Pim kinase inhibitors and their preparation method and application in pharmacy
摘要:
The present invention provides a PIM kinase inhibitor, having the formula The following compounds of formula I: The present invention also provides isomers of compounds of formula I, diastereomers thereof, enantiomers, tautomeric and salts thereof. In the above formula I E, J, Q, X, Y, Z, m are as defined in claim 1. PIM kinase activity by biochemical assays to test, compounds 1-63 were all significantly inhibit PIM kinase activity at a concentration of 3 micromolar activity of PIM-1 kinase inhibition rate are more than 50%, the highest It reached 100%. Compound embodiment also has considerable inhibition of the kinase activity of PM-3 and PIM-2. At 3 micromolar concentration of the compound, activity inhibition ratio PIM-2 PM-3 kinase, and up to 100%. Thus, the PIM kinase inhibitors of the present invention may be used for the treatment or prophylaxis of cancer, autoimmune diseases, allergic reactions or disease organ transplantation anti-rejection drug reactions. Greater clinical value. The present invention provides a preparation method.
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年份:
2012
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