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156 results about "GSK-3" patented technology
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Glycogen synthase kinase 3 is a serine/threonine protein kinase that mediates the addition of phosphate molecules onto serine and threonine amino acid residues. First discovered in 1980 as a regulatory kinase for its namesake, Glycogen synthase, GSK-3 has since been identified as a kinase for over forty different proteins in a variety of different pathways. In mammals GSK-3 is encoded by two paralogous genes, GSK-3 alpha (GSK3A) and GSK-3 beta (GSK3B). GSK-3 has recently been the subject of much research because it has been implicated in a number of diseases, including Type II diabetes (diabetes mellitus type 2), Alzheimer's disease, inflammation, cancer, and bipolar disorder.
5-substituted indazoles as kinase inhibitors
The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts,wherein A, R1, R2, R3 and m, are defined in the description. The present invention relates also to methods of making said compounds, and compositions containing said compounds which are useful for inhibiting kinases such as Glycogen Synthase kinase 3 (GSK-3), Rho kinase (ROCK), Janus Kinases (JAK), Cdc7, AKT, PAK4, PLK, CK2, KDR, MK2, JNK1, aurora, pim 1 and nek 2.
Owner:ABBVIE INC
GSK-3 inhibitors
Provided are thiadiazolidine compounds of formula I wherein R1 is an organic group having at least 8 atoms selected from C or O, which is not linked directly to the N through a —C(O)— and comprising at least an aromatic ring, and their pharmaceutical compositions. These compounds are selective GSK-3 inhibitors and have improved bioavailability. They are useful for the treatment of GSK-3 mediated diseases, among others Alzheimer's disease, type II diabetes, depression and brain injury.
Owner:ASD THERAPEUTICS PARTNERS LLC
Pyrazolylamine substituted quinazoline compounds useful as protein kinase inhibitors
This invention describes novel pyrazole compounds of formula III:wherein Ring D is a 5–7 membered monocyclic ring or 8–10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx and Ry are taken together with their intervening atoms to form a fused, unsaturated or partially unsaturated, 5–8 membered carbocyclo ring; and R2 and R2′ are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.
Owner:VERTEX PHARMA INC
Fused pyrimidyl pyrazole compounds useful as protein kinase inhibitors
This invention describes novel pyrazole compounds of formula IV: wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx and Ry are independently selected from T-R3, or taken together with their intervening atoms to form a fused, unsaturated or partially unsaturated, 5-8 membered ring having 1-3 ring heteroatoms selected from oxygen, sulfur, or nitrogen; and R2, R2′, T, and R3 are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.
Owner:VERTEX PHARMA INC
Pyrazole compounds useful as protein kinase inhibitors
This invention describes novel pyrazole compounds of formula IIc: wherein R1 is T-Ring D, wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx and Ry are taken together with their intervening atoms to form a fused, unsaturated or partially unsaturated, 5-7 membered ring having 0-3 heteroatoms; and R2 and R2′ are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of Aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.
Owner:VERTEX PHARMA INC
Inhibitors of GSK-3 and crystal structures of GSK-3beta protein and protein complexes
Owner:VERTEX PHARMA INC
Pyrazole compounds useful as protein kinase inhibitors
Owner:VERTEX PHARMA INC
Pyrazole compounds useful as protein kinase inhibitors
This invention describes novel pyrazole compounds of formula III: wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx and Ry are taken together with their intervening atoms to form a fused, unsaturated or partially unsaturated, 5-8 membered carbocyclo ring; and R2 and R2′ are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.
Owner:VERTEX PHARMA INC
GSK-3 inhibitors
This invention relates to methods of treating or preventing bone loss by administering to a human or animal subject pyrimidine and pyridine derivatives that inhibit the activity of glycogen synthase kinase 3 (GSK3), to pharmaceutical compositions containing the compounds, and to the use of the compounds and compositions alone or in combination with other pharmaceutically active agents.
