658700-07-3Relevant academic research and scientific papers
NOVEL UREA DERIVATIVES AS TEC KINASE INHIBITORS AND USES THEREOF
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Page/Page column 39; 51, (2013/03/26)
Provided are urea compounds of formula (I) as Tec kinase inhibitors, in particular ITK (interleukin-2 inducible tyrosine kinase) inhibitors. Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders mediated by ITK.
Discovery, SAR and X-ray structure of 1H-benzimidazole-5-carboxylic acid cyclohexyl-methyl-amides as inhibitors of inducible T-cell kinase (Itk)
Moriarty, Kevin J.,Takahashi, Hidenori,Pullen, Steven S.,Khine, Hnin Hnin,Sallati, Rosemarie H.,Raymond, Ernest L.,Woska Jr., Joseph R.,Jeanfavre, Deborah D.,Roth, Gregory P.,Winters, Michael P.,Qiao, Lei,Ryan, Declan,DesJarlais, Renee,Robinson, Darius,Wilson, Matthew,Bobko, Mark,Cook, Brian N.,Lo, Ho Yin,Nemoto, Peter A.,Kashem, Mohammed A.,Wolak, John P.,White, André,Magolda, Ronald L.,Tomczuk, Bruce
scheme or table, p. 5545 - 5549 (2009/06/18)
A series of novel potent benzimidazole based inhibitors of interleukin-2 T-cell kinase (Itk) were prepared. In this report, we discuss the structure-activity relationship (SAR), selectivity, and cell-based activity for the series. We also discuss the SAR associated with an X-ray structure of one of the small-molecule inhibitors bound to ITK.
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 153, (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.
