About: Imidazopyridines as Cyclin Dependent Kinase Inhibitors     Goto   Sponge   NotDistinct   Permalink

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  • In its many embodiments, the present invention provides a novel class of imidazo[1,2-a]pyridine compds. I [R = (un)substituted-alkyl, -aryl, -heteroaryl, -heterocyclyl, etc.; R1 = H, alkyl or aryl; R2 = H, (un)substituted-alkyl, -aryl, arylalkyl, alkenyl, etc.; R3 = H, halo, CF3, (un)substituted-alkyl, -aryl, etc.; R4 = H, halo, CF3, (un)substituted-alkyl, -cycloalkyl, etc.] as inhibitors of cyclin dependent kinases, methods of prepg. such compds., pharmaceutical compns. contg. one or more such compds., methods of prepg. pharmaceutical formulations comprising one or more such compds., and methods of treatment, prevention, inhibition, or amelioration of one or more diseases assocd. with the CDKs using such compds. or pharmaceutical compns. Thus, e.g., II was made by condensation of 8-amino-3-bromo-6-phenylimidazopyridine (prepn. given) with 5-formylpyrimidine. In inhibition assays with CDK2, I possessed excellent inhibitory properties, e.g., II possessed an IC50 value of 0.12 uM.
  • In its many embodiments, the present invention provides a novel class of imidazo[1,2-a]pyridine compds. I [R = (un)substituted-alkyl, -aryl, -heteroaryl, -heterocyclyl, etc.; R1 = H, alkyl or aryl; R2 = H, (un)substituted-alkyl, -aryl, arylalkyl, alkenyl, etc.; R3 = H, halo, CF3, (un)substituted-alkyl, -aryl, etc.; R4 = H, halo, CF3, (un)substituted-alkyl, -cycloalkyl, etc.] as inhibitors of cyclin dependent kinases, methods of prepg. such compds., pharmaceutical compns. contg. one or more such compds., methods of prepg. pharmaceutical formulations comprising one or more such compds., and methods of treatment, prevention, inhibition, or amelioration of one or more diseases assocd. with the CDKs using such compds. or pharmaceutical compns. Thus, e.g., II was made by condensation of 8-amino-3-bromo-6-phenylimidazopyridine (prepn. given) with 5-formylpyrimidine. In inhibition assays with CDK2, I possessed excellent inhibitory properties, e.g., II possessed an IC50 value of 0.12 uM. (en)
Title
  • Imidazopyridines as Cyclin Dependent Kinase Inhibitors
  • Imidazopyridines as Cyclin Dependent Kinase Inhibitors (en)
skos:prefLabel
  • Imidazopyridines as Cyclin Dependent Kinase Inhibitors
  • Imidazopyridines as Cyclin Dependent Kinase Inhibitors (en)
skos:notation
  • RIV/00216224:14310/04:00035992!RIV10-MSM-14310___
http://linked.open...tracePatentuVzoru
http://linked.open...avai/riv/aktivita
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  • N
http://linked.open...cisloPatentuVzoru
  • WO 2004/026867 A2
http://linked.open...eleniPatentuVzoru
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  • 567312
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  • RIV/00216224:14310/04:00035992
http://linked.open...riv/jazykVysledku
http://linked.open.../riv/klicovaSlova
  • cyclin dependent kinase; ínhibitors; pyrazolopyridine (en)
http://linked.open.../riv/klicoveSlovo
http://linked.open...ontrolniKodProRIV
  • [A6803A88E2E8]
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  • USA
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  • World Intellectual Property Organization
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  • Dwyer, Michael
  • Guzi, Timothy
  • Paruch, Kamil
  • Doll, Ronald
  • Girijavallabhan, Viyyoor
  • Keertikar, Kartik
http://linked.open...mniOchranaPatentu
http://linked.open...avai/riv/vlastnik
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  • Schering-Plough
http://localhost/t...ganizacniJednotka
  • 14310
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