Owner:MICHIGAN UNIVERISTY OF +1
Process for preparing 5-fluoro-1H-pyrazolo [3,4-B] pyridin-3-amine and derivatives thereof
![Process for preparing 5-fluoro-1H-pyrazolo [3,4-B] pyridin-3-amine and derivatives thereof](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/63fdb9a4-63aa-415b-bfec-98ad73771416/US08242272-20120814-C00001.png "Process for preparing 5-fluoro-1H-pyrazolo [3,4-B] pyridin-3-amine and derivatives thereof")
![Process for preparing 5-fluoro-1H-pyrazolo [3,4-B] pyridin-3-amine and derivatives thereof](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/63fdb9a4-63aa-415b-bfec-98ad73771416/US08242272-20120814-C00002.png "Process for preparing 5-fluoro-1H-pyrazolo [3,4-B] pyridin-3-amine and derivatives thereof")
![Process for preparing 5-fluoro-1H-pyrazolo [3,4-B] pyridin-3-amine and derivatives thereof](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/63fdb9a4-63aa-415b-bfec-98ad73771416/US08242272-20120814-C00003.png "Process for preparing 5-fluoro-1H-pyrazolo [3,4-B] pyridin-3-amine and derivatives thereof")
Owner:VERTEX PHARMA INC
Method for inducing transdifferentiation of somatic cells into neural stem cells and application thereof
ActiveCN104894060AGood pluripotent differentiation performanceNervous disorderNervous system cellsDiseaseTransdifferentiation
Provided are a method for inducing the transdifferentiation of somatic cells into neural stem cells and application for same. Using a combination of a histone deacetylase (HDAC) inhibitor, a glycogen synthase kinase (GSK-3) inhibitor, and a transforming growth factor β (TGF-β) signal pathway inhibitor, in a low-oxygen normal physiological environment, induce somatic cells such as fibroblasts and epithelial cells to form into neural stem cells having good pluripotency and passage stability.
Owner:CENT FOR EXCELLENCE IN MOLECULAR CELL SCI CHINESE ACAD OF SCI
5-substituted indazoles as kinase inhibitors
The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts,wherein A, R1, R2, R3 and m, are defined in the description. The present invention relates also to methods of making said compounds, and compositions containing said compounds which are useful for inhibiting kinases such as Glycogen Synthase kinase 3 (GSK-3), Rho kinase (ROCK), Janus Kinases (JAK), Cdc7, AKT, PAK4, PLK, CK2, KDR, MK2, JNK1, aurora, pim 1 and nek 2.
Owner:ABBVIE INC
Pyrro-quinoline quinine sodium salt derivative and preparation method thereof
InactiveCN101885725AGood water solubilityMild reaction conditionsOrganic active ingredientsNervous disorderQuinolineStructural formula
The invention relates to a pyrro-quinoline quinine (PQQ) sodium salt derivative and a preparation method thereof, belonging to the field of pharmacy. In the preparation method, PQQ is used as a raw material, and an acid-base neutralization reaction with PQQ is carried out in a basic solvent of sodium hydroxide to prepare the PQQ sodium salt derivative represented in the structural formula (I), wherein R1, R2 and R3 can be identical or different and respectively represents H, ammonium ion (NH3), potassium ion, sodium ion, magnesium ion, calcium ion or zinc ion, and at least one of R1, R2 and R3 is sodium ion. The invention has mild reaction conditions, easy product refining and purification, simple preparation steps and high yield more than 80%. The PQQ sodium salt derivative has the functions of inhibiting GSK-3 activity, reducing senile pigment formation in a transgenic mouse brain, reducing tau protein phosphorylation and the like. Thus, the PQQ sodium salt derivative can be medically used for treating senile dementia and other diseases.
Owner:SHANGHAI RIXIN BIOTECHNOLOGY CO LTD
Compositions useful as inhibitors of protein kinases
ActiveUS7601718B2Inhibiting GSK- activityAlleviate the conditionBiocideNervous disorderDiseasePTK Inhibitors
The present invention provides a compound of formula I:or a pharmaceutically acceptable salt or mixtures thereof. These compounds are inhibitors of protein kinases, particularly inhibitors of GSK mammalian protein kinase, and more particularly inhibitors of GSK-3 mammalian protein kinase. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of utilizing those compounds and compositions in the treatment of various protein kinase mediated disorders.
