468741-16-4Relevant academic research and scientific papers
Balancing oral exposure with Cyp3A4 inhibition in benzimidazole-based IGF-IR inhibitors
Zimmermann, Kurt,Wittman, Mark D.,Saulnier, Mark G.,Velaparthi, Upender,Langley, David R.,Sang, Xiaopeng,Frennesson, David,Carboni, Joan,Li, Aixin,Greer, Ann,Gottardis, Marco,Attar, Ricardo M.,Yang, Zheng,Balimane, Praveen,Discenza, Lorell N.,Vyas, Dolatrai
scheme or table, p. 4075 - 4080 (2009/04/07)
3-(Benzimidazol-2-yl)-pyridine-2-one-based ATP competitive inhibitors of Insulin-like Growth Factor 1 Kinase (IGF-IR) were optimized for reduced Cyp3A4 inhibition and improved oral exposure. The use of malonate as methyl anion synthon via SNAr reaction and double decarboxylation under mild conditions is demonstrated.
Benzimidazole C-2 heterocycles as kinase inhibitors
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Page/Page column 16, (2010/02/11)
Benzimidazole derivatives having the general formula I are provided. These compounds are useful as tyrosine kinase inhibitors, especially for the treatment of cancer.
Novel tyrosine kinase inhibitors
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Page 31, (2010/11/30)
The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase enzymes thereby making them useful as anti-cancer agents. The formula I compounds are also useful for the treatment of other diseases which can be treated by inhibiting tyrosine kinase enzymes.
