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41 条记录 (耗时 0.046 秒)

    Inhibitors of ion channels
    1.
    发明授权
    Inhibitors of ion channels 失效
    离子通道抑制剂

    公开(公告)号：US08063080B2

    公开(公告)日：2011-11-22

    申请号：US12561002

    申请日：2009-09-16

    申请人： Alan Fulp ,  Brian Marron ,  Mark J. Suto ,  Xiaodong Wang

    发明人： Alan Fulp ,  Brian Marron ,  Mark J. Suto ,  Xiaodong Wang

    IPC分类号： A61K31/427 ,  C07D277/52 ,  C07D277/28

    CPC分类号： C07D417/12 ,  C07D401/12 ,  C07D417/14

    摘要： Compounds, compositions and methods are provided which are useful in the treatment of diseases through the inhibition of sodium ion flux through voltage-gated sodium channels. More particularly, the invention provides heterocyclic aryl sulfonamides, compositions and methods that are useful in the treatment of central or peripheral nervous system disorders, particularly pain and chronic pain by blocking sodium channels associated with the onset or recurrence of the indicated conditions. The compounds, compositions and methods of the present invention are of particular use for treating neuropathic or inflammatory pain by the inhibition of ion flux through a voltage-gated sodium channel.

    摘要翻译： 提供了可用于通过电压门控钠通道抑制钠离子通量来治疗疾病的化合物，组合物和方法。 更具体地，本发明提供了可用于治疗中枢或周围神经系统疾病，特别是疼痛和慢性疼痛的杂环芳基磺酰胺，组合物和方法，其通过阻断与所述病症的发作或复发相关的钠通道。 本发明的化合物，组合物和方法特别用于通过电压门控钠通道抑制离子通量来治疗神经性或炎性疼痛。

    HETEROCYCLES AS POTASSIUM CHANNEL MODULATORS
    3.
    发明申请
    HETEROCYCLES AS POTASSIUM CHANNEL MODULATORS 有权
    杂质作为钾通道调节剂

    公开(公告)号：US20090062290A1

    公开(公告)日：2009-03-05

    申请号：US12193639

    申请日：2008-08-18

    申请人： Thomas Eugene Christos ,  George S. Amato ,  Robert N. Atkinson ,  Maria Graciela Barolli ,  Lilli Wolf-Gouveia ,  Mark J. Suto

    发明人： Thomas Eugene Christos ,  George S. Amato ,  Robert N. Atkinson ,  Maria Graciela Barolli ,  Lilli Wolf-Gouveia ,  Mark J. Suto

    IPC分类号： A61K31/5025 ,  A61K31/437 ,  C07D471/04 ,  A61K31/519 ,  C12N5/06 ,  A61P25/28 ,  C07D487/04

    CPC分类号： C07D471/04 ,  C07D487/04

    摘要： Compounds, compositions and methods are provided which are useful in the treatment of diseases through the modulation of potassium ion flux through voltage-dependent potassium channels. More particularly, the invention provides heterocycles, compositions and methods that are useful in the treatment of central or peripheral nervous system disorders (e.g., migraine, ataxia, Parkinson's disease, bipolar disorders, trigeminal neuralgia, spasticity, mood disorders, brain tumors, psychotic disorders, myokymia, seizures, epilepsy, seizure, retinal degeneration, hearing and vision loss, Alzheimer's disease, age-related memory loss, learning deficiencies, anxiety, neuronal degeneration and motor neuron diseases, maintaining bladder control or treating urinary incontinence) and as neuroprotective agents (e.g., to prevent stroke and the like) by modulating potassium channels associated with the onset or recurrence of the indicated conditions.

    摘要翻译： 提供了通过电压依赖钾通道调节钾离子通量可用于治疗疾病的化合物，组合物和方法。 更具体地说，本发明提供了可用于治疗中枢性或周围神经系统疾病（例如偏头痛，共济失调，帕金森病，双相情感障碍，三叉神经痛，痉挛状态，情绪障碍，脑肿瘤，精神病症）的杂环，组合物和方法 ，癫痫，癫痫，癫痫，癫痫发作，视网膜变性，听力和视力丧失，阿尔茨海默病，年龄相关记忆丧失，学习缺陷，焦虑，神经元变性和运动神经元疾病，维持膀胱控制或治疗尿失禁）和神经保护剂 （例如，为了预防中风等）通过调节与指示的病症的发作或复发相关的钾通道。

