About: Pyrazolopyrimidines as cyclin-dependent kinase inhibitors     Goto   Sponge   NotDistinct   Permalink

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  • The title compds. pyrazolo[1,5-a]pyrimidines [I R = H, alkyl, cycloalkyl, etc.; R2 = alkyl, halo, aryl, etc.; R3 = H, halo, aryl, etc.; R4 = H, halo, alkyl], useful as inhibitors of cyclin dependent kinases for treatment, prevention, inhibition, or amelioration of one or more diseases assocd. with the CDKs such as cancer, were prepd. Thus, reacting II (prepn. given) with 4-aminomethylpyridine afforded 93% III which showed IC50 of 0.020 .mu.M and 0.029 .mu.M against CDK2 kinase (cyclin A or cyclin E-dependent). The pharmaceutical compn. comprising the compd. I is claimed.
  • The title compds. pyrazolo[1,5-a]pyrimidines [I R = H, alkyl, cycloalkyl, etc.; R2 = alkyl, halo, aryl, etc.; R3 = H, halo, aryl, etc.; R4 = H, halo, alkyl], useful as inhibitors of cyclin dependent kinases for treatment, prevention, inhibition, or amelioration of one or more diseases assocd. with the CDKs such as cancer, were prepd. Thus, reacting II (prepn. given) with 4-aminomethylpyridine afforded 93% III which showed IC50 of 0.020 .mu.M and 0.029 .mu.M against CDK2 kinase (cyclin A or cyclin E-dependent). The pharmaceutical compn. comprising the compd. I is claimed. (en)
Title
  • Pyrazolopyrimidines as cyclin-dependent kinase inhibitors
  • Pyrazolopyrimidines as cyclin-dependent kinase inhibitors (en)
skos:prefLabel
  • Pyrazolopyrimidines as cyclin-dependent kinase inhibitors
  • Pyrazolopyrimidines as cyclin-dependent kinase inhibitors (en)
skos:notation
  • RIV/00216224:14310/04:00035987!RIV10-MSM-14310___
http://linked.open...tracePatentuVzoru
http://linked.open...avai/riv/aktivita
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  • N
http://linked.open...cisloPatentuVzoru
  • US 2004/209878 A1
http://linked.open...eleniPatentuVzoru
http://linked.open...vai/riv/dodaniDat
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  • 583275
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  • RIV/00216224:14310/04:00035987
http://linked.open...riv/jazykVysledku
http://linked.open.../riv/klicovaSlova
  • cyclin dependent kinase; inhibitor; pyrazolopyrimidine (en)
http://linked.open.../riv/klicoveSlovo
http://linked.open...ontrolniKodProRIV
  • [727FD9C0A3D6]
http://linked.open.../licencniPoplatek
http://linked.open...ydaniPatentuVzoru
  • USA
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  • United States Patent and Trademark Office
http://linked.open...in/vavai/riv/obor
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  • Alvarez, Carmen
  • Dwyer, Michael
  • Fischmann, Thierry
  • Guzi, Timothy
  • Madison, Vincent
  • Paruch, Kamil
  • Chan, Tin-Yau
  • Doll, Ronald
  • James, Ray
  • Paradkar, Vidyadhar
  • Park, Haengsoon
  • Rivera, Jocelyn
  • Girijavallabhan, Viyyoor
  • Mallams, Alan
  • Keertikar, Kartik
  • Dillard, Lawrence
  • Tran, Vinh
  • Hobbs, Douglas
  • Zhen, Min
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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