431062-01-0Relevant academic research and scientific papers
Design and synthesis of piperazine-indole p38α MAP kinase inhibitors with improved pharmacokinetic profiles
Tan, Xuefei,Tester, Richland W.,Luedtke, Gregory R.,Chakravarty, Sarvajit,Mavunkel, Babu J.,Perumattam, John J.,Lu, Qing,Nashashibi, Imad,Jung, Joon,Hu, Jie,Liclican, Albert,Almirez, Ramona,Tabora, Jocelyn,Tran, Vinh,Laney, Maureen,Levy, Daniel E.,Dugar, Sundeep
scheme or table, p. 828 - 831 (2010/06/13)
Derivatives of the 4-fluorobenzyl dimethylpiperazine-indole class of p38α MAP kinase inhibitors are described. Biological evaluation of these compounds focused on maintaining activity while improving pharmacokinetic (PK) properties. Improved properties were observed for structures bearing substitutions on the benzylic methylene.
Indole-type derivatives as inhibitors of p38 kinase
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Page/Page column 44, (2008/06/13)
The invention is directed to methods to inhibit p38-α kinase using compounds comprising a phenyl or thienyl coupled through a piperidine or piperazine nucleus to an indole residue wherein the indole residue mandatorily has a substituent on the ring nitrogen which is an amino or substituted amino group.
