Glycogen synthase kinase-3 inhibitors

Details Glycogen synthase kinase-3 inhibitors Glycogen synthase kinase-3 inhibitors

2003-12-11

2008-11-04

Russel, Jeffery E (Department: 1654)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

C530S327000, C530S328000, C530S345000

Reexamination Certificate

active

07446092

ABSTRACT:
Novel conjugates that are capable of inhibiting GSK-3 activity, a process of producing same, pharmaceutical compositions including same and methods of using same in the treatment of GSK-3 mediated conditions are disclosed. Methods of treating affective disorders using GSK-3 inhibitors are further disclosed.

REFERENCES:
patent: 1471621 (1923-10-01), McCord
patent: 2046068 (1936-06-01), Gray
patent: 3193159 (1965-07-01), Swindler
patent: 4186646 (1980-02-01), Martin
patent: 5462101 (1995-10-01), Mouchmouchian
patent: 6057117 (2000-05-01), Harrison et al.
patent: 6153618 (2000-11-01), Schultz et al.
patent: WO 95/01376 (1995-01-01), None
patent: WO 97/33601 (1997-09-01), None
patent: WO 97/41854 (1997-11-01), None
patent: WO 98/16528 (1998-04-01), None
patent: WO 00/45237 (2000-03-01), None
patent: WO 00/59206 (2000-05-01), None
patent: WO 00/74663 (2000-12-01), None
patent: WO 01/49709 (2001-07-01), None
patent: WO 02/24941 (2002-03-01), None
patent: WO 2005/000192 (2005-06-01), None
Taniguchi et al. Myristoylated Alanine-rich C Kinase Substrate . . . The Journal of Biological Chemistry. Jul. 15, 1994, vol. 269, No. 28, pp. 18299-18302.
Manenti et al. Affinity Purificatiion and Characterization of Myristoylated . . . The Journal Of Biological Chemistry. Nov. 5, 1992, vol. 267, No. 31, pp. 22310-22315.
Donella-Deana et al. “Dephosphorylation of Phosphopeptides by Colcineurin (Protein Phosphatase 2B)”, Eur. J. Biochem., 219(1-2): 109-117, 1994. Tab.1,2.
Otaka et al. “Synthesis and Application of N-Box-L-2-Amino-4-(Diethylphosphono)-4-,4-Difluorobutanoic Acid for Solid-Phase Synthesis of Nonhydrolyzable Phosphoserine Peptide Analogues”, Tetrahedron. Lett., 36(6): 927-930, 1995.
Othaka et al. “Development of New Methodology for the Synthesis of Functionalized α-Fluorophosphonates and Its Practical Application to the Preparation of Phosphopeptide Mimetics”, Chem. Commun., 12: 1081-1082, 2000.
Pap et al. “Role of Glycogen Synthase Kinase-3 in the Phosphatidylinositol 3-Kinase/Akt Cell Survival Pathway”, J. Biol. Chem., 273: 19929-19932, 1998.
Phiel “Molecular Targets of Lithium Action”, Annu. Rev. Pharmacol. Toxicology, 41: 789-813, 2001.
Barrett et al. “Proteinase Inhibitors”, Research Monographs in Cell and Tissue Physiology, V-XXII, 1986.
Roller et al. “Potent Inhibition of Protein-Tyrosine Phosphatase-1B Using the Phosphotyrosyl Mimetic Fluoro-O-Malonyl Tyrosine (FOMT)”, Bioorg. Med. Chem. Lett., 8(16): 2149-2150, 1998.
Rubinfeld et al. “Binding of GSK3Beta to the APC-Beta-Catenin Complex and Regulation of Complex Assembly”, Science, 272(5264): 1023-1026, 1996.
Sambrook et al. “Molecular Cloning: A Laboratory Manual”, Cold Spring Harbour Press, 2nd Ed., V-XXXII, 1989.
Schiller et al. “Synthesis for Side-Chain Cyclized Peptide Analogs on Solid Supports”, Int. J. Peptide Protein Res., 25: 171-177, 1985.
Shapiro et al. “Combained Fmoc-Alloc Strategy for A General SPPS of Phosphoserine Peptides: Preparation of Phosphorylation-Dependent Tau Antisera”, Bioorg. Med. Chem., 5(1): 147-156, 1997.
Sherman et al. “Compatibility of Thioamides With Reverse Turn Features: Synthesis and Conformational Analysis of Two Model Cyclic Pseudopeptides Containing Thioamides as Backbone Modifications”, Journal of the American Chemical Society, 112: 433-441, 1990.
Shulman et al. “Quantitation of Muscle Glycogen Synthesis in Normal Subjects and Subjects With Non-Insulin-Dependent Diabetes by 13C Nuclear Magnetic Resonance Spectroscopy”, New England Journal of Medicine, 322(4): 223-228, 1990.
Stambolic et al. “Lithium Inhibits Glycogen Synthase Kinase-3 Activity and Mimics Wingless Signalling in Intact Cells”, Curr. Biol., 6: 1664-1668, 1996.
ter Haar et al. “Structure of GSK-3 Beta Reveals A Primed Phosphorylation Mechanism”, Nat. Struct. Biol., 8(7): 593-596, 2001.
