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1. 发明申请

WO2009012242A3 SODIUM CHANNEL INHIBITORS 审中-公开
标题翻译：钠通道抑制剂
公开(公告)号：WO2009012242A3
公开(公告)日：2009-03-05
申请号：PCT/US2008070019
申请日：2008-07-14
申请人： ICAGEN INC , FULP ALAN BRADLEY , JOHNSON MATTHEW SCOTT , MARKWORTH CHRISTOPHER JOHN , MARRON BRIAN EDWARD , SECONI DARRICK CONWAY , WEST CHRISTOPHER WILLIAM , WANG XIAODONG , ZHOU SHULAN
发明人： FULP ALAN BRADLEY , JOHNSON MATTHEW SCOTT , MARKWORTH CHRISTOPHER JOHN , MARRON BRIAN EDWARD , SECONI DARRICK CONWAY , WEST CHRISTOPHER WILLIAM , WANG XIAODONG , ZHOU SHULAN
IPC分类号： C07D413/12 , A61K31/427 , A61P25/00 , C07D417/12
CPC分类号： C07D417/12 , C07D413/12
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 sulfonamides, compos i-tiona 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. Formula (II)
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，本发明提供了取代磺酰胺，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，其通过阻断与发作或复发的指示条件。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。式（II）

2. 发明申请

WO03037890A3 PIPERIDINES 审中-公开
标题翻译：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。

3. 发明专利

CA2693588C SODIUM CHANNEL INHIBITORS 未知
公开(公告)号：CA2693588C
公开(公告)日：2015-11-17
申请号：CA2693588
申请日：2008-07-14
申请人： ICAGEN INC
发明人： FULP ALAN BRADLEY , JOHNSON MATTHEW SCOTT , MARKWORTH CHRISTOPHER JOHN , MARRON BRIAN EDWARD , SECONI DARRICK CONWAY , WEST CHRISTOPHER WILLIAM , WANG XIAODONG , ZHOU SHULAN
IPC分类号： C07D413/12 , A61K31/427 , A61P25/00 , C07D417/12
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 sulfonamides, compos i-tiona 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. Formula (II)

4. 发明专利

CA2694748A1 SODIUM CHANNEL INHIBITORS 未知
公开(公告)号：CA2694748A1
公开(公告)日：2009-01-22
申请号：CA2694748
申请日：2008-07-14
申请人： ICAGEN INC
发明人： BEAUDOIN SERGE , JOHNSON MATTHEW SCOTT , MARRON BRIAN EDWARD , SUTO MARK J
IPC分类号： C07D277/52 , A61K31/426 , A61P25/00
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.

