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31 results about "Gsk 3beta" patented technology
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Inhibitors of GSK-3 and crystal structures of GSK-3beta protein and protein complexes
Owner:VERTEX PHARMA INC
3,4-dihydrobenzo[f][1,4]thiazepine compound or salts of same and medical use of same
InactiveCN101891706AInhibitory activityOrganic active ingredientsNervous disorderDiseaseDiabetes mellitus
The invention relates to 3,4-dihydrobenzo[f][1,4]thiazepine compound of the general formula I or salts of the same and medicinal use of the same, belonging to the field of pharmaceutical chemistry. The 3,4-dihydrobenzo[f][1,4]thiazepine compound can inhibit glycogen synthase kinase-3beta (GSK-3beta) and be used as the non-ATP competitive micromolecular inhibitor of the GSK-3beta to prepare medicaments used for preventing or treating diseases related to the GSK-3beta. The invention further discloses the application of a medical combination formed by the compound and pharmaceutically acceptablesalts of the same to preparation of medicaments for preventing or treating the diseases related to the GSK-3beta, such as diabetes, Alzheimer's diseases and tumors.
![3,4-dihydrobenzo[f][1,4]thiazepine compound or salts of same and medical use of same](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/64c8d796-b7ae-4f07-8728-a8af11fc99c4/HSA00000081542300011.PNG "3,4-dihydrobenzo[f][1,4]thiazepine compound or salts of same and medical use of same")
![3,4-dihydrobenzo[f][1,4]thiazepine compound or salts of same and medical use of same](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/64c8d796-b7ae-4f07-8728-a8af11fc99c4/HSA00000081542300012.PNG "3,4-dihydrobenzo[f][1,4]thiazepine compound or salts of same and medical use of same")
![3,4-dihydrobenzo[f][1,4]thiazepine compound or salts of same and medical use of same](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/64c8d796-b7ae-4f07-8728-a8af11fc99c4/DSA00000081542000011.PNG "3,4-dihydrobenzo[f][1,4]thiazepine compound or salts of same and medical use of same")
Owner:FUDAN UNIV
Modulation of GSK-3beta activity and its different uses
InactiveUS20020165197A1Prevent manifestationBiocideNervous disorderKinase activityAdenosine A3 Receptor Antagonists
The present invention concerns the modulation of glycogene synthase kinase 3beta (G3SK-3beta) by an adenosine receptor ligand. Depending on the type of ligand, the modulation may be manifested by down-regulation or up-regulation of the kinase's activity. Thus, there is provided by the present invention a method and pharmacetical compositions for achieving a therapeutic effect involved in modulating GSK-3beta activity in cells by the use of an adenosine receptor ligand or a combination of ARLs. When modulation involves activation of GSK-3beta activity the ARL may be an adenosine A1 receptor agonist (A1RAg), an adenosine A3 receptor agonist (A3RAg), an adenosine A2 receptor antagonist (A2RAn) or any combination of the same, while when modulation involves inhabition of GSK-3beta activity the ARL may be an adenosine A1 receptor antagonist (A1RAn), an adenosine A3 receptor antagonist (A3RAn), an adenosine A2 receptor agonist (A2RAg) or any combination of the same.
Owner:CAN-FITE BIOPHARMA LTD
Novel serology biomarker GSK3beta detection method for cognitive impairment of diabetic
The invention provides a novel serology biomarker GSK3beta detection method for cognitive impairment of a diabetic. The method comprises an enzyme activity assay method and a relative quantification dot-blot method. According to the enzyme activity assay method, a GSK-3beta enzyme activity assay kit of GENMED is applied; GSK-3beta phosphorylation is performed under the suppression of GSK-3alpha; along with oxidation reaction of reduced form of nicotinamide-adenine dinucleotid (NADH), a pyruvate kinase and lactic dehydrogenase continuous circulation method reaction system adopts the spectrophotometric method to measure the peak value change after oxidization so as to reflect GSK 3beta activity in a sample. The dot-blot method transfers blood platelet protein to an NC film according to the antigen and antibody fixation reaction principle and then utilizes antibody to perform detection. The novel serology biomarker GSK3beta detection method is used for studying GSK-3beta protein and enzyme activity expression in the diabetic blood and is expected to become a serology biomarker for early diagnosis of Alzheimer's disease (AD).
