September 16, 2013

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The following patent record is from the CAplusSM database.


Patent Number: WO 20133095761
Title: Preparation of imidazopyridine derivatives as PI3 kinase inhibitors
Inventor(s): Rivero, Ralph A.; Tedesco, Rosanna
Patent Assignee(s): Glaxosmithkline LLC, USA
Source: PCT Int. Appl., 67pp. CODEN: PIXXD2
Language: English

This invention relates to the use of imidazopyridine derivs. I [R1 = H, OH, CO2H; R2 = H, alkyl; R6 and R7 = alkyl, halo, CF3; or R6 and R7 combine with the ring to which they are attached to form naphthyl] for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3'OH kinase family (hereinafter PI3 kinases), suitably, PI3Ka, PI3Kd, PI3Kß, and/or PI3K?.  Eight compds. I were prepd. and formulated.  E.g., a multi-step synthesis of II, starting from 1H-imidazo[4,5-b]pyridine, was described.  Exemplified compds. I were tested and found to be inhibitors of PI3 kinases, particularly PI3Kß. The activities (IC50) of exemplified compds. range from about 1 nM to about 10 µM against PI3Kß.  Suitably, the present invention relates to the use of imidazopyridines I in the treatment of one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries.  More suitably, the present invention relates to PI3Kß selective imidazopyridine compds. for treating cancer.

Please note:  Abstracts and Titles for patent records in CAplus are routinely enhanced to better describe the claimed invention.

 View the full-text here.

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