Inhibitors of glycogen synthase 3 kinase
Abstract
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.
- Inventors:
-
- Oakland, CA
- Palo Alto, CA
- Berkeley, CA
- Victoria, AU
- Issue Date:
- Research Org.:
- Lawrence Berkeley National Laboratory (LBNL), Berkeley, CA (United States)
- OSTI Identifier:
- 873412
- Patent Number(s):
- 6153618
- Assignee:
- Chiron Corporation (Emeryville, CA)
- Patent Classifications (CPCs):
-
A - HUMAN NECESSITIES A61 - MEDICAL OR VETERINARY SCIENCE A61P - SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
C - CHEMISTRY C07 - ORGANIC CHEMISTRY C07D - HETEROCYCLIC COMPOUNDS
- DOE Contract Number:
- AC03-76SF00098
- Resource Type:
- Patent
- Country of Publication:
- United States
- Language:
- English
- Subject:
- inhibitors; glycogen; synthase; kinase; compounds; formula; str1; alkyl; cycloalkyl; aryl; aralkyl; heteroaryl; heteroaralkyl; substituted; 0-3; substituents; selected; halo; hydroxy; alkoxy; amino; alkyl-amino; nitro; acyl; alkoxy-acyl; amnino-acyl; pharmaceutically; acceptable; salts; esters; effective; gsk3; substituents selected; pharmaceutically acceptable; acceptable salt; /514/999/
Citation Formats
Schultz, Peter, Ring, David B, Harrison, Stephen D, and Bray, Andrew M. Inhibitors of glycogen synthase 3 kinase. United States: N. p., 2000.
Web.
Schultz, Peter, Ring, David B, Harrison, Stephen D, & Bray, Andrew M. Inhibitors of glycogen synthase 3 kinase. United States.
Schultz, Peter, Ring, David B, Harrison, Stephen D, and Bray, Andrew M. Sat .
"Inhibitors of glycogen synthase 3 kinase". United States. https://www.osti.gov/servlets/purl/873412.
@article{osti_873412,
title = {Inhibitors of glycogen synthase 3 kinase},
author = {Schultz, Peter and Ring, David B and Harrison, Stephen D and Bray, Andrew M},
abstractNote = {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.},
doi = {},
journal = {},
number = ,
volume = ,
place = {United States},
year = {Sat Jan 01 00:00:00 EST 2000},
month = {Sat Jan 01 00:00:00 EST 2000}
}
Save to My Library
You must Sign In or Create an Account in order to save documents to your library.
Works referenced in this record:
Lithium inhibits glycogen synthase kinase-3 activity and mimics Wingless signalling in intact cells
journal, December 1996
- Stambolic, Vuk; Ruel, Laurent; Woodgett, James R.
- Current Biology, Vol. 6, Issue 12
Stimulation of MAP kinase by v- raf transformation of fibroblasts fails to induce hyperphosphorylation of transfected tau
journal, May 1995
- Latimer, Donna A.; Gallo, Jean-Marc; Lovestone, Simon
- FEBS Letters, Vol. 365, Issue 1
Tau protein kinase I is essential for amyloid beta-protein-induced neurotoxicity.
journal, August 1993
- Takashima, A.; Noguchi, K.; Sato, K.
- Proceedings of the National Academy of Sciences, Vol. 90, Issue 16
Cytokinin-Derived Cyclin-Dependent Kinase Inhibitors: Synthesis and cdc2 Inhibitory Activity of Olomoucine and Related Compounds
journal, February 1997
- Havlíček, Libor; Hanuš, Jan; Veselý, Jaroslav
- Journal of Medicinal Chemistry, Vol. 40, Issue 4
Amyloid β peptide induces cytoplasmic accumulation of amyloid protein precursor via tau protein kinase I/glycogen synthase kinase-3β in rat hippocampal neurons
journal, September 1995
- Takashima, Akihiko; Yamaguchi, Haruyasu; Noguchi, Kaori
- Neuroscience Letters, Vol. 198, Issue 2
Intercellular Signaling: A kinase for cell-fate determination?
journal, March 1995
- Briscoe, Celia; Firtel, Richard A.
- Current Biology, Vol. 5, Issue 3
GSK3: a SHAGGY frog story
journal, July 1996
- Welsh, Gavin I.; Wilson, Clive; Proud, Christopher G.
- Trends in Cell Biology, Vol. 6, Issue 7
Identification of the glycogenic compound 5-iodotubercidin as a general protein kinase inhibitor
journal, April 1994
- Massillon, D.; Stalmans, W.; van de Werve, G.
- Biochemical Journal, Vol. 299, Issue 1
Networking with proline-directed protein kinases implicated in Tau phosphorylation
journal, May 1995
- Pelech, Steven L.
- Neurobiology of Aging, Vol. 16, Issue 3
Glycogen synthase kinase-3β phosphorylates tau protein at multiple sites in intact cells
journal, September 1995
- Sperbera, Brian R.; Leight, Susan; Goedert, Michel
- Neuroscience Letters, Vol. 197, Issue 2
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
journal, January 1996
- Takashima, Akihiko; Noguchi, Kaori; Michel, Gilles
- Neuroscience Letters, Vol. 203, Issue 1
Inhibition of Cyclin-Dependent Kinases by Purine Analogues
journal, September 1994
- Vesely, Jaroslav; Havlicek, Libor; Strnad, Miroslav
- European Journal of Biochemistry, Vol. 224, Issue 2
A molecular mechanism for the effect of lithium on development.
journal, August 1996
- Klein, P. S.; Melton, D. A.
- Proceedings of the National Academy of Sciences, Vol. 93, Issue 16
Inactivation of glycogen synthase kinase-3β by phosphorylation: new kinase connections in insulin and growth-factor signalling
journal, November 1993
- Sutherland, C.; Leighton, I. A.; Cohen, P.
- Biochemical Journal, Vol. 296, Issue 1
A Structure-Based Library Approach to Kinase Inhibitors
journal, January 1996
- Norman, Thea C.; Gray, Nathanael S.; Koh, John T.
- Journal of the American Chemical Society, Vol. 118, Issue 31
Alzheimer's disease-like phosphorylation of the microtubule-associated protein tau by glycogen synthase kinase-3 in transfected mammalian cells
journal, December 1994
- Lovestone, Simon; Reynolds, C. Hugh; Latimer, Donna
- Current Biology, Vol. 4, Issue 12
Modulation of PHF-like tau phosphorylation in cultured neurones and transfected cells
journal, May 1995
- Anderton, B. H.; Brion, J. -P.; Couck, A-M.
- Neurobiology of Aging, Vol. 16, Issue 3
Inhibition of Glycogen Synthase Kinase-3 by Insulin in Cultured Human Skeletal Muscle Myoblasts
journal, May 1995
- Borthwick, A. C.; Wells, A. M.; Rochford, J. J.
- Biochemical and Biophysical Research Communications, Vol. 210, Issue 3