Owner:HUAZHONG UNIV OF SCI & TECH
Application of SBT as inhibitor of GSK-3beta
InactiveCN102552269AImprove the level ofLower levelNervous disorderInorganic active ingredientsDiseaseMedicine
The invention provides an application of SBT as an inhibitor of GSK-3beta, and particularly SBT is applicable to the prevention and treatment of alzheimer disease and senility. Currently, no research on the application of SBT to the prevention and treatment of AD and senility is reported at home and abroad. The invention firstly discloses that SBT has the effect of increasing the p-GSK-3beta level, decreasing the GSK-3beta level, and protecting nerves, and thus is applicable to the prevention and / or treatment of AD and senility.
Owner:SHANGHAI RIXIN BIOTECHNOLOGY CO LTD
Applications of 2,3-dihydro[1,5] benzothiazepine compounds or salts thereof in preparation of GSK-3beta inhibitor
The invention belongs to the field of pharmaceutical chemistry, and discloses 2,3-dihydro[1,5] benzothiazepine compounds of non-adenosine triphosphate (ATP) competitive inhibition glycogen synthase kinase-3beta (GSK-3beta) with a structure shown in formula I. The compounds can inhibit the activity of the GSK-3beta in a non ATP competitive mode, and can be used as micromolecule inhibitors of the GSK-3beta for preparing medicines for preventing or treating GSK-3beta related diseases. The invention further provides applications of the compounds, pharmaceutical acceptable salts thereof, or medicine compositions thereof to preventing or treating the GSK-3beta related diseases. The GSK-3beta related diseases can be diabetes and an Alzheimer's disease.
![Applications of 2,3-dihydro[1,5] benzothiazepine compounds or salts thereof in preparation of GSK-3beta inhibitor](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/49c1d7e7-cb1a-48de-9d7c-db0024cc87f7/H2009101744569E0000011.png "Applications of 2,3-dihydro[1,5] benzothiazepine compounds or salts thereof in preparation of GSK-3beta inhibitor")
![Applications of 2,3-dihydro[1,5] benzothiazepine compounds or salts thereof in preparation of GSK-3beta inhibitor](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/49c1d7e7-cb1a-48de-9d7c-db0024cc87f7/H2009101744569E0000012.png "Applications of 2,3-dihydro[1,5] benzothiazepine compounds or salts thereof in preparation of GSK-3beta inhibitor")
![Applications of 2,3-dihydro[1,5] benzothiazepine compounds or salts thereof in preparation of GSK-3beta inhibitor](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/49c1d7e7-cb1a-48de-9d7c-db0024cc87f7/H2009101744569E0000021.png "Applications of 2,3-dihydro[1,5] benzothiazepine compounds or salts thereof in preparation of GSK-3beta inhibitor")
Owner:FUDAN UNIV
Application of magnetic induction protein to improvement of neurodegenerative diseases
ActiveCN108853501AImprove survival rateEasy to learnNervous disorderPeptide/protein ingredientsBAX ProteinGsk 3beta
The invention relates to the field of magnetic genetics, and particularly relates to application of magnetic induction protein to improvement of neurodegenerative diseases. According to the application of magnetic induction protein to improvement of the neurodegenerative diseases disclosed by the invention, an experiment proves that the magnetic induction protein is imported into PD cells so thata result shows that a survival ratio of the PD cells is increased under the effect of a magnetic field, and alpha-synuclein and GSK-3beta levels in the PD cells are reduced; the magnetic induction protein is imported into an AD rat model; under the effect of the magnetic field, Bcl-2 expression of AD-model rat hippocampus CA1 area is increased, and Bax protein expression is reduced, and the learning and memory abilities of the rats are improved; therefore, the magnetic induction protein has the effects of improving the neurodegenerative diseases. The invention also provides the medicine for improving the neurodegenerative diseases, and the medicines comprise magnetic induction protein or gene engineering carriers for expressing the magnetic induction protein.
