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1. 发明申请

WO2007056099A2 INHIBITORS OF ION CHANNELS 审中-公开
标题翻译：离子通道抑制剂
公开(公告)号：WO2007056099A2
公开(公告)日：2007-05-18
申请号：PCT/US2006/042882
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： A61K31/513 , A61K31/497 , A61K31/4439 , A61K31/426 , C07D417/02
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：提供了可用于通过抑制通过电压门控钠通道的钠离子流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外周神经系统疾病，特别是通过阻断与发作相关的钠通道引起的疼痛和慢性疼痛或指定条件的重现。本发明的化合物，组合物和方法特别用于通过抑制通过电压门控钠通道的离子通量来治疗神经性疼痛或炎性疼痛。

2. 发明申请

WO2009012242A2 SODIUM CHANNEL INHIBITORS 审中-公开
标题翻译：钠通道抑制剂
公开(公告)号：WO2009012242A2
公开(公告)日：2009-01-22
申请号：PCT/US2008/070019
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 , C07D417/12 , A61K31/427 , A61P25/00
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, 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。更具体地说，本发明提供取代磺酰胺，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，特别是通过阻断与发作或复发有关的钠通道的疼痛和慢性疼痛的方法的指示条件。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。

3. 发明申请

WO2007021941A2 INHIBITORS OF VOLTAGE-GATED SODIUM CHANNELS 审中-公开
标题翻译：电压门控通道的抑制剂
公开(公告)号：WO2007021941A2
公开(公告)日：2007-02-22
申请号：PCT/US2006/031390
申请日：2006-08-11
申请人： ICAGEN, INC. , FULP, Alan , MARRON, Brian , SUTO, Mark, J. , WANG, Xiaodong
发明人： FULP, Alan , MARRON, Brian , SUTO, Mark, J. , WANG, Xiaodong
IPC分类号： A61K31/513 , A61K31/497 , A61K31/4965 , A61K31/4439 , A61K31/427 , A61K31/426 , A61K31/4196 , A61K31/4192
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。

4. 发明申请

WO2005121126A1 POLYCYCLIC PYRAZINES AS POTASSIUM ION CHANNEL MODULATORS 审中-公开
标题翻译：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。

5. 发明申请

WO2005100340A2 POLYCYCLIC PYRIDINES AS POTASSIUM ION CHANNEL MODULATORS 审中-公开
公开(公告)号：WO2005100340A2
公开(公告)日：2005-10-27
申请号：PCT/US2005/012524
申请日：2005-04-13
申请人： ICAGEN, INC. , WANG, Xiaodong , SPEAR, Kerry, L. , FULP, Alan, B. , SECONI, Darrick
发明人： WANG, Xiaodong , SPEAR, Kerry, L. , FULP, Alan, B. , SECONI, Darrick
IPC分类号： C07D401/00
CPC分类号： C07D401/14 , C07D471/04 , C09B57/10
摘要： The present invention provides a genus of polycyclic pyridines that are useful as modulators of potassium ion channels. The modulators of the invention are of use in both therapeutic and diagnostic methods.

6. 发明申请

WO2005100349A2 POLYCYCLIC PYRIDINES AS POTASSIUM ION CHANNEL MODULATORS 审中-公开
标题翻译：作为钾离子通道调节剂的多环吡啶
公开(公告)号：WO2005100349A2
公开(公告)日：2005-10-27
申请号：PCT/US2005/012837
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 , KUBOTA, Hideki , KAZAMI, Jun-ichi
发明人： WANG, Xiaodong , SPEAR, Kerry, Leigh , FULP, Alan, Bradley , SECONI, Darrick , SUZUKI, Takeshi , ISHII, Takahiro , MORITOMO, Ayako , KUBOTA, Hideki , KAZAMI, Jun-ichi
IPC分类号： C07D417/14
CPC分类号： C07D401/04 , C07D213/61 , C07D213/65 , C07D213/73 , C07D213/74 , C07D213/75 , C07D213/80 , C07D213/82 , C07D401/14 , C07D405/04 , C07D409/04 , C07D417/04 , C07D417/14 , C07D453/02 , C07D471/04 , C09B57/10
摘要： The present invention provides a genus of polycyclic pyridines that are useful as modulators of potassium ion channels. The modulators of the invention are of use in both therapeutic and diagnostic methods.
摘要翻译：本发明提供了可用作钾离子通道调节剂的多环吡啶类。本发明的调节剂可用于治疗和诊断方法。