Owner:VERTEX PHARMA INC
Benzofuran-3-yl(indol-3-yl) maleimides as potent GSK3 inhibitors
Compounds of formula:and pharmaceutically acceptable salts, esters and solvates thereof, where variables are defined in the specification, useful generally as inhibitors of protein kinases and particularly useful for inhibition of GSK-3.Pharmaceutically compositions and medicaments containing a compound of the invention are provided. The invention provides methods of treatment of protein kinase-related disease, disorders or conditions. The invention provides methods of treatment of GSK-3-related diseases, disorders or conditions. More specifically, methods of treatment of bipolar disorder, including mania, schizophrenia, stroke, epilepsy, motor neuron disease, cranial or spinal trauma, neurodegenerative disorders, including multiple sclerosis (MS), Alzheimer's disease, Fragile X syndrome, autism, Huntington's disease, Parkinson's disease, amylotrophic lateral sclerosis (ALS), AIDS-associated dementia, diabetes, particularly type II diabetes, cardiomycete hypertrophy, reperfusion / ischemia, cancer, particularly colorectal cancer, pancreatic cancer, allergies and / or asthma and hair loss or baldness.
Owner:THE BOARD OF TRUSTEES OF THE UNIV OF ILLINOIS
Pyrrolopyrimidine thion derivatives
InactiveUS20050153992A1Strong inhibitory activityEasy to manufactureAntibacterial agentsOrganic active ingredientsHydrogen atomHalogen
A compound having GSK-3 inhibiting function. A1 and A3 are a single bond, an aliphatic hydrocarbon group; A2 and A4 are a single bond, CO, COO, CONR, O, OCO, NR, NRCO, NRCOO, etc.; G1 is a single bond, an aliphatic hydrocarbon, aromatic hydrocarbon, heterocyclic; G2 is a hydrogen atom, an aliphatic hydrocarbon, an alicyclic hydrocarbon, an aromatic hydrocarbon, heterocyclic; A5 is a single bond, NR; R2 is H, halogen, an aliphatic hydrocarbon, alicyclic hydrocarbon, aromatic hydrocarbon, heterocyclic; A6 is a single bond, NR, CO, NRCO, NRCONR, CONR, COO, O, etc.; R3 is H, halogen, nitro, saturated aliphatic hydrocarbon, alicyclic hydrocarbon, aromatic hydrocarbon, heterocyclic; and when A6 is CR═CR or C≡C; R3 may be a trimethylsilyl, formyl, acyl, carboxyl, alkoxylcarbonyl, carbamoyl, alkylcarbamoyl or cyano group; and R is H or an aliphatic hydrocarbon group.
Owner:TEIJIN PHARMA CO LTD
Pyrazole compounds useful as protein kinase inhibitors
This invention describes novel pyrazole compounds of formula IV: wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx and Ry are independently selected from T-R3, or taken together with their intervening atoms to form a fused, unsaturated or partially unsaturated, 5-8 membered ring having 1-3 ring heteroatoms selected from oxygen, sulfur, or nitrogen; and R2, R2′, T, and R3 are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.
Owner:VERTEX PHARMA INC
Heterocyclic inhibitors of glycogen synthase kinase GSK-3
Compounds of general formula (I): where A, E, G, X, Y and the bond - - - take various meanings are of use in the preparation of a pharmaceutical formulation, for example in the treatment of a disease in which GSK-3 is involved, including Alzheimer's disease or the non-dependent insulin diabetes mellitus, or hyperproliferative disease such as cancer, displasias or metaplasias of tissue, psoriasis, arteriosclerosis or restenosis.
