Icagen, Inc.

Astellas Pharma Gmbh

Darrick Seconi

Xiaodong Wang

Alan Bradley Fulp

Brian Edward Marron

Kerry Leigh Spear

Takeshi Suzuki

Mark J Suto

Serge Beaudoin

Ayako Moritomo

Christopher John Markworth

Christopher William West

Shulan Zhou

Matthew Scott Johnson

Xiadong Wang

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.

Inhibitors of ion channels

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.

Sodium channel inhibitors

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.

Imines as ion channel modulators

The present invention provides a genus of polycyclic pyrazines of formula (I): wherein A and B are independently substituted or unsubstituted 5- or 6- membered heterocycloalkyl, or substituted or unsubstituted 5- or 6- membered heteroaryl, Wis Wis &#x2014;CH&#x2550;, &#x2014;NH&#x2014;, &#x2014;N&#x2550;, &#x2014;S&#x2014;, or &#x2014;O&#x2014;; Zis Zis &#x2014;CH&#x2550;, &#x2014;NH&#x2014;, &#x2014;N&#x2550;, &#x2014;S&#x2014;, or &#x2014;O&#x2014;; Y is a bond, &#x2014;CH&#x2550;N&#x2014;NH&#x2014;, &#x2014;NH&#x2014;CH, or &#x2014;NR&#x2014;; s and t are independently integers from 1 to 4; and the substituents R, R, Rand Rare as defined in the specification for compounds of formula (I). The polycyclic pyrazine compounds are useful as modulators of potassium ion channels in both therapeutic and diagnostic methods.

Polycyclic pyrazines as potassium ion channel modulators

The present invention provides a genus of polycyclic pyrimidines that are useful as modulators of potassium ion channels. The modulators of the invention are of use in both therapeutic and diagnostic methods.

Polycyclic pyrimidines as potassium ion channel modulators

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.

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Cary, NC, United States of America

Darrick Seconi