Pyrazolopyrimidines as Protein Kinase Inhibitors

P 2006

Pyrazolopyrimidines as Protein Kinase Inhibitors

PARUCH, Kamil, Timothy GUZI, Michael DWYER a Gerald SHIPPS

Základní údaje

Originální název

Pyrazolopyrimidines as Protein Kinase Inhibitors

Název česky

Pyrazolopyrimidines as Protein Kinase Inhibitors

Autoři

PARUCH, Kamil, Timothy GUZI, Michael DWYER a Gerald SHIPPS

Vydání

Číslo: US 2006/094706 A1, Vydavatel: United States Patent and Trademark Office, Místo vydání: USA, Název vlastníka: Schering-Plough, 2006

Další údaje

Jazyk

angličtina

Typ výsledku

Patent

Obor

30200 3.2 Clinical medicine

Stát vydavatele

Spojené státy

Utajení

není předmětem státního či obchodního tajemství

Organizační jednotka

Přírodovědecká fakulta

Klíčová slova česky

HCV; checkpoint kinase; CDK2

Klíčová slova anglicky

HCV; checkpoint kinase; CDK2

Štítky

CDK2, checkpoint kinase, HCV

Změněno: 25. 6. 2009 15:06, doc. Mgr. Kamil Paruch, Ph.D.

Anotace

ORIG CZ

V originále

The invention provides a novel class of pyrazolopyrimidines I [R2 = halo; R3 = satd. or partially unsatd. heterocyclyl radical; R4 = H, halo, haloalkyl, aryl, etc.] as inhibitors of protein and/or checkpoint kinases, methods of prepg. such compds., pharmaceutical compns. including one or more such compds., methods of prepg. pharmaceutical formulations including one or more such compds., and methods of treatment, prevention, inhibition, or amelioration of one or more diseases assocd. with the protein or checkpoint kinases using such compds. or pharmaceutical compns. E.g., a multi-step synthesis of II, startting from 3-aminopyrazole and Et 2-ethylacetoacetate, was given. II showed IC50 of 0.1 .mu.M against CDK2 kinase. The invention also relates to the inhibition of hepatitis C virus (HCV) replication. In particular, embodiments of the invention provide compds. III [G1 = OH, cyano, CO2H, etc.; G2 and G3 = alkyl, cycloalkyl, aryl, etc.] and methods for inhibiting HCV RNA-dependent RNA polymerase enzymic activity. The compds. III inhibited HCV RNA-dependent RNA polymerase (RdRp) at the concn. from >10 to <1 .mu.M. The invention also provides compns. and methods for the prophylaxis and treatment of HCV infection.

Česky

viz Anotace

Citovat

PARUCH, Kamil, Timothy GUZI, Michael DWYER a Gerald SHIPPS. Pyrazolopyrimidines as Protein Kinase Inhibitors. 2006. Patent. Číslo: US 2006/094706 A1. Vydavatel: United States Patent and Trademark Office. Místo vydání: USA. Název vlastníka: Schering-Plough. Datum registrace: 6. 10. 2005. Datum přijetí: 4. 5. 2006.

@misc{838354,
   author = {Paruch, Kamil and Guzi, Timothy and Dwyer, Michael and Shipps, Gerald},
   keywords = {HCV; checkpoint kinase; CDK2},
   language = {eng},
   title = {Pyrazolopyrimidines as Protein Kinase Inhibitors},
   year = {2006}
}

TY  - PAT
ID  - 838354
AU  - Paruch, Kamil - Guzi, Timothy - Dwyer, Michael - Shipps, Gerald
PY  - 2006
TI  - Pyrazolopyrimidines as Protein Kinase Inhibitors
KW  - HCV
KW  - checkpoint kinase
KW  - CDK2
N2  - The invention provides a novel class of pyrazolopyrimidines I [R2 = halo; R3 = satd. or partially unsatd. heterocyclyl radical; R4 = H, halo, haloalkyl, aryl, etc.] as inhibitors of protein and/or checkpoint kinases, methods of prepg. such compds., pharmaceutical compns. including one or more such compds., methods of prepg. pharmaceutical formulations including one or more such compds., and methods of treatment, prevention, inhibition, or amelioration of one or more diseases assocd. with the protein or checkpoint kinases using such compds. or pharmaceutical compns. E.g., a multi-step synthesis of II, startting from 3-aminopyrazole and Et 2-ethylacetoacetate, was given. II showed IC50 of 0.1 .mu.M against CDK2 kinase. The invention also relates to the inhibition of hepatitis C virus (HCV) replication. In particular, embodiments of the invention provide compds. III [G1 = OH, cyano, CO2H, etc.; G2 and G3 = alkyl, cycloalkyl, aryl, etc.] and methods for inhibiting HCV RNA-dependent RNA polymerase enzymic activity. The compds. III inhibited HCV RNA-dependent RNA polymerase (RdRp) at the concn. from >10 to <1 .mu.M. The invention also provides compns. and methods for the prophylaxis and treatment of HCV infection.
ER  -

PARUCH, Kamil, Timothy GUZI, Michael DWYER a Gerald SHIPPS. \textit{Pyrazolopyrimidines as Protein Kinase Inhibitors}. 2006. Patent. Číslo: US 2006/094706 A1. Vydavatel: United States Patent and Trademark Office. Místo vydání: USA. Název vlastníka: Schering-Plough. Datum registrace: 6. 10. 2005. Datum přijetí: 4. 5. 2006.

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