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    INHIBITORS OF ION CHANNELS
    2.
    发明申请
    INHIBITORS OF ION CHANNELS 审中-公开
    离子通道的抑制剂

    公开(公告)号：WO2007056099A3

    公开(公告)日：2007-07-12

    申请号：PCT/US2006042882

    申请日：2006-11-02

    申请人： ICAGEN INC ,  WANG XIAODONG ,  FULP ALAN ,  MARRON BRIAN ,  BEAUDOIN SERGE ,  SECONI DARRICK ,  SUTO MARK

    发明人： WANG XIAODONG ,  FULP ALAN ,  MARRON BRIAN ,  BEAUDOIN SERGE ,  SECONI DARRICK ,  SUTO MARK

    IPC分类号： A01N43/40

    CPC分类号： C07D277/52 ,  C07D417/12 ,  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 substituted aryl sulfonamides, compositions comprising these compounds, as well as methods of using these compounds or compositions 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，本发明提供取代的芳基磺酰胺，包含这些化合物的组合物，以及使用这些化合物或组合物治疗中枢或周围神经系统疾病，特别是疼痛和慢性疼痛的方法，其通过阻断与起始相关的钠通道或 指示条件复发。 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。

    POLYCYCLIC PYRAZINES AS POTASSIUM ION CHANNEL MODULATORS
    4.
    发明申请
    POLYCYCLIC PYRAZINES AS POTASSIUM ION CHANNEL MODULATORS 审中-公开
    聚氯乙烯作为钾离子通道调节剂

    公开(公告)号：WO2005121126A1

    公开(公告)日：2005-12-22

    申请号：PCT/US2005/012525

    申请日：2005-04-13

    申请人： ICAGEN, INC. ,  ASTELLAS PHARMA INC. ,  WANG, Xiaodong ,  SPEAR, Kerry, Leigh ,  FULP, Alan, Bradley ,  SECONI, Darrick ,  SUZUKI, Takeshi ,  ISHII, Takahiro ,  MORITOMO, Ayako

    发明人： WANG, Xiaodong ,  SPEAR, Kerry, Leigh ,  FULP, Alan, Bradley ,  SECONI, Darrick ,  SUZUKI, Takeshi ,  ISHII, Takahiro ,  MORITOMO, Ayako

    IPC分类号： C07D401/12

    CPC分类号： C07D401/14 ,  C07D213/73 ,  C07D401/04 ,  C07D405/04 ,  C07D405/14 ,  C07D409/04 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

    摘要： The present invention provides a genus of polycyclic pyrazines of formula I (I) that are useful as modulators of potassium ion channels. The modulators of the invention are of use in both therapeutic and diagnostic methods; wherein A and B are independently substituted or unsubstituted 5- or 6-membered heterocycloalkyl, or substituted or unsubstituted 5- or 6- membered heteroaryl, W 1 is formula II (II); W 2 is -CH=, -NH-, -N=, -S-, or -O-; Z 1 is formula III (III) or formula IV (IV); Z 2 is -CH=, -NH-, -N=, -S-, or -O-; Y is a bond, -CH=N-NH-, -NH-CH 2 -, or -NR 5 -; s and t are independently integers from 1 to 4; R 1 , R 2A , R 2B and R 3 are independently or unsubstituted alkyle, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted 3- to 7- membered cycloalkyl,, substituted or unsubstituted 5- to 7-membered heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; and R 5 is H, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted 3- to 7- membered cycloalkyl,, substituted or unsubstituted 5- to 7-membered heterocycloalkyl, substituted or unsubstituted aryl or substituted or unsubstituted heteroaryl; wherein if s is greater than one, then each R 1 is optionally different; wherein if t is greater than on, then each R 3 is optionally different; wherein two R 1 groups are optionally joined together with the atoms to which they are attached to form a substituted or unsubstituted ring; and wherein two R 3 groups are optionally joined together with the atoms to which they are attached to form a susbtituted or unsubstituted ring.

    摘要翻译： 本发明提供了可用作钾离子通道调节剂的式I（I）的多环吡嗪属。 本发明的调节剂可用于治疗和诊断方法; 其中A和B独立地为取代或未取代的5-或6-元杂环烷基，或取代或未取代的5-或6-元杂芳基，W 1为式II（II）; W 2是-CH =，-NH-，-N =，-S-或-O-; Z 1是式III（III）或式IV（IV）; Z 2是-CH =，-NH-，-N =，-S-或-O-; Y是键，-CH = N-NH-，-NH-CH 2 - 或-NR 5 - ; s和t独立地为1至4的整数; R 1，R 2A，R 2B和R 3独立地是未取代的烷基，取代或未取代的烷基，取代或未取代的杂烷基，取代或未取代的3-至7-元环烷基，取代或未取代的 5-至7-元杂环烷基，取代或未取代的芳基或取代或未取代的杂芳基; 并且R 5是H，取代或未取代的烷基，取代或未取代的杂烷基，取代或未取代的3-至7-元环烷基，取代或未取代的5-至7-元杂环烷基，取代或未取代的芳基或取代或未取代的杂芳基 ; 其中如果s大于1，则每个R 1任选地不同; 其中如果t大于on，则每个R 3任选地不同; 其中两个R 1基团任选地与它们所连接的原子连接在一起形成取代或未取代的环; 并且其中两个R 3基团任选地与它们所连接的原子连接在一起以形成未取代或未取代的环。

