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1. 发明申请

WO0208183A3 POTASSIUM CHANNEL INHIBITORS 审中-公开
标题翻译：钾通道抑制剂
公开(公告)号：WO0208183A3
公开(公告)日：2002-07-04
申请号：PCT/US0123595
申请日：2001-07-26
申请人： ICAGEN INC , BEAUDOIN SERGE , GROSS MICHAEL F , REED AIMEE D , WICKENDEN ALAN D , ZOU ANRUO
发明人： BEAUDOIN SERGE , GROSS MICHAEL F , REED AIMEE D , WICKENDEN ALAN D , ZOU ANRUO
IPC分类号： A61P9/06 , C07D213/40 , C07D233/54 , C07D233/64 , C07D409/12 , A61K31/417 , A61K31/4402 , A61K31/505 , C07D239/26
CPC分类号： C07D213/40 , C07D233/64 , C07D409/12
摘要： Compounds which are useful as potassium channel inhobitors and which because of their slow off-rate are especially useful for the treatment of cardiac arrhythmias are described.
摘要翻译：描述了用作钾通道抑制剂并且因其缓慢解离速率而特别适用于治疗心律失常的化合物。

2. 发明申请

WO03088908A2 HETEROCYCLO INHIBITORS OF POTASSIUM CHANNEL FUNCTION 审中-公开
标题翻译：钾离子通道功能的杂环抑制剂
公开(公告)号：WO03088908A2
公开(公告)日：2003-10-30
申请号：PCT/US0311807
申请日：2003-04-16
申请人： SQUIBB BRISTOL MYERS CO , LLOYD JOHN , JEON YOON T , FINLAY HEATHER , ICAGEN INC , YAN LIN , BEAUDOIN SERGE , GROSS MICHAEL F
发明人： LLOYD JOHN , JEON YOON T , FINLAY HEATHER , YAN LIN , BEAUDOIN SERGE , GROSS MICHAEL F
IPC分类号： C07D233/04 , A61K31/445 , A61K31/4535 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/497 , A61K31/506 , A61K31/5377 , A61K31/55 , A61P1/04 , A61P3/10 , A61P9/00 , A61P9/06 , A61P11/08 , A61P25/06 , A61P25/08 , A61P25/28 , A61P29/00 , A61P37/00 , A61P43/00 , C07D211/26 , C07D211/28 , C07D211/34 , C07D211/58 , C07D211/62 , C07D211/64 , C07D211/96 , C07D223/04 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/06 , C07D417/12 , C07D521/00 , A61K
CPC分类号： C07D211/26 , C07D211/34 , C07D211/62 , C07D211/64 , C07D211/96 , C07D223/04 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/12
摘要： Novel heterocyclo compounds useful as inhibitors of potassium channel function (especially inhibitors of the Kv1 subfamily of voltage gated K+ channels, especially inhibitors Kv1.5 which has been linked to the ultra-rapidly activating delayed rectifier K+ current IKur), methods of using such compounds in the prevention and treatment of arrhythmia and IKur-associated conditions, and pharmaceutical compositions containing such compounds.
摘要翻译：可用作钾通道功能抑制剂的新型杂环化合物（特别是电压门控K +通道的Kv1亚族抑制剂，特别是与超快速激活延迟整流K +电流IKur连接的抑制剂Kv1.5），使用这些化合物的方法在预防和治疗心律失常和IKur相关病症中，以及含有这些化合物的药物组合物。

4. 发明申请

WO2007056099A3 INHIBITORS OF ION CHANNELS 审中-公开
标题翻译：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。