Owner:HEYE HEALTH TECH CO LTD
Small interference RNAs for human GSK-3beta gene and application thereof
InactiveCN102776176AEfficient expressionInhibit expressionMetabolism disorderGenetic material ingredientsGsk 3betaCoding region
The invention relates to a set of siRNAs directed at the human GSK-3beta gene and application thereof. According to the invention, sequences at the coding region of the human GSK-3beta gene are selected as target sites of the siRNAs, and the siRNAs are designed based on 10 to 30 (preferably, 15 to 27, and more preferably, 19 to 23) continuous base sequences in the target sites. Cell experiments prove that the siRNAs can reduce expression of the human GSK-3beta gene in a sequence-specific manner and thus reduce the expression level of GSK-3beta protein.
Owner:SHANGHAI TENTH PEOPLES HOSPITAL
Application of fungus polyketide in preparation of medicine used for treating alzheimer disease
InactiveCN103393625AInhibit apoptosisReduce apoptosisOrganic active ingredientsNervous disorderBeta-cateninPolyketide
The invention relates to an application of fungus polyketide in preparation of a medicine used for treating alzheimer disease. According to the application, a fungus polyketide compound is prepared into an injection preparation used for treating the alzheimer disease, molecular weight of the fungus polyketide compound is 478.434Da, and 10mg / Kg injection preparation is intraperitoneally injected everytime; the fungus polyketide compound overcomes the defects that similar medicines in the past can not influence a pathological process and specificity can not be determined; a fungus polyketide compound injection medicine is adopted, is a small molecule compound, can penetrate through a blood brain barrier and can act on a pathological process of the alzheimer disease (AD), a decision for developing a medicine used for treating AD at present is met, an Abeta nerve toxic effect can be directly inhibited, and Abeta-induced nerve cell apoptosis is inhibited, namely nerve cell apoptosis is reduced by activating an Akt / GSK-3beta / beta-catenin signal channel.
Owner:THE AFFILIATED DRUM TOWER HOSPITAL MEDICAL SCHOOL OF NANJING UNIV
GSK-3beta inhibitors in the treatment of bone-related diseases
The present invention relates to methods for preventing and / or treating bone-related diseases in mammals, especially humans, using GSK-3β inhibitors. The invention also concerns methods for selecting in vitro and / or in vivo compounds useful for preventing and / or treating bone-related diseases in mammals, including humans.
Owner:PROSKELIA PHARMA
3-substituted-1,5-benzodiazepine compound and pharmaceutical application thereof
ActiveCN110407770AInhibitory activityOrganic active ingredientsNervous disorderBenzeneBenzodiazepine
The invention belongs to the technical field of medicine, and relates to a 3-substituted-1,5-benzodiazepine compound with a general molecular formula of a formula I and application of the 3-substituted-1,5-benzodiazepine compound to medicine. The 3-substituted-1,5-benzodiazepine compound can selectively inhibit the activity of glycogen synthase kinase-3beta (GSK 3beta) and can be used for the preparation of the medicine for preventing and / or treating diseases with abnormal pathological characteristics of the GSK 3beta, wherein the diseases includes cancer, neurological diseases, metabolic syndromes and the like. (Please see the specification for the formula.)
Owner:FUDAN UNIV
Application of lithium preparation in preparation of anti-osteosarcoma medicament
InactiveCN101991600AOrganic active ingredientsInorganic active ingredientsLithium chlorideLithium orotate
The invention relates to new application of a lithium preparation in targeted therapy of osteosarcoma, and belongs to the technical field of medicaments. Shown by experiments, the lithium preparation has remarkable in vivo and in vitro anti-osteosarcoma effects; the effects of the lithium preparation are possibly realized by phosphorylating GSK-3beta (glycogen synthase kinase 3beta) to inhibit the function of the lithium preparation; and when the lithium preparation is used with classical chemotherapeutic adriamycin medicament and the like, the tumor killing effect of the lithium preparation is obviously enhanced. The lithium salt in the lithium preparation is selected from lithium chloride, lithium carbonate, lithium sulfate, lithium citrate, lithium orotate or other pharmaceutical or used lithium salt. The medicament can be orally taken or injected and also can be compounded with other medicaments such as adriamycin to form a compound preparation and when the preparation is prepared, the preparation contains the lithium salt and pharmaceutically acceptable carrier or excipient.
