854638-56-5Relevant articles and documents
Optimisation of ITK inhibitors through successive iterative design cycles
Herdemann, Matthias,Weber, Alexander,Jonveaux, Jér?me,Schwoebel, Frank,Stoeck, Michael,Heit, Isabelle
scheme or table, p. 1852 - 1856 (2011/05/05)
Based on a hit cluster of compounds inhibiting interleukin-2 inducible T-cell kinase (ITK) in the submicromolar range a series of ITK inhibitor libraries were synthesized. Through iterative design cycles including kinase crystal structure information, indolylindazole libraries were identified which showed low nanomolar activity in enzymatic and cellular assays. The potential of these novel lead series was confirmed through in vivo tests in an anti-CD3-IL2 mouse model. The intravenous administration of highly potent ITK inhibitor 11o resulted in dose-dependent, efficient suppression of IL-2.
Novel pyridazinone derivatives as inhibitors of CDK2
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Page/Page column 34, (2008/06/13)
The present invention relates to compounds according to the general formula (I), with the definitions of the substituents X, R1 and R2 given below in the text, as well as their physiologically acceptable salts, methods for producing these compounds and their use as pharmaceuticals. These compounds are kinase inhibitors, in particular inhibitors of the kinase CDK2 (cyclin-dependent kinase 2)