Owner:AUTONOMOUS UNIVERSITY OF MADRID +1
Glycogen synthase kinase-3 inhibitors
Novel peptide inhibitors of GSK-3, compositions containing same and uses thereof are disclosed. The novel peptide inhibitors are substrate-competitive inhibitors and have an amino acid sequence designed so as to bind to a defined binding site subunit in GSK-3. Also disclosed are GSK-3 substrate competitive inhibitors which bind to the defined binding site subunit in the enzyme. Also disclosed are mutants of GSK-3 and uses thereof for identifying a putative GSK-3 substrate competitive inhibitor.
Owner:RAMOT AT TEL AVIV UNIV LTD
Methods and compositions for expansion of stem cells and other cells
Presented herein are methods of generating a multipotent or immature cell from a mature somatic cell, involving contacting a mature somatic cell with one or more small molecule compounds selected from: a histone deacetylase (HDAC) inhibitor; a glycogen synthase kinase 3 (GSK-3) inhibitor; one or more transforming growth factor-beta receptor (TGF-βR) inhibitors; one or more lysine-specific demethylase 1 (LSD1) inhibitors; a cAMP agonist; a histone lysine methyltransferase (EZH2) inhibitor; and a histone methyltransferase (HMTase) G9a inhibitor; valproic acid. Also provided are methods of generating a multipotent or immature cell from a somatic cell, by driving expression of OCT4, or an OCT4 functional homolog or derivative, under the control of a high expressing promoter. Presented herein are also methods of stem cell expansion, stem cell regeneration and differentiation, which comprise contacting stem cells with one or more small chemical compounds.
Owner:THE RES FOUND OF STATE UNIV OF NEW YORK
Detecting disease association with aberrant glycogen synthase kinase 3beta expression
The present invention provides a method for diagnosing a disease or disorder associated with aberrant GSK-3β expression and / or activity or for determining the predisposition of a subject to the disease or disorder. In particular, the methods of the present invention comprise detecting a marker that comprises one or more polymorphisms and / or one or more allelic variants of a glycogen synthase kinase 3β gene. The present invention also relates to a method for identifying new markers that are diagnostic of a disease or disorder associated with aberrant GSK-3β expression and / or activity. Furthermore, the present invention relates to methods of identifying and producing candidate compounds for the treatment of a disease or disorder associated with aberrant GSK-3β expression and / or activity.
Owner:GARVAN INST OF MEDICAL RES
Heterocyclic compounds and their use as glycogen synthase kinase-3 inhibitors
ActiveUS20120077840A1Use of compositionPrevention and/or treatmentBiocideSenses disorderTreatment useGlycogen synthase
Owner:ABBVIE DEUTSHLAND GMBH & CO KG
GSK-3 inhibitors
The invention relates to urea derivatives of formula (I) as inhibitors of glycogen synthase kinase 3β, GSK-3, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which GSK-3 is involved, such as Alzheimer's disease or non-insulin dependent diabetes mellitus.
Owner:ASD THERAPEUTICS PARTNERS LLC
Inhibitors of GSK-3 and uses thereof
InactiveUS6916798B2Enhancing glycogen synthesisDecreased blood levelBiocideMonoazo dyesDiabetes mellitusDisease
The present invention relates to compounds of formula I that are useful as GSK-3 inhibitors. The invention also relates to methods of using compounds of formula I or pharmaceutical compositions comprising compounds of formula I to inhibit GSK-3 activity. The invention further provides methods of utilizing these compounds and pharmaceutical compositions in the treatment and prevention of various disorders, such as diabetes and Alzheimer's disease. The invention also relates to methods for inhibiting Aurora-2 activity and for treating or preventing Aurora-2-mediated diseases using compounds of formula I or pharmaceutical compositions comprising compounds of formula I. The invention also relates to methods for inhibiting cyclin-dependent kinase-2 activity and for treating or preventing inhibiting cyclin-dependent kinase-2-mediated diseases using compounds of formula I or pharmaceutical compositions comprising compounds of formula I.