Owner:SUN YAT SEN UNIV
Methods of producing T memory stem cell populations
ActiveUS10316289B2Polypeptide with localisation/targeting motifImmunoglobulin superfamilyMammalGsk 3beta
Provided are methods of producing an isolated T memory stem cell population, the method comprising a) isolating nave T cells from a mammal, wherein the mammal is not a mouse; b) activating the nave T cells and expanding the numbers of nave T cells in the presence of one or more non-specific T cell stimuli, one or more cytokines, and a GSK-3beta inhibitor. Also provided are methods of producing an isolated T memory stem cell population, the method comprising a) isolating lymphocytes from a mammal; b) sorting the lymphocytes using flow cytometry into a population comprising a phenotype comprising i) CD95+, CD45RO−, and CCR7+; and ii) CD62L+ or one or more of CD27+, CD28+, CD45RA+, and CD127+ to produce an isolated T memory stem cell population. Further embodiments of the invention provide related cells, populations of cells, pharmaceutical compositions, and methods of treating or preventing cancer.
Owner:UNITED STATES OF AMERICA
Application of GSK-3beta inhibitor to in-vitro induction of human Breg cells and method for separating and inducing Breg cells
ActiveCN108753714AConform to functional statusWide variety of sourcesBlood/immune system cellsCell culture active agentsCell activityExperimental methods
The invention discloses application of a GSK-3beta inhibitor to in-vitro induction of human Breg cells and a method for inducing the human Breg cells in vitro by the GSK-3beta inhibitor. In the effects of inducing the human Breg cells in vitro by the GSK-3beta inhibitor and inducing transformation of common B cells into the Breg cells by the GSK-3beta inhibitor, the induction purity of inducing the Breg cells by the GSK-3beta inhibitor is high, secretion of Breg inflammatory cytokines is decreased after induction, and the Breg inhibiting function is enhanced after induction. By the method forinducing the human Breg cells in vitro by the GSK-3beta inhibitor, the operation is simple, a short time is consumed, the purity is high, the cell activity damage is high, the transformation efficiency is high, the cell activity is high, a source is wide, the pollution possibility is low, an insufficient amount of Breg in basic and clinical researches can be made up, and a novel experimental method is provided for further research on the Breg cells.
Owner:夏永祥
1,4-disubstituted-2-piperazinone compounds and pharmaceutical use thereof
ActiveCN110396067AEnhanced inhibitory effectOrganic active ingredientsNervous disorderDiseaseMedicine
The invention belongs to the technical field of medicine and relates to a 1,4-disubstituted-2-piperazinone compound having a general structure formula of the formula I, and pharmaceutical use thereof.The compound can selectively inhibit activity of glycogen syntheses kinase 3beta (GSK 3beta), and can be used for preparing medicines preventing and / or treating diseases with GSK 3beta abnormal pathological features, the diseases including cancer, neurological disease, metabolic syndrome and the like.
Owner:FUDAN UNIV
Application of progestational hormone in preparing glycogen synthase kinase-3beta inhibitor medicine, and glycogen synthase kinase-3beta inhibitor
PendingCN108272804AGood inhibitory effectEnhance expressive abilityOrganic active ingredientsRespiratory disorderGsk 3betaProgesterones
The invention discloses application of progestational hormone in preparing a glycogen synthase kinase-3beta (GSK-3beta) inhibitor medicine, and a glycogen synthase kinase-3beta (GSK-3beta) inhibitor,and belongs to the field of medicines. The invention discloses the application of the progestational hormone as an active ingredient in preparing the glycogen synthase kinase-3beta (GSK-3beta) inhibitor medicine; the progestational hormone is selected from one or several of 17alpha-hydroxyprogesterone caproate (17-HPC), medroxyprogesterone (MPA) or natural progesterone (P4). The glycogen synthasekinase-3beta (GSK-3beta) inhibitor taking the progestational hormone as the active ingredient, provided by the invention, is simple in composition, a preparation method is simplified, and the progestational hormone is easy to popularize and promote.
