Inhibitors of glycogen synthase 3 kinase

Schultz, Peter; Ring, David B; Harrison, Stephen D; Bray, Andrew M

Inhibitors of glycogen synthase 3 kinase

Patent · Fri Dec 31 23:00:00 EST 1999

OSTI ID:873412

Schultz, Peter ^[1]; Ring, David B ^[2]; Harrison, Stephen D ^[3]; Bray, Andrew M ^[4]

Oakland, CA
Palo Alto, CA
Berkeley, CA
Victoria, AU

Compounds of formula 1: ##STR1## wherein R.sub.1 is alkyl, cycloalkyl, aryl, aralkyl, heteroaryl, or heteroaralkyl, substituted with 0-3 substituents selected from lower alkyl, halo, hydroxy, lower alkoxy, amino, lower alkyl-amino, and nitro; R.sub.2 is hydroxy, amino, or lower alkoxy; R.sub.3 is H, lower alkyl, lower acyl, lower alkoxy-acyl, or amnino-acyl; R.sub.4 is H or lower alkyl; and pharmaceutically acceptable salts and esters thereof; are effective inhibitors of GSK3.

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Research Organization:: Lawrence Berkeley National Laboratory (LBNL), Berkeley, CA

DOE Contract Number:: AC03-76SF00098

Assignee:: Chiron Corporation (Emeryville, CA)

Patent Number(s):: US 6153618

OSTI ID:: 873412

Country of Publication:: United States

Language:: English

References (19)

Networking with proline-directed protein kinases implicated in Tau phosphorylation Pelech, Steven L. Neurobiology of Aging, Vol. 16, Issue 3 https://doi.org/10.1016/0197-4580(94)00187-6	journal	May 1995
Stimulation of MAP kinase by v- raf transformation of fibroblasts fails to induce hyperphosphorylation of transfected tau Latimer, Donna A.; Gallo, Jean-Marc; Lovestone, Simon FEBS Letters, Vol. 365, Issue 1 https://doi.org/10.1016/0014-5793(95)00434-B	journal	May 1995
A molecular mechanism for the effect of lithium on development. Klein, P. S.; Melton, D. A. Proceedings of the National Academy of Sciences, Vol. 93, Issue 16 https://doi.org/10.1073/pnas.93.16.8455	journal	August 1996
Exposure of rat hippocampal neurons to amyloid β peptide (25–35) induces the inactivation of phosphatidyl inositol-3 kinase and the activation of tau protein kinase I/glycogen synthase kinase-3β Takashima, Akihiko; Noguchi, Kaori; Michel, Gilles Neuroscience Letters, Vol. 203, Issue 1 https://doi.org/10.1016/0304-3940(95)12257-5	journal	January 1996
Identification of the glycogenic compound 5-iodotubercidin as a general protein kinase inhibitor Massillon, D.; Stalmans, W.; van de Werve, G. Biochemical Journal, Vol. 299, Issue 1 https://doi.org/10.1042/bj2990123	journal	April 1994
Intercellular Signaling: A kinase for cell-fate determination? Briscoe, Celia; Firtel, Richard A. Current Biology, Vol. 5, Issue 3 https://doi.org/10.1016/S0960-9822(95)00045-5	journal	March 1995
Glycogen synthase kinase-3β phosphorylates tau protein at multiple sites in intact cells Sperbera, Brian R.; Leight, Susan; Goedert, Michel Neuroscience Letters, Vol. 197, Issue 2 https://doi.org/10.1016/0304-3940(95)11902-9	journal	September 1995
Alzheimer's disease-like phosphorylation of the microtubule-associated protein tau by glycogen synthase kinase-3 in transfected mammalian cells Lovestone, Simon; Reynolds, C. Hugh; Latimer, Donna Current Biology, Vol. 4, Issue 12 https://doi.org/10.1016/S0960-9822(00)00246-3	journal	December 1994
Book review Golub, Mari S. Toxicology, Vol. 121, Issue 2 https://doi.org/10.1016/S0300-483X(97)00058-9	journal	August 1997
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/514/999/
0-3
acceptable
acceptable salt
acyl
alkoxy
alkoxy-acyl
alkyl
alkyl-amino
amino
amnino-acyl
aralkyl
aryl
compounds
cycloalkyl
effective
esters
formula
glycogen
gsk3
halo
heteroaralkyl
heteroaryl
hydroxy
inhibitors
kinase
nitro
pharmaceutically
pharmaceutically acceptable
salts
selected
str1
substituents
substituents selected
substituted
synthase

Inhibitors of glycogen synthase 3 kinase

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References (19)

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