658700-03-9Relevant academic research and scientific papers
Hit-to-lead studies on benzimidazole inhibitors of ITK: Discovery of a novel class of kinase inhibitors
Snow, Roger J.,Abeywardane, Asitha,Campbell, Scot,Lord, John,Kashem, Mohammed A.,Khine, Hnin Hnin,King, Josephine,Kowalski, Jennifer A.,Pullen, Steven S.,Roma, Teresa,Roth, Gregory P.,Sarko, Christopher R.,Wilson, Noel S.,Winters, Michael P.,Wolak, John P.,Cywin, Charles L.
, p. 3660 - 3665 (2008/02/09)
Benzimidazole 1 was identified as a selective inhibitor of ITK by high throughput screening. Hit-to-lead studies defined the SAR at all three substituents. Reversing the amide linkage at C6 led to 16, with a fivefold improvement of potency. This enhanceme
SUBSTITUTED BENZIMIDAZOLE COMPOUNDS
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Page 151, (2008/06/13)
Disclosed are substituted benzimidazole compounds of formula (I) wherein R1, R2, R3, R4 and Xa are defined herein. The compounds of the invention inhibit Itk kinase and are therefore useful for treating diseases and pathological conditions involving inflammation, immunological disorders and allergic disorders. Also disclosed are processes for preparing these compounds and the pharmaceutical compositions comprising these compounds.
