC分类号: C07K14/705

    摘要: The present invention is based on the discovery and cloning of two variants of the small conductance calcium activated potassium channel type 3 (hKCa3/KCNN3) gene. The isoform variants are identical to the structure of the SKCa3-1a transcript with regard to exons 2–8, but differ in that one variant, SKCa3-1b, contains exon 1b in place of exon 1a and in that the other variant, SKCa3-1c, contains exon 1c in place of exon 1a. When expressed simultaneously with SKCa3-1a, the variants will independently dominantly negatively suppress SKCa3-1a and other functional members of the SKCa channel family. Accordingly, the present invention provides the novel gene variants, methods for the detection of the variants and treatment of disorders related to the activity of these variants. Kits employing the methods of the invention are also described.

    摘要翻译: 本发明基于小电导钙激活钾通道3型(hKCa3 / KCNN3)基因的两个变体的发现和克隆。 异构体变体与外显子2-8的SKCa3-1a转录物的结构相同,但不同之处在于,一个变体SKCa3-1b含有外显子1b代替外显子1a,而另一个变体SKCa3- 1c,含有外显子1c代替外显子1a。 当与SKCa3-1a同时表达时,变体将独立地主要负面地抑制SKCa3-1a和SKCa3通道家族的其它功能成员。 因此,本发明提供了新的基因变体,检测变体的方法和治疗与这些变体的活性有关的紊乱。 还描述了采用本发明方法的试剂盒。