Owner:SHENZHEN EVERGREEN THERAPEUTICS CO LTD
Benzothiazinone compounds, and preparation method and medicinal application thereof
The invention relates to benzothiazinone compounds with a general structural formula as shown in a formula I which is described in the specification, and a preparation method and medicinal applicationthereof, belonging to the field of pharmaceutical chemistry. The benzothiazinone compounds with the general structural formula as shown in the formula I are non-ATP competitive small-molecule inhibitors for glycogen synthase kinase-3beta (GSK-3beta), can selectively inhibit the activity of GSK-3beta and are applicable to preparation of drugs used for preventing or treating diseases related to GSK-3beta. The compounds as shown in the formula I have good in-vivo and in-vitro inhibition activity to tumors and can be used for preparing drugs for preventing or treating tumors. The invention also discloses a synthetic method for the benzothiazinone compounds with the general structural formula as shown in the formula I.
Owner:FUDAN UNIV
2,3-dihydrobenzazapine*compound or its salt and its medical application
ActiveCN103214431BHas inhibitory effectNo obvious inhibitory effectOrganic active ingredientsNervous disorderDiseasePancreas Cancers
The invention belongs to the pharmaceutical chemistry field, and relates to a 2,3-dihydrobenzazapine*compound with a structure shown in a formula I, the 2,3-dihydrobenzazapine*compound is capable of inhibiting glycogen synthase kinase-3beta(GSK-3beta), and is a small-molecule inhibitor of GSK-3beta, a non ATP competition effect mode is taken for inhibiting the activity of GSK-3beta, no obvious inhibition effect is provided on the tested various protein kinase, and the 2,3-dihydrobenzazapine*compound has high kinases selectivity, and can be used for preparing medicines for preventing or treating the diseases due to GSK-3beta abnormity. The invention further comprises an application of a pharmaceutically acceptable salt or a pharmaceutical composition of the compound for preventing or treating the relative diseases to GSK-3beta, the relative diseases to GSK-3beta are diabetes, Alzheimer's disease, stomach cancer, colorectal cancer, pancreas cancer, liver cancer or mixed acute leukemia, but the relative diseases are not limited by the above diseases.
Owner:FUDAN UNIV
Compound, preparation method and application in preparation of GSK-3beta inhibitor
ActiveCN110483508ANovel structureStrong specificityOrganic active ingredientsNervous disorderChemical structureDepolymerization
The invention provides a compound, a preparation method and application of the compound in preparation of a GSK-3 beta inhibitor. The chemical structure of the compound is shown as a formula I shown in the specification. The compound provided by the invention has GSK-3beta inhibition activity, can directly act on A[beta], can inhibit the aggregation of A[beta] and promote depolymerization of A[beta] aggregate, and is a novel GSK-3beta inhibitor. The compound can also inhibit Cu<2+>-induced A[beta] aggregation and depolymerize Cu<2+>-induced A[beta] aggregate, and can act on multiple aspects related to AD pathogenesis in a multi-targeting manner.
Owner:SHANDONG UNIV
Applications of 2,3-dihydro[1,5] benzothiazepine compounds or salts thereof in preparation of GSK-3beta inhibitor
InactiveCN101735211BHas inhibitory effectOrganic active ingredientsNervous disorderDiseaseDiabetes mellitus
The invention belongs to the field of pharmaceutical chemistry, and discloses 2,3-dihydro[1,5] benzothiazepine compounds of non-adenosine triphosphate (ATP) competitive inhibition glycogen synthase kinase-3beta (GSK-3beta) with a structure shown in formula I. The compounds can inhibit the activity of the GSK-3beta in a non ATP competitive mode, and can be used as micromolecule inhibitors of the GSK-3beta for preparing medicines for preventing or treating GSK-3beta related diseases. The invention further provides applications of the compounds, pharmaceutical acceptable salts thereof, or medicine compositions thereof to preventing or treating the GSK-3beta related diseases. The GSK-3beta related diseases can be diabetes and an Alzheimer's disease.
