529505-85-9Relevant academic research and scientific papers
NEW BENZIMIDAZOLES DERIVATIVES AS TEC KINASES FAMILY INHIBITORS
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Page/Page column 94; 95, (2017/04/11)
The present invention relates to a novel family of covalent kinases inhibitors. Compounds of this class have been found to have inhibitory activity against members of the Tec kinase family, particularly ITK, BTK, BMX, Tec and/or RLK. The present invention is directed to a compound of Formula I or pharmaceutically acceptable salt, solvate, solvate of salt, stereoisomer, tautomer, isotope, prodrug, complex or biologically active metabolite thereof, and its use in therapy.
HETEROCYCLIC AMIDES AS ITK INHIBITORS
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Page/Page column 61; 63, (2014/03/21)
The present invention is directed to heterocyclic amide 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,
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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, (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 are useful for treating diseases and pathological cond
