Target and Its Patented Drug(s)

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Target General Information
Patent(s) and the Corresponding Patented Drug(s)
References
Target General Information  Top
Target ID T76910 Target Info
Target Name Glycogen synthase kinase-3 alpha (GSK-3A)
Synonyms Serine/threonineprotein kinase GSK3A; Serine/threonine-protein kinase GSK3A; Glycogen synthase kinase3 alpha; Glycogen synthase kinase 3; GSK3 alpha; GSK-3 alpha; GSK-3
Target Type Successful Target
Gene Name GSK3A
Biochemical Class Kinase
UniProt ID
GSK3A_HUMAN
Patent(s) and the Corresponding Patented Drug(s)  Top
World Intellectual Property Organization (WIPO)
Patent ID WO2015155738
Title Use of Gsk-3 Inhibitors or Activators Which Modulate Pd-1 or T-Bet Expression To Modulate T Cell Immunity.
Abstract The present application generally relates to the discovery that glycogen synthase kinase 3 (GSK-3) is an upstream signalling molecule that controls PD-1 transcription and Tbet expression by immune cells and in particular T-cells. Based on this discovery, and in view of the known immunosuppressive effect of PD-1 on immunity and the promoting effect of Tbet on T cell immunity, the present invention relates to the use of GSK-3 inhibitors to promote immunity, including cytotoxic T cell immunity in subjects in need thereof, especially subjects with chronic conditions wherein inhibiting PD-1 expression and/or blockade or Tbet upregulation is therapeutically desirable such as cancer and infectious conditions. Further, based on this discovery the present invention relates to the use of compounds which promote GSK-3 expression or activity to suppress immunity, especially aberrant T cell immunity in subjects in need thereof, e.g., subjects with chronic conditions wherein PD-1 upregulation or Tbet down regulation is therapeutically desirable such as allergic, autoimmune or inflammatory conditions. Also, screening methods for identifying immune agonists and antagonists, especially antibodies, are provided.
Applicant(s) Rudd, Christopher
Representative Drug(s) D0J6UW Drug Info N.A. Click to Show More [1]
2 D0QW6B Drug Info N.A. [1]
Patent ID WO2013182519
Title Combination of Lysosomotropic or Autophagy Modulating Agents and A Gsk-3 Inhibitor for Treatment of Cancer.
Abstract The invention relates to combinations oflysosomotropic agent or agents modulating autophagy, such as chloroquine, 3-methyladenine or bafilomycin A1, and a GSK-3 inhibitor, such as (2'Z,3'E)-6-bromoindirubin-3'-acetoxime, TDZD-8 or L803-mts. These compositions are useful in the treatment of cancer, proliferative inflammatory diseases, degenerative diseases and some infectious diseases, preferably cancer. The tumor cell survival is particularly dependent on proper endoplasmic reticulumf unction.
Applicant(s) Universitaet Basel
Representative Drug(s) D03SNE Drug Info N.A. Click to Show More [1]
2 D06KNK Drug Info N.A. [1]
Patent ID WO2011064549
Title Composition and Method for Differentiation of Human Embryonic Stem Cells.
Abstract Described are methods for inducing differentiation of a human embryonic stem cell or a population of human embryonic stem cells toward a cell or population of cells characteristic of the definitive endoderm, the method comprising incubating the cell or population of cells with a GSK-3 inhibitor. Also described are methods for inducing differentiation of a cell or population of cells, characteristic of the definitive endoderm, towards a hepatocyte-like cell or a population of hepatocyte-like cells, and methods for inducing differentiation of a human embryonic stem cell or a population of human embryonic stem cells toward a hepatocyte-like cell or a population of hepatocyte-like cells. Further described are cells obtained by the methods and uses thereof in therapy and toxicity screening.
Applicant(s) Stem Cells for Safer Medicines Limited
Representative Drug(s) D0I2RF Drug Info N.A. Click to Show More [1]
2 D0NG2F Drug Info N.A. [1]
Patent ID WO2014050779
Title Combination of Gsk3 Inhibitor and Anti-Dr5 Antibody.