![Applications of 2,3-dihydro[1,5] benzothiazepine compounds or salts thereof in preparation of GSK-3beta inhibitor](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/8077e5c0-bd92-4fe8-a94d-83d331e15c97/H2009101744569E00011.png "Applications of 2,3-dihydro[1,5] benzothiazepine compounds or salts thereof in preparation of GSK-3beta inhibitor")
![Applications of 2,3-dihydro[1,5] benzothiazepine compounds or salts thereof in preparation of GSK-3beta inhibitor](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/8077e5c0-bd92-4fe8-a94d-83d331e15c97/H2009101744569E00012.png "Applications of 2,3-dihydro[1,5] benzothiazepine compounds or salts thereof in preparation of GSK-3beta inhibitor")
![Applications of 2,3-dihydro[1,5] benzothiazepine compounds or salts thereof in preparation of GSK-3beta inhibitor](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/8077e5c0-bd92-4fe8-a94d-83d331e15c97/H2009101744569E00021.png "Applications of 2,3-dihydro[1,5] benzothiazepine compounds or salts thereof in preparation of GSK-3beta inhibitor")
Owner:FUDAN UNIV
Application of AE as medicine for preventing and treating hyperlipemia
InactiveCN109700800AInhibitory activityTo achieve the effect of prevention and treatment of hyperlipidemiaOrganic active ingredientsMetabolism disorderDiseaseNatural source
The invention provides an application of a natural product small molecule AE for preparing a medicine for preventing and treating hyperlipemia diseases. The study results indicate that AE can up-regulate the phosphorylation levels of GSK-3beta and Akt protein on a PTP-1B signaling pathway, thereby can down-regulate the protein level of PTP-1B, can inhibit the activity of PTP-1B, and plays a role in the prevention and treatment of hyperlipidemia. As a natural sourced novel PTP-1B signaling pathway regulator, AE has a good application prospect.
Owner:TIANJIN UNIV OF SCI & TECH
A method of inhibiting fibroblast differentiation of MSCs, MSCs and DNA fragments
ActiveCN107012172BInhibit expressionInhibition of differentiationSkeletal/connective tissue cellsFermentationBeta-cateninFibroblast
Owner:JIANGSU PROVINCIAL CENT FOR DISEASE PREVENTION & CONTROL
GSK-3beta inhibitor and application as novel target spot for diabetic nephropathy intervention
InactiveCN109453191AAvoid damageImprove protectionMetabolism disorderInorganic active ingredientsInjury causeMedicine
The invention belongs to the technical field of medical preparations containing effective components, and discloses application of a GSK-3beta inhibitor as a novel target spot for diabetic nephropathyintervention. According to a method for using the GSK-3beta inhibitor as the novel target spot for diabetic nephropathy intervention, an siRNA technology and an inhibitor of the siRNA technology areused, so that the fact that after expression or activity of GSK-3beta is inhibited, podocyte injury caused by high glucose is relieved to some extent is found, and means that the GSK-3beta participates in a podocyte injury process caused by the high glucose, and plays an important part; studies of animal experiments further prove a conclusion drawn on a cellular level, and the fact that the GSK-3beta inhibitor can relieve podocyte injury, caused by the high glucose, and proteinuria is proven again, so that a novel idea is provided for finding a novel treatment measure of diabetic nephropathy.