Owner:VERTEX PHARMA INC
Uses of chemicals to modulate GSK-3 signaling for treatment of bipolar disorder and other brain disorders
Aspects of this invention are related, at least in part, to the use of chemical compounds able to inhibit GSK-3 and / or to stabilize β-catenin and formulations thereof. Some aspects of this invention relate to compositions comprising such compounds. Some aspects of the invention provide methods of using such compounds and / or compositions in the treatment of subjects having a neurological disease and / or psychiatric disorder. Some aspects of this invention provide methods of using ruboxistaurin, enzastaurin, sunitinib, midostaurin, lestaurtinib, 7-hydroxystaurosporine, and / or Chir99021 in the treatment of subjects having a neurological disease and / or psychiatric disorder. In some embodiments, compounds are administered in combination with Lithium.
Owner:MASSACHUSETTS INST OF TECH +1
Pyrrolopyrimidinone derivatives
InactiveUS20060160831A1Easy to manufactureProcess stabilityBiocideOrganic active ingredientsHalogenTrimethylsilyl
A compound having GSK-3 inhibitory activity. A1 and A3 are a single bond, an aliphatic hydrocarbon group; A2 and A4 are a single bond, CO, COO, CONR, O, OCO, NR, NRCO, NRCOO, etc.; G1 is a single bond, an aliphatic hydrocarbon, aromatic hydrocarbon, heterocyclic; G2 is H, an aliphatic hydrocarbon, an alicyclic hydrocarbon, an aromatic hydrocarbon, heterocyclic; A5 is a single bond, NR; R2 is H, halogen, an aliphatic hydrocarbon, alicyclic hydrocarbon, aromatic hydrocarbon, heterocyclic; A6 is a single bond, NR, CO, NRCO, NRCONR, CONR, COO, O, etc.; R3 is H, halogen, nitro, saturated aliphatic hydrocarbon, alicyclic hydrocarbon, aromatic hydrocarbon, heterocyclic; and R3 may be a trimethylsilyl, formyl, acyl, carboxyl, alkoxylcarbonyl, carbamoyl, alkylcarbamoyl, or cyano group when A6 is CR═CR or C≡C, wherein R is H or an lower aliphatic hydrocarbon group.
Owner:TEIJIN LTD
5-heteroaryl substituted indazoles as kinase inhibitors
The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein A, R1, R2, R3 and m, are defined in the description. The present invention relates also to methods of making said compounds, and compositions containing said compounds which are useful for inhibiting kinases such as Glycogen Synthase kinase 3 (GSK-3), Rho kinase (ROCK), Janus Kinases (JAK), AKT, PAK4, PLK, CK2, KDR, MK2, JNK1, aurora, pim 1 and nek 2.
Owner:ABBOTT LAB INC +1
Pyrazole Compound
InactiveUS20090156582A1Easy to useImprove solubilityBiocideNervous disorderDiseasePathology diagnosis
The present invention provides a pyrazole compound represented by the formula (I):wherein ring A0 is a pyrazole ring optionally further having 1 or 2 substituents; Ra is a substituted carbamoyl group; and Rb is an optionally substituted acylamino group, or a salt thereof or a prodrug thereof, which is useful as an agent for the prophylaxis or treatment of GSK-3β related pathology or disease, and a GSK-3β inhibitor including same.
Owner:TAKEDA PHARMA CO LTD
Dihydropyrazolopyridine compounds and pharmaceutical use thereof
The present invention provides dihydropyrazolopyridine compounds represented by the formula (I): wherein each symbol is as defined in the specification, optically active forms thereof, and pharmaceutically acceptable salts thereof and hydrates thereof. The compounds of the present invention show a selective and strong inhibitory activity on glycogen synthase kinase-3 beta (GSK-3β), and are useful as medicaments for prevention and / or treatment of diabetes, diabetic complications and neurodegenerative diseases or as immunopotentiators.
Owner:MITSUBISHI TANABE PHARMA CORP
Glycogen synthase kinase-3 inhibitors
InactiveUS7378432B2Easy to useReduced activityBiocidePeptide/protein ingredientsBinding siteGlycogen synthase
Owner:TEL AVIV UNIV FUTURE TECH DEVMENT
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