Icagen, Inc.

Research Triangle Institute

Astellas Pharma Gmbh

Alan Bradley Fulp

Xiaodong Wang

Darrick Seconi

Brian Edward Marron

Kerry Leigh Spear

Mark J Suto

Yanan Zhang

Rangan Maitra

Herbert H Seltzman

Takeshi Suzuki

Takahiro Ishii

Serge Beaudoin

Ayako Moritomo

Albert Michiel Van Rhee

Christopher John Markworth

Christopher William West

Shulan Zhou

Matthew Scott Johnson

Xiadong Wang

The invention provides compounds capable of acting as antagonists at cannabanoid receptors according to the following formula: Such compounds may be used to treat conditions for which the cannabinoid receptor system has been implicated, such as obesity, liver disease, diabetes, pain, and inflammation.

Peripherally restricted diphenyl purine derivatives

The invention provides compounds capable of acting as antagonists at cannabanoid receptors according to the following formula: Such compounds may be used to treat conditions for which the cannabinoid receptor system has been implicated, such as obesity, liver disease, diabetes, pain, and inflammation. 

Pyrazole derivatives as cannabinoid receptor 1 antagonists

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

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.

The present invention provides a genus of asymmetric benzimidazole compounds, methods and pharmaceut1cal compositions that are useful as modulators of potassium ion channels. The compounds of the invention are of use in both therapeutic and diagnostic methods.

Asymmetric benzimidazoles and related compounds as potassium channel modulators

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 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.

Bis-benzimidazoles and related compounds as potassium 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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Willow Spring, NC, United States of America

Alan Bradley Fulp