Owner:THE FIRST AFFILIATED HOSPITAL OF ZHENGZHOU UNIV
USE OF 7-(PYRIMIDIN-4 YL)-IMIDAZO[1,2-a]PYRIMIDIN-5(1H)-ONES AS GSK-3BETA INHIBITORS
The invention relates to a imidazo[1,2-a]pyrimidone derivative represented by formula (I) or a salt thereof:Wherein:X represents a bond, an ethenylene group, an ethynylene group, a methylene group optionally substituted;a carbonyl group, an oxygen atom, a sulfur atom, a sulfonyl group, a sulfoxide group or a nitrogen atom being optionally substituted;R1 represents a 2, 4 or 5-pyrimidinyl optionally substituted;R2 represents a C1-6 alkyl group, a C1-2 perhalogenated alkyl group, a C1-3 halogenated alkyl group, a benzyl group, a benzene ring, a naphthalene ring, 5,6,7,8-tetrahydronaphthalene ring, a pyridine ring, an indole ring, a pyrrole ring, a thiophene ring, a furan ring or an imidazole ring, the benzyl group and the rings being optionally substituted;and n represents 0 to 3.The invention relates also to a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and / or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3β, such as Alzheimer disease.
![USE OF 7-(PYRIMIDIN-4 YL)-IMIDAZO[1,2-a]PYRIMIDIN-5(1H)-ONES AS GSK-3BETA INHIBITORS](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/baae53b3-89b1-4064-95cc-3da1f678f65a/US20080318980A1-20081225-C00001.png "USE OF 7-(PYRIMIDIN-4 YL)-IMIDAZO[1,2-a]PYRIMIDIN-5(1H)-ONES AS GSK-3BETA INHIBITORS")
![USE OF 7-(PYRIMIDIN-4 YL)-IMIDAZO[1,2-a]PYRIMIDIN-5(1H)-ONES AS GSK-3BETA INHIBITORS](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/baae53b3-89b1-4064-95cc-3da1f678f65a/US20080318980A1-20081225-C00002.png "USE OF 7-(PYRIMIDIN-4 YL)-IMIDAZO[1,2-a]PYRIMIDIN-5(1H)-ONES AS GSK-3BETA INHIBITORS")
![USE OF 7-(PYRIMIDIN-4 YL)-IMIDAZO[1,2-a]PYRIMIDIN-5(1H)-ONES AS GSK-3BETA INHIBITORS](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/baae53b3-89b1-4064-95cc-3da1f678f65a/US20080318980A1-20081225-C00003.png "USE OF 7-(PYRIMIDIN-4 YL)-IMIDAZO[1,2-a]PYRIMIDIN-5(1H)-ONES AS GSK-3BETA INHIBITORS")
Owner:SANOFI SA +1
Use of gsk-3β inhibitor to induce human breg cells in vitro and methods for isolating and inducing breg cells
ActiveCN108753714BWide variety of sourcesLarge baseBlood/immune system cellsCell culture active agentsExperimental methodsCell activity
The invention discloses application of a GSK-3beta inhibitor to in-vitro induction of human Breg cells and a method for inducing the human Breg cells in vitro by the GSK-3beta inhibitor. In the effects of inducing the human Breg cells in vitro by the GSK-3beta inhibitor and inducing transformation of common B cells into the Breg cells by the GSK-3beta inhibitor, the induction purity of inducing the Breg cells by the GSK-3beta inhibitor is high, secretion of Breg inflammatory cytokines is decreased after induction, and the Breg inhibiting function is enhanced after induction. By the method forinducing the human Breg cells in vitro by the GSK-3beta inhibitor, the operation is simple, a short time is consumed, the purity is high, the cell activity damage is high, the transformation efficiency is high, the cell activity is high, a source is wide, the pollution possibility is low, an insufficient amount of Breg in basic and clinical researches can be made up, and a novel experimental method is provided for further research on the Breg cells.
Owner:夏永祥
Dot blotting method for detecting activity of GSK-3beta proteins of human blood platelets
InactiveCN104698188AEasy to operateQuick assessment methodDisease diagnosisBiological testingAntigenHuman platelet
The invention provides a dot blotting method for detecting the activity of GSK-3beta proteins of human blood platelets. The dot blotting method comprises the steps of preparing the proteins of the blood platelets to realize the uniform concentration, drying sample dots on an NC film in air, closing by 5 percent of skim milk powder, then respectively adding primary antibodies for 1: 1000GSK-3beta and Ser9-GSK-3beta, performing dilution, adding 1:10000 fluorescent secondary antibodies marked with IRDyeT 800 channels of the Licor Company, performing dilution again, and finally scanning with fluorescence. According to the antigen and antibody combination reaction theory, the method disclosed by the invention can be used for performing simple and quick quantitative analysis on the activity of the GSK-3beta proteins and can be used for diagnosing and preventing senile dementia.
