608142-93-4Relevant articles and documents
Structure guided optimization, in vitro activity, and in vivo activity of pan-PIM kinase inhibitors
Burger, Matthew T.,Han, Wooseok,Lan, Jiong,Nishiguchi, Gisele,Bellamacina, Cornelia,Lindval, Mika,Atallah, Gordana,Ding, Yu,Mathur, Michelle,Mcbride, Chris,Beans, Elizabeth L.,Muller, Kristine,Tamez, Victoriano,Zhang, Yanchen,Huh, Kay,Feucht, Paul,Zavorotinskaya, Tatiana,Dai, Yumin,Holash, Jocelyn,Castillo, Joseph,Langowski, John,Wang, Yingyun,Chen, Min Y.,Garcia, Pablo D.
supporting information, p. 1193 - 1197 (2014/01/06)
Proviral insertion of Moloney virus (PIM) 1, 2, and 3 kinases are serine/threonine kinases that normally function in survival and proliferation of hematopoietic cells. As high expression of PIM1, 2, and 3 is frequently observed in many human malignancies, including multiple myeloma, non-Hodgkins lymphoma, and myeloid leukemias, there is interest in determining whether selective PIM inhibition can improve outcomes of these human cancers. Herein, we describe our efforts toward this goal. The structure guided optimization of a singleton high throughput screening hit in which the potency against all three PIM isoforms was increased >10,000-fold to yield compounds with pan PIM Kis 10 pM, nanomolar cellular potency, and in vivo activity in an acute myeloid leukemia Pim-dependent tumor model is described.
BICYCLIC PYRIDAZINE COMPOUNDS AS PIM INHIBITORS
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Page/Page column 59; 60, (2012/11/13)
The invention relates to bicyclic compounds of formulas I and I', and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of Pim-1 and/or Pim-2, and/or Pim-3 protein kinase activity or enzyme function. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein, and their use in the prevention and treatment of Pim kinase related conditions and diseases, preferably cancer.
HETEROCYCLIC AMIDE COMPOUNDS AS PROTEIN KINASE INHIBITORS
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Page/Page column 66-67, (2009/03/07)
The present invention related to novel heterocyclic amide compounds of Formula 1: as disclosed herein or a pharmaceutically accept able salt, solvate, ester, prodrug or stereoisomer thereof. Also disclosedare compositions comprising said compounds, and methods for using said compounds for treating or preventing a proliferative disease, an anti-proliferative disorder, inflammation, arthritis, a neurological or neurodenerative disease, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral disease or a fungal disease