The present invention is directed to the use of 2,4,5-trisubstituted imidazole compounds and compositions in the treatment of CNS injuries to the brain.
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(2008/06/13)
Use of kinase inhibitors for treating neurodegenerative diseases
The present invention relates to methods of treating neurodegenerative diseases, including but not limited to Parkinson's disease. In particular, the present invention provides methods utilizing the administration of pyridyl imidazoles having simultaneous inhibitory activity towards p38 mitogen-activated protein (MAP) kinase and c-jun-N-terminal kinase (JNK). The present invention also provides methods for preventing apoptosis of dopamine neurons using pyridyl imidazoles. The present invention also provides methods for the treatment of neurodegenerative diseases, including but not limited to Parkinson's disease.
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(2008/06/13)
Substituted imidazoles as glucagon receptor antagonists
A modestly active, nonselective triarylimidazole lead was optimized for binding affinity with the human glucagon receptor. This led to the identification of a 2- and/or 4-alkyl or alkyloxy substituent on the imidazole C4-aryl group as a structural determinant for significant enhancement in binding with the glucagon receptor (e.g., 41, IC50 = 0.053 μM) and selectivity (> 1000 ×) over p38 MAP kinase in this class of compounds.
Chang, Linda L.,Sidler, Kelly L.,Cascieri, Margaret A.,De Laszlo, Stephen,Koch, Greg,Li, Bing,MacCoss, Malcolm,Mantlo, Nathan,O'Keefe, Stephen,Pang, Margaret,Rolando, Anna,Hagmann, William K.
p. 2549 - 2553
(2007/10/03)
Pyrimidinyl imidazoles
Novel 2,4,5-triaryl imidazole compounds and compositions for use in therapy.
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(2008/06/13)
Pyridyl imidazoles
Novel 2,4,5-triaryl imidazole compounds and compositions for use in therapy.
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(2008/06/13)
Imidazole derivatives and their use as cytokine inhibitors
As cytokine inhibitors 2,4,5-triarylimidazole compounds and compositions for use as cytokine inhibitors.
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(2008/06/13)
Regulation of stress-induced cytokine production by pyridinylimidazoles inhibition of CSBP kinase
Members of three classes of pyridinylimidazoles bind with varying affinities to CSBP (p38) kinase which is a member of a stress-induced signal transduction pathway. Based upon SAR and protein homology modeling, the pharmacophore and three potential modes of binding to the enzyme are presented. For a subset of pyridinylimidazoles, binding is shown to correlate with inhibition of CSBP kinase activity, whereas no significant inhibition of PKA, PKα and ERK kinase activity is observed.
Gallagher, Timothy F.,Seibel, George L.,Kassis, Shouki,Laydon, Jeffrey T.,Blumenthal, Mary Jane,Lee, John C.,Lee, Dennis,Boehm, Jeffrey C.,Fier-Thompson, Susan M.,Abt, Jeffrey W.,Soreson, Margaret E.,Smietana, Juanita M.,Hall, Ralph F.,Garigipati, Ravi S.,Bender, Paul E.,Erhard, Karl F.,Krog, Arnold J.,Hofmann, Glenn A.,Sheldrake, Peter L.,McDonnell, Peter C.,Kumar, Sanjay,Young, Peter R.,Adams, Jerry L.
p. 49 - 64
(2007/10/03)
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