Applicant(s) Daiichi Sankyo Company, Limited
Patent ID WO2015131788
Title Treatment of Neurological Conditions.
Abstract Provided are methods of producing a neuronal phenotype in a glial cell or somatic non-neuronal cell. The methods comprise contacting the glial cell or the somatic non-neuronal cell with a composition including small molecules. Also provided are methods for screening for a therapeutic agent for a neurological condition of a subject.
Applicant(s) Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences
Patent ID WO2014083132
Title Maturation of Hepatocyte-Like Cells Derived From Human Pluripotent Stem Cells.
Abstract The present invention relates to directed differentiation and maturation of hepatocyte-like cells. In particular, the present invention relates to exposure of hepatocyte-like cells to an activator of a retinoic acid responsive receptor, such as retinoic acid (RA), optionally in combination with an inhibitor of GSK-3 (Glycogen synthase kinase 3) or activator of Wnt signalling and/or with the overlay of the cells with one or more components characteristic of the mammalian extracellular matrix (matrix overlay).The present invention also relates to exposure of hepatocyte-like cells to an activator of a retinoic acid responsive receptor, such as retinoic acid (RA), optionally in combination with an inhibitor of a cycline dependent kinase (CDK) and/or with the overlay of the cells with one or more components characteristic of the mammalian extracellular matrix (matrix overlay). The hepatocyte-like cells obtained in accordance with the present invention show a phenotype which is more similar to that of primary hepatocytes than previously shown.
Applicant(s) Takara Bio Europe Ab
Representative Drug(s) D00PWQ Drug Info N.A. [1]
Patent ID WO2014059383
Title Gsk3 Inhibitors and Methods of Use Thereof.
Abstract The present invention provides compounds of formula I, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting kinase (e.g., GSK3 (e.g., GSK3a or GSK3P) or CK1) activity. The present invention further provides methods of using the compounds described herein for treating kinase-mediated disorders, such as neurological diseases, psychriatic disorders, metabolic disorders, and cancer. I.
Applicant(s) The Broad Institute, Inc
Representative Drug(s) D0FV9Z Drug Info N.A. [1]
Patent ID WO2014053580
Title Anticonvulsant Activity of Gsk-3Beta Inhibitors.
Abstract The present invention relates to the anticonvulsant activity of GSK-3gamainhibitors and the use of GSK-3gama inhibitors as agents for the treatment of neurological disorders characterized by seizures such as epilepsy.
Applicant(s) Katholieke Universiteit Leuven
Representative Drug(s) D0I2RF Drug Info N.A. [1]
Patent ID WO2014003098
Title Tricyclic Compound.
Abstract To provide a novel compound which inhibits GSK3 and is useful for the treatment of diseases associated with GSK. Provided is a compound represented by genera formula (1) or a salt thereof. (In the formula, R1, R2, R3, R4, X1 and X2 are as defined in the description.).
Applicant(s) Daiichi Sankyo Co Ltd
Patent ID WO2013150284
Title Tolerisation- Inducing Composition.
Abstract The present invention relates to a composition comprising a tolerogenic peptide and a GSK-3 inhibitor and uses thereof. The invention also relates to the use of a GSK-3 inhibitor to accelerate the peptide-mediated shift in secretion profile of lymphocytes from pro-inflammatory to anti-inflammatory cytokines. The GSK-3 inhibitor may be used to enhance antigen-specific immunotherapy.
Applicant(s) University of Bristol
Patent ID WO2011116930
Title Directed Differentiation and Maturation of Pluripotent Cells Into Hepatocyte Like Cells By Modulation of Wnt-Signalling Pathway.
Abstract Provided are improved methods using Glycogen synthase kinase 3 (GSK3) inhibitors by which endodermal cells, notably endodermal cells derived from human pluripotent stem cells (hPS), such as but not limited to hiPS-cells and hES-cells may be differentiated into hepatocyte like cells. The specific modulation of wingless integration gene (WNT)-signalling pathway and use of GSK3 inhibitors achieve direct differentiation and maturation of hepatocytes derived from human pluripotent stem (hPS) cells. GSK-3 inhibitors, when added to the growth medium at certain developmental stages, leads to more mature and functional features for the hepatocyte like cells as well as more pure and homogenous populations of hepatocyte like cells. Provided are also hepatocyte like cells obtained by these methods as well as compositions comprising them.