7. 发明申请

WO2006084031A1 IMINES AS ION CHANNEL MODULATORS 审中-公开
标题翻译： IMINES作为离子通道调制器
公开(公告)号：WO2006084031A1
公开(公告)日：2006-08-10
申请号：PCT/US2006/003677
申请日：2006-02-01
申请人： ICAGEN, INC. , WANG, Xiaodong , FULP, Alan, Bradley , SECONI, Darrick
发明人： WANG, Xiaodong , FULP, Alan, Bradley , SECONI, Darrick
IPC分类号： C07C257/14 , C07C259/14 , C07C259/12 , C07C257/22 , C07C251/80 , C07C251/40 , C07D213/61 , C07F9/24 , C07F9/02 , A61K31/155 , A61K31/15 , A61K31/44 , A61K31/66 , A61P7/00
CPC分类号： C07D213/54 , C07C251/40 , C07C251/80 , C07C257/06 , C07C257/14 , C07C257/22 , C07C259/12 , C07C259/14 , C07D213/58 , C07D413/06 , C07F9/12
摘要： The present invention provides a class of chemical compounds useful in the treatment of sickle cell disease, diseases characterized by unwanted or abnormal cell proliferation and for the treatment of ocular disorders such as glaucoma. The active compounds are tri-(aryl or heteroaryl) methane compounds or analogues thereof which further comprise an imine moiety and where the tertiary carbon atom can be replaced with a different atom such as Si, Ge, N or P. The compounds enhance resistance to degradation in a biological medium, inhibit potassium flux in a cell, reduce mammalian cell proliferation, reduce the Gardos channel of erythrocytes, reduce sickle erythrocyte dehydration and/or delay the occurrence of erythrocyte sickling or deformation.
摘要翻译：本发明提供了一类用于治疗镰状细胞病，特征在于不想要的或异常细胞增殖的疾病和用于治疗眼部疾病如青光眼的化合物。活性化合物是三（芳基或杂芳基）甲烷化合物或其类似物，其还包含亚胺部分，其中叔碳原子可被不同的原子如Si，Ge，N或P替代。化合物增强了对在生物培养基中降解，抑制细胞内的钾通量，减少哺乳动物细胞增殖，减少红细胞的Gardos通道，减少镰状红细胞脱水和/或延缓红细胞镰状或变形的发生。

8. 发明申请

WO2005099673A1 POLYCYLIC THIAZOLES AS POTASSIUM ION CHANNEL MODULATORS 审中-公开
标题翻译：多氯联苯作为离子通道调节剂
公开(公告)号：WO2005099673A1
公开(公告)日：2005-10-27
申请号：PCT/US2005/012911
申请日：2005-04-13
申请人： ICAGEN, INC. , ASTELLAS PHARMA INC. , WANG, Xiaodong , SPEAR, Kerry, Leigh , PULP, Alan, Bradley , SECONI, Darrick , SUZUKI, Takeshi , ISHII, Takahiro , MORITOMO, Ayako , KUBOTA, Hideki
发明人： WANG, Xiaodong , SPEAR, Kerry, Leigh , PULP, Alan, Bradley , SECONI, Darrick , SUZUKI, Takeshi , ISHII, Takahiro , MORITOMO, Ayako , KUBOTA, Hideki
IPC分类号： A61K9/20
CPC分类号： C07D417/14
摘要： The present invention provides a genus of polycyclic thiazoles that are useful as modulators of potassium ion channels. The modulators of the invention are of use in both therapeutic and diagnostic methods.
摘要翻译：本发明提供了可用作钾离子通道调节剂的多环噻唑属。本发明的调节剂在治疗和诊断方法中都有用。

9. 发明申请

WO2003094861A3 BIS-BENZIMIDAZOLES AND RELATED COMPOUNDS AS POTASSIUM CHANNEL MODULATORS 审中-公开
公开(公告)号：WO2003094861A3
公开(公告)日：2003-11-20
申请号：PCT/US2003/015225
申请日：2003-05-13
申请人： ICAGEN, INC. , WANG, Xiaodong , FULP, Alan, Bradley , VAN RHEE, Albert, Michiel , SPEAR, Kerry, Leigh
发明人： WANG, Xiaodong , FULP, Alan, Bradley , VAN RHEE, Albert, Michiel , SPEAR, Kerry, Leigh
IPC分类号： C07D403/10
摘要： The present invention provides a genus of bis-benzimidazole compounds, methods and pharmaceutical compositions that are useful as modulators of potassium ion channels. The compounds of the invention are of use in both therapeutic and diagnostic methods.

10. 发明申请

WO2005002503A2 ASYMMETRIC BENZIMIDAZOLES AND RELATED COMPOUNDS AS POTASSIUM CHANNEL MODULATORS 审中-公开
标题翻译：不对称苯并咪唑及其相关化合物作为钾通道调节剂
公开(公告)号：WO2005002503A2
公开(公告)日：2005-01-13
申请号：PCT/US2004/015155
申请日：2004-05-13
申请人： ICAGEN, INC. , WANG, Xiaodong , FULP, Alan, Bradley
发明人： WANG, Xiaodong , FULP, Alan, Bradley
IPC分类号： A61K
CPC分类号： C07D403/10 , C07D235/08 , C07D401/10 , C07D403/14 , C07D413/10 , C07D413/14 , C07D471/04 , C07D491/04
摘要： The present invention provides a genus of asymmetric benzimidazole compounds, methods and pharmaceutical compositions that are useful as modulators of potassium ion channels. The compounds of the invention are of use in both therapeutic and diagnostic methods.
摘要翻译：本发明提供了一类非对称苯并咪唑化合物，用作钾离子通道调节剂的方法和药物组合物。本发明的化合物可用于治疗和诊断方法。

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