Owner:HUAZHONG UNIV OF SCI & TECH
Application of CBD as drug for treating METH addiction
PendingCN110339185AAttenuation of the induced CPP phenomenon in ratsUnderstanding PharmacologyNervous disorderHydroxy compound active ingredientsPhosphorylationGsk 3beta
The invention relates to application of cannabidiol as a Sigma1R / AKT / GSK-3beta / CREB signal path inhibitor and as a drug for treating METH addiction. It is found that METH can induce rat CPP, CBD has an inhibitory effect on the METH addiction and phosphorylation of an AKT-GSK3beta-CREB signal path, the CBD can weaken the phenomenon that the METH induces the rat CPP by regulating a Sigma1R / AKT / GSK-3beta / CREB signal path after being in use in advance, and the therapeutic effect of the high-dose CBD (40, 80 mg / kg) is better. The application of the CBD is conductive to knowing the pharmacological effects of the CBD, provides new ways to treat the METH addiction, provides new theoretical guidance for drug abuse mechanism research and withdrawal therapy, and also provides new ideas and options for developing effective drugs for treating drug addiction.
Owner:KUNMING MEDICAL UNIVERSITY
Gsk-3β inhibitor or salt thereof and pharmaceutical use thereof
The invention belongs to the pharmaceutical chemistry field, and discloses a compound for inhibiting glycogen synthase kinase-3beta (GSK-3beta) in a formula I, its pharmaceutically acceptable salt, or an application of its pharmaceutical composition for preventing and treating the GSK-3beta-related diseases. The compound is a GSK-3beta small-molecule inhibitor, its action mode is non-ATP-competitive competition, and can be used for preparing the medicines for preventing and treating the GSK-3beta-related diseases, and the GSK-3beta-related diseases can be diabetes, Alzheimer's disease, stomach cancer, colorectal cancer, pancreas cancer, liver cancer or mixed acute leukemia. According to the compound, R1, R2, R3, X, Y are consistent with detailed description in the invention.
Owner:FUDAN UNIV
3,4-dihydrogen-benzo[f][1,4] thiazepine*-5(2H)-ketones and their applications in medicine
ActiveCN110407769AInhibitory activityNo obvious inhibitory effectOrganic active ingredientsNervous disorderDiseaseThiazepine
The invention belongs to the technical field of medicine and relates to 3,4-dihydrogen-benzo[f][1,4] thiazepine*-5(2H)-ketones with the general structure of formula I and their applications in medicine. These compounds selectively inhibit the activity of glycogen synthesis kinases-3 beta (GSK 3beta), which can be used to prepare medicaments for preventing and / or treating diseases having GSK 3betaabnormal pathological characteristics, such as cancer, neurological diseases, inflammation, metabolic syndrome, and the like.
![3,4-dihydrogen-benzo[f][1,4] thiazepine*-5(2H)-ketones and their applications in medicine](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/f1cc2eb9-f627-4f22-b727-c2f582d22077/HDA0001643495390000011.png "3,4-dihydrogen-benzo[f][1,4] thiazepine*-5(2H)-ketones and their applications in medicine")
![3,4-dihydrogen-benzo[f][1,4] thiazepine*-5(2H)-ketones and their applications in medicine](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/f1cc2eb9-f627-4f22-b727-c2f582d22077/HDA0001643495390000021.png "3,4-dihydrogen-benzo[f][1,4] thiazepine*-5(2H)-ketones and their applications in medicine")
![3,4-dihydrogen-benzo[f][1,4] thiazepine*-5(2H)-ketones and their applications in medicine](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/f1cc2eb9-f627-4f22-b727-c2f582d22077/FDA0001643495370000011.png "3,4-dihydrogen-benzo[f][1,4] thiazepine*-5(2H)-ketones and their applications in medicine")
Owner:FUDAN UNIV
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