5. 发明专利

ES2523196T3 Inhibidores de los canales de sodio 未知
公开(公告)号：ES2523196T3
公开(公告)日：2014-11-21
申请号：ES08781823
申请日：2008-07-14
申请人： ICAGEN INC
发明人： BEAUDOIN SERGE , JOHNSON MATTHEW SCOTT , MARRON BRIAN EDWARD , SUTO MARK J
IPC分类号： C07D277/52 , A61K31/426 , A61P29/00
摘要： Un compuesto de acuerdo con la Fórmula I:**Fórmula** o una sal o solvato aceptable farmacéuticamente del mismo, en la que R1, R2, R3, R4, R5 y R6 están cada uno independientemente seleccionados entre H, halógeno, alquilo de C1-8, arilo, heteroarilo o heterocicloalquilo, en los que dos o más elementos seleccionados entre R1, R2, R3, R4, R5 y R6 están opcionalmente unidos para formar un anillo carbocíclico o heterocíclico de 4-8 elementos teniendo desde 1-3 heteroátomos como elementos del anillo seleccionados entre O, N o S; R7 es un elemento seleccionado entre alquilo de C1-8, heterocicloalquilo, arilo y heteroarilo, con la condición de que R7 sea distinto de metilo, y R7 no esté unido al resto S(O)2 de la Fórmula (I) mediante un enlace azufrenitrógeno; en la que la porción alifática de los grupos R1, R2, R3, R4, R5, R6, R7 está opcionalmente substituida con desde 1-3 substituyentes Ra seleccionados entre el grupo que consiste en -ORb, >=O, >=NRb, >=N-ORb, >=NRbRb, -SRb, - halógeno, -Si(Rb)3,-OC(O)Rb, -C(O)Rb, -CO2Rb, -CON(Rb)2, -OC(O)N(Rb)2, -NRbC(O)Rb, -NRb-C(O)N(Rb)2, - NRbC(O)2Rb, -NRb-C(NRbRb)>=NRb, -S(O)Rb, -S(O)2Rb, -S(O)2N(Rb)2, -NRSO2Rb, alquilo de C1-8, -Rb, -CN y -NO2, en los que cada Rb es independientemente H, alquilo de C1-8, arilo o heteroarilo y dos grupos Rb cuando están unidos al mismo átomo de nitrógeno están opcionalmente combinados conjuntamente con el átomo de nitrógeno al cual están unidos para formar un anillo de 5-6 elementos teniendo desde 0-2 heteroátomos adicionales como elementos del anillo seleccionados entre O, N o S; en los que cada grupo Rb está además opcionalmente substituido con desde 1-3 substituyentes Rc seleccionados entre -ORd, >=O, >=NRd, >=N-ORd, >=NRdRd, -SRd, - halógeno, -Si(Rd)3,-OC(O)Rd, -C(O)Rd, -CO2Rd, -CON(Rd)2, -OC(O)N(Rd)2, -NRdC(O)Rd, -NRd-C(O)N(Rd)2, - NRdC(O)2Rd, -NRd-C(NRdRd)>=NRd, -S(O)Rd, -S(O)2Rd, -S(O)2N(Rd)2, -NRSO2Rd, alquilo de C1-8, -CN y -NO2, en los que cada Rd es H, alquilo de C1-8 o arilo y dos grupos Rd cuando están unidos al mismo átomo de nitrógeno están opcionalmente combinados conjuntamente con el átomo de nitrógeno al cual están unidos para formar un anillo de 5-6 elementos teniendo desde 0-2 heteroátomos adicionales como elementos del anillo seleccionados entre O, N o S; el resto arilo o heteroarilo de los grupos R1, R2, R3, R4, R5, R6 y R7 están opcionalmente substituido con desde 1-3 substituyentes Re seleccionados entre halógeno, -ORbf, -NRfRf, -SRf, -halógeno, -Si(Rf)3,- OC(O)Rf, -C(O)Rf, -CO2Rf, -CON(Rf)2, -OC(O)N(Rf)2, -NRfC(O)Rf, -NRf-C(O)N(Rf)2, -NRfC(O)2Rf, -NRf- C(NRfRf)>=NRf, -S(O)Rf, -S(O)2Rf, -S(O)2NRfRf, -NRSO2Rf, alquilo de C1-8, -CN, y -NO2, alquilo de C1-8, -N3, - CH(Ph)2, fluoroalcoxi de C1-4, y fluoroalquilo de C1-4, en los que en los que Rf es -H, alquilo de C1-8, arilo o heteroarilo y dos grupos Rf cuando están unidos al mismo átomo de nitrógeno están opcionalmente combinados conjuntamente con el átomo de nitrógeno al cual están unidos para formar un anillo de 5-6 elementos teniendo desde 0-2 heteroátomos adicionales como elementos del anillo seleccionados entre O, N o S; en los que la porción alifática del grupo Rf está además opcionalmente substituida con desde 1-3 substituyentes Ra y la porción aromática del grupo Rf está además opcionalmente substituida con desde 1-3 substituyentes Rg seleccionados entre -ORh, -NRhRh, -SRh, -halógeno, -Si(Rh)3,-OC(O)Rh, -C(O)Rh, -CO2Rh, -CON(Rh)2, -OC(O)N(Rh)2, - NRhC(O)Rh, -NRh-C(O)N(Rh)2, -NRhC(O)2Rh, -NRh-C(NRhRh)>=NRh, -S(O)Rh, -S(O)2Rh, -S(O)2NRhRh, -NRSO2Rh, -CN y -NO2, alquilo de C1-8, -N3, -CH(Ph)2, fluoroalcoxi de C1-4, y fluoroalquilo de C1-4, en los que Rh es -H o alquilo de C1-8; en los que dos grupos Rh cuando están unidos al mismo átomo de nitrógeno están opcionalmente combinados con el átomo de nitrógeno al cual están unidos para formar un anillo de 5-6 elementos teniendo desde 0-2 heteroátomos adicionales como elementos del anillo seleccionados entre O, N o S; B es un elemento seleccionado entre cicloalquileno de C3-7, arileno y heteroarileno, o B está opcionalmente unido a R7 para formar un anillo fusionado, en el que el cicloalquileno está opcionalmente substituido con desde 1- 3 substituyentes Rb y el resto arileno o heteroarileno está opcionalmente substituido con desde 1-3 substituyen45 tes Rg;

6. 发明专利

CA2465328C PIPERIDINES 未知
公开(公告)号：CA2465328C
公开(公告)日：2011-06-14
申请号：CA2465328
申请日：2002-11-01
申请人： ICAGEN INC
发明人： GROSS MICHAEL FRANCIS , ATKINSON ROBERT NELSON , JOHNSON MATTHEW SCOTT
IPC分类号： C07D401/04 , A61K31/00 , A61K31/4439 , A61P25/04 , 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 of Formula I, 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.

7. 发明专利

CA2693588A1 SODIUM CHANNEL INHIBITORS 未知
公开(公告)号：CA2693588A1
公开(公告)日：2009-01-22
申请号：CA2693588
申请日：2008-07-14
申请人： ICAGEN INC
发明人： FULP ALAN BRADLEY , JOHNSON MATTHEW SCOTT , MARKWORTH CHRISTOPHER JOHN , MARRON BRIAN EDWARD , SECONI DARRICK CONWAY , WEST CHRISTOPHER WILLIAM , WANG XIAODONG , ZHOU SHULAN
IPC分类号： C07D413/12 , A61K31/427 , A61P25/00 , C07D417/12
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 sulfonamides, compos i-tiona 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. Formula (II)

8. 发明专利

CA2465328A1 PIPERIDINES 未知
公开(公告)号：CA2465328A1
公开(公告)日：2003-05-08
申请号：CA2465328
申请日：2002-11-01
申请人： ICAGEN INC
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
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 chroni c 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.

9. 发明公开

EP2175728A4 SODIUM CHANNEL INHIBITORS 有权
标题翻译： NATRIUMKANALHEMMER
公开(公告)号：EP2175728A4
公开(公告)日：2010-09-15
申请号：EP08781823
申请日：2008-07-14
申请人： ICAGEN INC
发明人： BEAUDOIN SERGE , JOHNSON MATTHEW SCOTT , MARRON BRIAN EDWARD , SUTO MARK J
IPC分类号： C07D277/52 , A61K31/426 , A61P29/00
CPC分类号： C07D277/52

10. 发明公开

EP1451173A4 PIPERIDINES 审中-公开
标题翻译： PIPERIDINE
公开(公告)号：EP1451173A4
公开(公告)日：2005-10-26
申请号：EP02792225
申请日：2002-11-01
申请人： ICAGEN INC
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

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