5. 发明申请

WO02060874A8 POTASSIUM CHANNEL INHIBITORS 审中-公开
标题翻译：钾通道抑制剂
公开(公告)号：WO02060874A8
公开(公告)日：2003-02-20
申请号：PCT/US0148601
申请日：2001-12-19
申请人： ICAGEN INC
发明人： BEAUDOIN SERGE , REED AIMEE D , GROSS MICHAEL
IPC分类号： C07C311/20 , C07D213/38 , C07D213/61 , C07D213/74 , C07D213/75 , C07D213/80 , C07D213/82 , C07D233/54 , C07D239/42 , C07D405/12 , C07D409/12 , A61K31/18 , A61K31/44
CPC分类号： C07D213/74 , C07C311/20 , C07C2602/08 , C07D213/38 , C07D213/61 , C07D213/75 , C07D213/80 , C07D213/82 , C07D233/64 , C07D239/42 , C07D405/12 , C07D409/12
摘要： Compounds useful as potassium channel inhibitors and especially useful for the treatment of cardiac arrhythmias and cell proliferative disorders of the formula (I) are described, wherein A, B and D are selected from a substituted carbon atom, a nitrogen atom or N}O, wherein at least one of A, B and D is substituted carbon atom and at most only one of A, B and D is N}O; E is hydrogen, or alkyl; G is hydrogen, or alkyl; or E and G taken together form a bond (site of unsaturation); R is selected from hydrogen, alkyl, carbocycloalkyl, aryl, (aryl)alkyl, heterocyclo, (heterocyclo)alkyl, heteroaryl and (heteroaryl)alkyl; R is selected from alkyl, carbocycloalkyl, aryl, (aryl)alkyl, heterocyclo, (heterocyclo)alkyl, heteroaryl and (heteroaryl)alkyl; R is selected from hydrogen (H), alkyl, carbocycloalkyl, aryl, (aryl)alkyl, heterocyclo, (heterocyclo)alkyl, heteroaryl, (heteroaryl)alkyl, aminoalkyl; substituted aminoalkyl, carboxyalkyl, alkoxyalkanoyl, aminoalkanoyl, substituted aminoalkanoyl, alkanoylaminoalkyl, alkanoyl(substituted amido)alkyl, aroylamidoalkyl, aroyl(substituted amido)alkyl, heterocyclocarbonylamidoalkyl, heterocyclocarbonyl(substituted amido)alkyl, heteroaroylamidoalkyl, and heteroaroyl(substituted amido)alkyl; R is selected from alkyl, carbocycloalkyl, aryl, (aryl)alkyl, heteroaryl and heterocyclo; R and R are each independently selected from hydrogen, fluoro and alkyl, or R and R taken together, along with the carbon atom to which they are both attached, form a 3-membered to 7-membered carbocyclic, or heterocyclic ring; R is independently selected from hydrogen, alkyl, hydroxy, alkoxy, amino, substituted amino, nitro, cyano, halo, carboxy, alkoxycarbonyl, aminocarbonyl, substituted aminocarbonyl and n is 1, 2 or 3; Z is selected from hydrogen, alkyl, hydroxy, SH, alkoxy, aryloxy, alkylthio, amino, substituted amino, alkoxycarbonyl, alkanoylamido, aroylamido, heterocyclocarbonylamido, heteroaroylamido, alkanoyl(alkylsubstituted)amido, aroyl(alkylsubstituted)amido, heteroaroyl(alkylsubstituted)amido and heterocyclocarbonyl(alkyl substituted)amido.
摘要翻译：描述了可用作钾通道抑制剂并且特别可用于治疗式（I）的心律失常和细胞增殖性病症的化合物，其中A，B和D选自取代的碳原子，氮原子或N} O，其中A，B和D中的至少一个为取代的碳原子，A，B和D中至多一个为N} O; E是氢或烷基; G是氢或烷基; 或E和G一起形成键（不饱和位点）; R 1选自氢，烷基，碳环烷基，芳基，（芳基）烷基，杂环基，（杂环）烷基，杂芳基和（杂芳基）烷基; R 2选自烷基，碳环烷基，芳基，（芳基）烷基，杂环基，（杂环）烷基，杂芳基和（杂芳基）烷基; R 3选自氢（H），烷基，碳环烷基，芳基，（芳基）烷基，杂环基，（杂环）烷基，杂芳基，（杂芳基）取代的氨基烷基，羧基烷基，烷氧基烷酰基，氨基烷酰基，取代的氨基烷酰基，烷酰基氨基烷基，烷酰基（取代的酰胺基）烷基，芳酰胺基烷基，芳酰基（取代的酰胺基）烷基，杂环羰基氨基烷基，杂环羰基（取代的酰胺基）烷基，杂芳酰氨基烷基和杂芳酰基（取代的酰氨基） R 4选自烷基，碳环烷基，芳基，（芳基）烷基，杂芳基和杂环; R 5和R 6各自独立地选自氢，氟和烷基，或者R 5和R 6一起连同它们所连接的碳原子一起形成3元环至7元碳环或杂环; R 7独立地选自氢，烷基，羟基，烷氧基，氨基，取代的氨基，硝基，氰基，卤素，羧基，烷氧基羰基，氨基羰基，取代的氨基羰基，n是1,2或3; Z选自氢，烷基，羟基，SH，烷氧基，芳氧基，烷硫基，氨基，取代氨基，烷氧基羰基，烷酰氨基，芳酰胺基，杂环羰基酰胺基，杂芳酰氨基，烷酰基（烷基取代的）酰胺基，芳酰基（烷基取代的）酰胺基，杂芳酰基和杂环羰基（烷基取代的）酰氨基。

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