    Cytokine restraining agents and methods of use in pathologies and conditions associated with altered cytokine levels
    6.
    发明授权
    Cytokine restraining agents and methods of use in pathologies and conditions associated with altered cytokine levels 失效
    细胞因子抑制剂和与改变的细胞因子水平相关的病理学和病症中使用的方法

    公开(公告)号：US5760001A

    公开(公告)日：1998-06-02

    申请号：US447143

    申请日：1995-05-22

    申请人： Beverly E. Girten ,  Richard A. Houghten ,  Costas C. Loullis ,  Mark J. Suto ,  Ronald R. Tuttle

    发明人： Beverly E. Girten ,  Richard A. Houghten ,  Costas C. Loullis ,  Mark J. Suto ,  Ronald R. Tuttle

    IPC分类号： A61K38/00 ,  C07K5/087 ,  C07K5/117 ,  C07K7/06 ,  C07K14/68 ,  C07K14/695

    CPC分类号： C07K7/06 ,  C07K14/68 ,  C07K14/695 ,  C07K5/0812 ,  C07K5/1024 ,  A61K38/00

    摘要： The present invention relates to novel peptides that are potent cytokine restraining agents. In addition, the present invention relates to pharmaceutical compositions comprising a pharmaceutically acceptable carrier and a cytokine restraining agent. Administration of such a cytokine restraining agent to a subject restrains, but does not necessarily suppress, cytokine activity completely. Thus, the present invention provides a method of restraining pathologically elevated cytokine activity in a subject. The invention also provides methods of treating disuse deconditioning and diseases mediated by nitric oxide and cytokines, such as diabetes and glomerulonephritis, a method of organ protection, a method of organ protection, and a method of reducing the negative side effects of cancer chemotherapy, such as nephrotoxicity.

    摘要翻译： 本发明涉及有效的细胞因子抑制剂的新型肽。 此外，本发明涉及包含药学上可接受的载体和细胞因子抑制剂的药物组合物。 对受试者施用这种细胞因子抑制剂抑制，但不一定抑制细胞因子活性。 因此，本发明提供抑制受试者中病理升高的细胞因子活性的方法。 本发明还提供了治疗废用脱毒和由一氧化氮和细胞因子如糖尿病和肾小球肾炎介导的疾病，器官保护方法，器官保护方法和降低癌症化学疗法的负面副作用的方法， 作为肾毒性。

    Process for chiral 3-(1-amino-1,1-bisalkylmethyl)-1-substituted-pyrrolidines
    9.
    发明授权
    Process for chiral 3-(1-amino-1,1-bisalkylmethyl)-1-substituted-pyrrolidines 失效
    手性3-（1-氨基-1,1-双烷基甲基）-1-取代吡咯烷的方法

    公开(公告)号：US5347017A

    公开(公告)日：1994-09-13

    申请号：US88464

    申请日：1993-07-07

    申请人： Victor Fedij ,  Mark J. Suto ,  James N. Wemple ,  James R. Zeller

    发明人： Victor Fedij ,  Mark J. Suto ,  James N. Wemple ,  James R. Zeller

    IPC分类号： C07D207/09 ,  C07D207/50

    CPC分类号： C07D207/09

    摘要： The process for the preparation of chiral 3-(1-amino-1,1-bisalkylmethyl)-1-substituted-pyrrolidines used as key intermediates for the preparation of naphthyridine and quinolone antibacterial agents which comprises reacting readily available chiral 1-substituted-3-pyrrolidinols to their corresponding chiral sulfonate esters; converting the sulfonate esters to chiral 1-substituted-3-cyanopyrrolidines having an inverse configuration, and then dialkylating the chiral cyanopyrrolidines with alkyl lithium in the presence of a Lewis acid without racemization at the asymmetric carbon atom is described.

    摘要翻译： 用作制备萘啶和喹诺酮抗菌剂的关键中间体的手性3-（1-氨基-1,1-双烷基甲基）-1-取代吡咯烷的制备方法，其包括使容易获得的手性1-取代-3 - 吡咯烷醇与其相应的手性磺酸酯; 将磺酸酯转化成具有相反构型的手性1-取代-3-氰基吡咯烷酮，然后在不对称碳原子下进行外消旋化的路易斯酸存在下，用烷基锂二烷基化手性氰基吡咯烷。