    FUSED RING HETEROCYCLES AS POTASSIUM CHANNEL MODULATORS
    6.
    发明申请
    FUSED RING HETEROCYCLES AS POTASSIUM CHANNEL MODULATORS 审中-公开
    作为钾通道调节剂的融合环杂环

    公开(公告)号：WO2005025293A2

    公开(公告)日：2005-03-24

    申请号：PCT/US2004/029868

    申请日：2004-09-10

    申请人： ICAGEN, INC. ,  MCNAUGHTON-SMITH, Grant, Andrew ,  AMATO, George, Salvatore ,  THOMAS, James, Barnwell, Jr.

    发明人： MCNAUGHTON-SMITH, Grant, Andrew ,  AMATO, George, Salvatore ,  THOMAS, James, Barnwell, Jr.

    IPC分类号： C07D239/92 ,  C07D285/24 ,  C07D401/12 ,  C07D409/12 ,  C07D413/12 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04 ,  C07D513/04

    CPC分类号： C04B35/632 ,  C07D239/92 ,  C07D285/24 ,  C07D401/12 ,  C07D409/12 ,  C07D413/12 ,  C07D471/04 ,  C07D487/04 ,  C07D513/04

    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 quinazolinone, 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, hearing and vision loss, Alzheimer's disease, age-related memory loss, learning deficiencies, anxiety 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： 提供了用于通过调节通过电压依赖性钾通道的钾离子通量来治疗疾病的化合物，组合物和方法。 更具体地说，本发明提供了可用于治疗中枢或周围神经系统疾病（例如偏头痛，共济失调，帕金森氏病，双相性精神障碍，三叉神经痛，痉挛状态，心境障碍，脑肿瘤，精神病性障碍等的喹唑啉酮，组合物和方法 ，失眠，癫痫发作，癫痫，听力和视力丧失，阿尔茨海默病，与年龄有关的记忆丧失，学习缺陷，焦虑和运动神经元疾病，维持膀胱控制或治疗尿失禁）和作为神经保护剂（例如预防中风和 类似）通过调节与指示病症的发作或复发有关的钾通道。

    PIPERIDINES
    8.
    发明申请
    PIPERIDINES 审中-公开
    哌啶

    公开(公告)号：WO03037890A3

    公开(公告)日：2003-08-21

    申请号：PCT/US0235173

    申请日：2002-11-01

    申请人： ICAGEN INC ,  GROSS MICHAEL FRANCIS ,  ATKINSON ROBERT NELSON ,  JOHNSON MATTHEW SCOTT

    发明人： GROSS MICHAEL FRANCIS ,  ATKINSON ROBERT NELSON ,  JOHNSON MATTHEW SCOTT

    IPC分类号： A61K31/00 ,  A61K31/4439 ,  A61P25/04 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14

    CPC分类号： C07D401/04 ,  A61K31/00 ,  A61K31/4439 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14

    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-dependent sodium channels. More particularly, the invention provides substituted piperidines, and compositions containing these compounds. Also provided are methods using the compounds of the invention for the treatment of central or peripheral nervous system disorders, particularly pain and chronic pain by blocking sodium channels associated with the onset or recurrance 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 channel that includes a PN3 subunit.

    摘要翻译： 提供了通过抑制钠离子通过电压依赖钠通道来治疗疾病的化合物，组合物和方法。 更具体地说，本发明提供取代的哌啶和含有这些化合物的组合物。 还提供了使用本发明化合物治疗中枢性或周围神经系统疾病，特别是疼痛和慢性疼痛的方法，其通过阻断与所述病症的发作或复发有关的钠通道。 本发明的化合物，组合物和方法特别用于通过包含PN3亚基的通道抑制离子通量来治疗神经性或炎性疼痛。

    PYRAZOLOPYRIMIDINES
    10.
    发明申请
    PYRAZOLOPYRIMIDINES 审中-公开
    吡唑并嘧啶

    公开(公告)号：WO2003037900A2

    公开(公告)日：2003-05-08

    申请号：PCT/US2002/035171

    申请日：2002-11-01

    申请人： ICAGEN, INC. ,  ATKINSON, Robert, Nelson ,  GROSS, Michael, Francis ,  VAN RHEE, Michiel, Albert

    发明人： ATKINSON, Robert, Nelson ,  GROSS, Michael, Francis ,  VAN RHEE, Michiel, Albert

    IPC分类号： C07D487/04

    CPC分类号： C07D487/04 ,  A61K31/519

    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-dependent sodium channels. More particularly, the invention provides pyrazolopyrimidines, 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 recurrance 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 channel that includes a PN3 subunit.

    摘要翻译： 提供了通过抑制钠离子通过电压依赖钠通道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吡唑并嘧啶类，组合物和方法，其通过阻断与所述病症的发作或复发有关的钠通道。 本发明的化合物，组合物和方法特别用于通过包含PN3亚基的通道抑制离子通量来治疗神经性或炎性疼痛。