Hiroki Shimizu

Summary

Affiliation: Daiichi Sankyo Co
Country: Japan

Publications

  1. ncbi Discovery of imidazo[1,2-b]pyridazine derivatives as IKKbeta inhibitors. Part 1: Hit-to-lead study and structure-activity relationship
    Hiroki Shimizu
    R and D Division, Daiichi Sankyo Co, Ltd, Edogawa ku, Tokyo, Japan
    Bioorg Med Chem Lett 20:5113-8. 2010
  2. ncbi Discovery of imidazo[1,2-b]pyridazines as IKK? inhibitors. Part 2: improvement of potency in vitro and in vivo
    Hiroki Shimizu
    R and D Division, Daiichi Sankyo Co, Ltd, Edogawa ku, Tokyo, Japan
    Bioorg Med Chem Lett 21:904-8. 2011
  3. ncbi Discovery of imidazo[1,2-b]pyridazines as IKK? inhibitors. Part 3: exploration of effective compounds in arthritis models
    Hiroki Shimizu
    R and D Division, Daiichi Sankyo Co, Ltd, Tokyo, Japan
    Bioorg Med Chem Lett 21:4550-5. 2011

Detail Information

Publications3

  1. ncbi Discovery of imidazo[1,2-b]pyridazine derivatives as IKKbeta inhibitors. Part 1: Hit-to-lead study and structure-activity relationship
    Hiroki Shimizu
    R and D Division, Daiichi Sankyo Co, Ltd, Edogawa ku, Tokyo, Japan
    Bioorg Med Chem Lett 20:5113-8. 2010
    ..Also, these compounds showed high kinase selectivity. The structure-activity relationship was revealed and the interaction model of imidazo[1,2-b]pyridazine compounds with IKKbeta was constructed...
  2. ncbi Discovery of imidazo[1,2-b]pyridazines as IKK? inhibitors. Part 2: improvement of potency in vitro and in vivo
    Hiroki Shimizu
    R and D Division, Daiichi Sankyo Co, Ltd, Edogawa ku, Tokyo, Japan
    Bioorg Med Chem Lett 21:904-8. 2011
    ..Another is to increase the affinity for IKK? by the introduction of additional substituents based on the hypothesis derived from an interaction model study. These improved compounds showed inhibitory activity of TNF? production in mice...
  3. ncbi Discovery of imidazo[1,2-b]pyridazines as IKK? inhibitors. Part 3: exploration of effective compounds in arthritis models
    Hiroki Shimizu
    R and D Division, Daiichi Sankyo Co, Ltd, Tokyo, Japan
    Bioorg Med Chem Lett 21:4550-5. 2011
    ..The compound we have acquired, which had both potent activities and good pharmacokinetic profiles based on improved physicochemical properties, demonstrated efficacy on collagen-induced arthritis models in mice and rats...