Applicant(s) Cellartis Ab
Representative Drug(s) D0I2RF Drug Info N.A. [1]
United States Patent and Trademark Office (USPTO)
Patent ID US20160058738
Title Pharmaceutical Composition for Preventing or Treating Ovary Granulosa Cell Tumors Containing Glycogen Synthase Kinase-3 Beta Inhibitor As Active Ingredient, and Functional Health Food Composition.
Applicant(s) Chung-Ang University
Representative Drug(s) D0A3MV Drug Info N.A. Click to Show More [1]
2 D0QW6B Drug Info N.A. [1]
Patent ID US9469618
Title Thiadiazolidinediones As Gsk-3 Inhibitors.
Representative Drug(s) D02OGA Drug Info N.A. Click to Show More [1]
2 D0CR2E Drug Info N.A. [1]
3 D0QE2H Drug Info N.A. [1]
Patent ID US8697698
Title Pyrazole Compounds Useful As Protein Kinase Inhibitors.
Representative Drug(s) D03ETN Drug Info N.A. Click to Show More [1]
2 D08CWE Drug Info N.A. [1]
3 D0J9YX Drug Info N.A. [1]
Patent ID US8653088
Title Compositions Useful As Inhibitors of Protein Kinases.
Representative Drug(s) D03ETN Drug Info N.A. Click to Show More [1]
2 D08CWE Drug Info N.A. [1]
3 D0J9YX Drug Info N.A. [1]
Patent ID US8642598
Title Heterocyclic Compounds and Their Use As Glycogen Synthase Kinase 3 Inhibitors.
Representative Drug(s) D06ZRL Drug Info N.A. Click to Show More [1]
2 D0RD9V Drug Info N.A. [1]
Patent ID US2015152389
Title Generation of Cardiomyocytes From Human Pluripotent Stem Cells.
Representative Drug(s) D0I2RF Drug Info N.A. [1]
Patent ID US2012172376
Title Heterocyclic Compounds and Their Use As Glycogen Synthase Kinase-3 Inhibitors.
Representative Drug(s) D01WAJ Drug Info N.A. Click to Show More [1]
2 D0NO7V Drug Info N.A. [1]
Patent ID US2012077840
Title Heterocyclic Compounds and Their Use As Glycogen Synthase Kinase-3 Inhibitors.
Representative Drug(s) D01WAJ Drug Info N.A. Click to Show More [1]
2 D0NO7V Drug Info N.A. [1]
Patent ID US08633210
Title Triazole Compounds Useful As Protein Kinase Inhibitors.
Representative Drug(s) D03ETN Drug Info N.A. Click to Show More [1]
2 D08CWE Drug Info N.A. [1]
3 D0J9YX Drug Info N.A. [1]
Patent ID US20140005184
Title Spirocyclic Aminoquinolones As Gsk-3 Inhibitors.
Representative Drug(s) D09PGW Drug Info EC50 = 3200 nM; IC50 = 36000 nM [1]
Patent ID US08686042
Title Gsk-3 Inhibitors.
Patent ID US8778936
Title Pyrazole Compounds That Modulate The Activity of Cdk, Gsk and Aurora Kinases.
Representative Drug(s) D0M9JE Drug Info N.A. [1]
Patent ID US8648069
Title 5-Substituted Indazoles As Kinase Inhibitors.
Patent ID US2005153992
Title Pyrrolopyrimidine Thion Derivatives.
Representative Drug(s) D0P8RK Drug Info N.A. [1]
European Patent Office (EPO)
Patent ID EP2769720
Title Heterocyclic Gsk-3 Allosteric Modulators.
Representative Drug(s) D04RDR Drug Info N.A. Click to Show More [1]
2 D0A4QD Drug Info N.A. [1]
References  Top
REF 1 Glycogen synthase kinase 3 (GSK-3) inhibitors: a patent update (2014-2015).Expert Opin Ther Pat. 2017 Jun;27(6):657-666.

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