Cycloalkyl—containing 5-acylindolinones, the...

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

Reexamination Certificate

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C514S326000, C514S418000, C546S187000, C548S486000

Reexamination Certificate

active

11077355

ABSTRACT:
The present invention relates to cycloalkyl-containing 5-acylindolinones of general formulawherein R1to R3are defined as in claims1to6, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on protein kinases, particularly an inhibiting effect on the activity of glycogen synthase kinase (GSK-3).

REFERENCES:
patent: 7176231 (2007-02-01), Heckel et al.
patent: WO 01/27080 (2001-04-01), None
Bramson, H. N., et al. “Oxindole-based Inhibitors of Cyclin-Dependent Kinase 2 (CDK2): Design, Synthesis, Enzymatic Activities, and X-ray Crystallographic Analysis”, Journal of Medicinal Chemistry, vol. 44, p. 4339-4358, 2001 XP002274118.
Embi, et al. “Glycogen Synthase Kinase-3 from Rabbit Skeletal Muscle: Separation from Cyclic-AMP-Dependent Protein Kinase and Phosphorylase Kinase”, Eur. J. Bio. Chem. vol. 107, pp. 519-527, 1980.
S. Nikoulina, et al. “Potential Role of Glycogen Synthase kinase-3 in Skeletal Muscle Insulin Resistance of Type 2 Diabetes” Diabetes, vol. 49, pp. 263-271, 2000.
Cohen, et al. Nature Reviews: Molecular Cellular Biology, vol. 2, 1-8, 2001.
Cross, et al. “Selective small-molecule inhibitors of glycogen synthase kinase-3 activity protect primary neurones from death”, J. Neurochemistry, vol. 77, pp. 94-102, 2001.
Sato, N., et al. “Maintenance of Pluripotency in human and mouse embryonic stem cells through activation of Wnt signaling by a pharmacological GSK-3-specific inhibitor”, Nature Medicine, vol. 10, pp. 55-63, 2004.

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