Thomas “Excitatory Amino Acids in Health and Disease”, J. Am. Geriatr. Soc., 43: 1279-1289, 1995.
Thorsett et al. “Dipeptide Mimics. Conformationally Restricted Inhibitors of Angiotensin-Converting Enzyme”, Biochem. Biophys. Res. Commun., 111(1): 166-171, 1983.
Tong et al. “Activation of Glycogen Synthase Kinase-3 Beta (GSK-3 Beta) by Platelet Activating Factor Mediates Migration and Cell Death in Cerebellar Granule Neurons”, Eur. J. Neurosci., 13: 1913-1922, 2001.
Veber et al. “Conformationally Restricted Bicyclic Analogs of Somatostatin”, Proc. Natl. Acad. Sci. USA, 75(6): 2636-2640, 1978.
Welsh et al. “Glycogen Synthase Kinase-3 Is Rapidly Inactivated in Response to Insulin and Phosphorylates Eukaryotic Initiation Factor Eif-2B”, Biochem. J., 294(Pt 3): 625-629, 1993.
Wiemann et al. “Synthesis of Suitably Protected Hydroxymethylene Phosphonate- and ‘Phosphat Phosphonate’-Analogues of Phosphoserine and Their Incorporation Into Synthetic Peptides”, Tetrahedron, 56: 1331-1337, 2000.
Ye et al. “L-O-(2-Malonyl)Tyrosine: A New Phosphotyrosyl Mimetic for the Preparation of Src Homology 2 Domain Inhibitory Peptides”, J. Med. Chem., 38(21): 4270-4275, 1995.
Eldar-Finkleman et al. “The Insulin Mimetic Action of Glycogen Synthase Kinase-3 Inhibitors”, Diabetologia, 45(Suppl.2): A 70, 38th Annual Meeting for the European Association for the Study of Diabetes (EASD), Budapest, Hungary, 2002. Abstract.
Plotkin et al. “Insulin Mimetic Action of Synthetic Phosphorylated Peptide Inhibitors of Glycogen Synthase Kinase-3”, Journal of Pharmacology and Experimental Therapeutics, 305(3): 974-980, 2003.
Leclerc et al. “Indirubins Inhibit Glycogen Synthase Kinase-3β and CDK5/P25, Two Proteins Kinases Involved in Abnormal Tau Phosphorylation in Alzheimer's Disease”, The Journal of Biological Chemistry, 276(1): 251-260, 2001.
Hotamisligil et al. “IRS-1-Mediated Inhibition of Insulin Receptor Tyrosine Kinase Activity in TNT-α- and Obesity-Induced Insulin Resistance”, Science, 271: 665-667, 1996.
Tanti et al. “Serine/Threonine Phosphorylation of Insulin Receptor Substrate 1 Modulates Insulin Receptor Signaling”, The Journal of Biological Chemistry, 269(8): 6051-6057, 1994.
Fahraeus et al. “Inhibition of PRB Phosphorylation and Cell-Cycle Progression by A 20-Residue Peptide Derived From P16 CDKN2/INK4A”, Current Biology, 6(1): 84-91, 1996.
Mitchell et al. “Heat-Stable Inhibitor Protein Derived Peptide Substrate Analogs: Phosphorylation by cAMP-Dependent and cGMP-Dependent Protein Kinases”, Am. Chemical Soc., 1994.
Maniatis “Signal Transduction: Catalysis by A Multiprotein IkB Kinase Complex”, Science, 278(5339): 818, 1997. Extract.
American Diabetes Association “Standards of Medical Care for Patients With Diabetes Mellitus”, Diabetes Care, 17(6): 616-623, 1994.
Hawiger “Non-Invasive Intracellular Delivery of Functional Peptides”, Curr. Opin. Chem. Biol., 3: 89-94, 1999.
Moreno et al. “Glycogen Synthase Kinase 3 Phosphorylation of Different Residues in the Presence of Different Factors: Analysis on TAU Protein”, Mol.Cell.Biochem., 165(1):47-54, 1996. Tab.1.
Correll et al. “Inhibition of GSK3 Beta Mediates Cell Survival . . . Society For Neuroscience Abstracts” 25(2): 1519, 1999. Abstract No. 605.8.
Oelrichs et al. “Unique Toxic Peptides Isolated From Sawfly Larvae in Three Continents”, Toxicon, 37(3): 537-544, 1999. Fig.3.
Fiol et al. “Ordered Multisite Protein Phosphorylation. Analysis of Glycogen Synthase. Kinase-3 Action Using Model Peptide Substrates”, The Journal of Biological Chemistry, 265(11): 6061-6065, 1990. vol. 2: Abstract.
Barber et al. “Insulin Rescues Retinal Neurons From Apoptosis by A Phosphotidylinositol 3-Kinase/Akt-Mediated Mechanism That Reduces the Activation of Caspase-3”, The Journal of Biological Chemistry,

Affiliated with

Also associated with

Rating

Glycogen synthase kinase-3 inhibitors does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Glycogen synthase kinase-3 inhibitors, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Glycogen synthase kinase-3 inhibitors will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-4043572