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30 results about "Atp competitive" patented technology
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CDK inhibitor for the treatment of mesothelioma
ActiveUS8912194B2Prevent proliferationOrganic active ingredientsOrganic chemistryMesotheliomaCDK inhibitor
Owner:NERVIANO MEDICAL SERVICES SRL
Use of CDK inhibitor for the treatment of glioma
ActiveUS8946226B2Prevent proliferationReduce molecular weightOrganic active ingredientsOrganic chemistryGlioblastomaCytotoxicity
Owner:NERVIANO MEDICAL SERVICES SRL
Use of small molecule inhibitors/activators in combination with (DEOXY)nucleoside or (DEOXY)nucleotide analogs for treatment of cancer and hematological malignancies or viral infections
InactiveUS20150290235A1Good treatment effectLow toxicityBiocideCarbohydrate active ingredientsPTK InhibitorsAnticarcinogen
A method for treating patients afflicted with cancer (including hematological malignancies) or viral infections, wherein the patients are under treatment or are to be treated with at least one anticancer or antiviral agent, and in particular (deoxy)nucleotide or (deoxy)nucleoside analog drugs, includes administering at least one small molecule inhibitor / activator (including ATP competitive inhibitors, signal transduction inhibitors / activators, protein kinase inhibitors / activators, and tyrosine kinase inhibitors / activators) in combination with the (deoxy) nucleotide or (deoxy)nucleoside analog, and wherein the small molecule inhibitor / activator is administered in sufficient amount to modulate deoxynucleotide or deoxynucleoside kinase activity (and in particular deoxycytidine kinase activity) to modulate activation of the (deoxy)nucleotide or (deoxy)nucleoside analog in vivo with a subsequent therapeutically beneficial anticancer or antiviral effect. The combined treatments together include a therapeutically effective amount.
Owner:AB SCIENCE
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/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/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/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
Use of cdk inhibitor for the treatment of glioma
ActiveUS20110190311A1Prevent proliferationReduce molecular weightOrganic active ingredientsOrganic chemistryGlioblastomaCytotoxicity
The invention provides a low molecular weight ATP-competitive CDK inhibitor able to cross the blood brain barrier for use in the treatment of malignant glioma and, in particular, of glioblastoma. The compound can be administered together with one or more agents selected from the group consisting of cytotoxic or cytostatic agents and ionizing radiation.
Owner:NERVIANO MEDICAL SERVICES SRL
Preparation of two novel non-ATP (Adenosine Triphosphate) competitive FGFR1 (Fibroblast Growth Factor Receptor1) inhibitors and anti-tumor activity of two novel non-ATP competitive FGFR1 inhibitors
InactiveCN103214472AStrong inhibitory activityGood kinase selectivityOrganic active ingredientsOrganic chemistryWilms' tumorAntitumor activity
The invention provides FGFR1 (Fibroblast Growth Factor Receptor1) non-ATP (Adenosine Triphosphate) competitive inhibitor acrylamide compounds. Besides, the invention also provides a medicine composite of the compounds, anti-tumor application of the compounds, and the like.
Owner:WENZHOU MEDICAL UNIV
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/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/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/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
Treatment of Drug-Resistant Proliferative Disorders
α,β-Unsaturated sulfones, sulfoxides and sulfonamides according to Formula I:wherein Ar1, Ar2, X, n, * and R are as defined herein are useful for the treatment of proliferative disorders which are resistant to treatment by ATP-competitive kinase inhibitors.
Owner:TEMPLE UNIVERSITY
Application of mTOR signal path inhibitor to preparation of medicament for preventing or treating extragenetic hearing impairment
InactiveCN108310386AAvoid damageImprove hearingOrganic active ingredientsSenses disorderEverolimusMTOR signaling pathway
The invention discloses application of a mTOR signal path inhibitor to preparation of a medicament for preventing or treating extragenetic hearing impairment. The mTOR signal path inhibitor is selected from at least one of sirolimus, sirolimus analogue and second-generation mTOR signal path inhibitor; the sirolimus analogue is selected from at least one of everolimus, temsirolimus and Deforolimus;the second-generation mTOR signal path inhibitor is selected from at least one of PI3K / mTOR double inhibitor, selective mTORC1 / 2 inhibitor and ATP competitive mTOR kinase inhibitor. As found by the inventor of the application, the mTOR signal path inhibitor can effectively relieve damage to inner ear hair cells and spiral ganglion cells caused by non-genetic factors such as ototoxic drug, remarkably improve the impaired listening ability, and effectively prevent and treat extragenetic hearing impairment.
Owner:SOUTHERN MEDICAL UNIVERSITY
Application of desloratadine in preparation of medicine taking TGF-beta I type receptor as target spot
PendingCN113628677AInhibitory activityPrevent proliferationMolecular designInstrumentsReceptorFibrosis
Owner:LIAONING UNIVERSITY
Use of a kinase inhibitor for the treatment of particular resistant tumors
InactiveUS20100022532A1High affinitySignificant inhibitory potencyBiocideMicrobiological testing/measurementDiseaseInhibitory potency
The invention provides low molecular weight compounds, namely 1H-thieno[2,3-c]pyrazoles, showing a high affinity for the ATP pocket of ABL tyrosine kinase. These compounds are thus ATP-competitive tyrosine kinase inhibitors displaying a significant inhibitory potency also, and in particular, towards BCR-ABL inhibitor-resistant T315I ABL mutants. The compounds of the invention find a useful application in the treatment of BCR-ABL inhibitor-resistant ABL-mediated diseases, such as Imatinib-resistant chronic myelogenous leukemia. Moreover, the invention provides a screening method for the identification of compounds capable of binding the ATP pocket of a kinase protein, in particular of the T315I mutant ABL kinase.
Owner:NERVIANO MEDICAL SCI
Combination of an atp-competitive inhibitor of bcr/abl kinase activity and a tyrphostin analog
The present invention relates to a combination of (a) an ATP-competitive inhibitor of Bcr / abl kinase activity and (b)) a tyrphostin analog, and the use of said combination or product for the treatment of bcr / abl-related diseases.
Owner:KAUFMANN SCOTTH +1
Combinations of (a) an atp-competitive inhibitor of c-acl kinase activity with (b) two or more other antineoplastic agents
InactiveUS20050113384A1Low host toxicityImprove anti-tumor effectOrganic active ingredientsAntineoplastic agentsDiseaseKinase activity
The invention relates to combinations of (a) an ATP-competitive inhibitor of c-abl kinase activity with (b) two or more other antineoplastic agents for simultaneous, separate or sequential use, in particular for the delay of progression or treatment of a proliferative disease.
Owner:AVRAMIS IOANNIS ALEXANDER
Therapeutic methods and compositions involving allosteric kinase inhibition
Owner:AMITECH THERAPEUTIC SOLUTIONS
One is the synthesis method of ATP competitive small molecule AKT inhibitor A443654
ActiveCN104610229BReduced reaction time for preparationHigh yieldOrganic chemistryBulk chemical productionSynthesis methodsSuzuki reaction
The invention discloses a synthesis method of an ATP competitive small-molecule AKT inhibitor A443654. According to the method, a compound 1 is used as a starting raw material, and the compound 6 (A-443654) is obtained through amino group protection, Suzuki reaction and protecting group removal. Usage of poisonous reagent hexamethylditin is avoided, the method is high in safety, environment-friendly, high in reaction yield and suitable for industrial large-scale production, the reaction time is shortened, and the process cost is reduced. The flow chart of the synthesis method is shown in the specification.
Owner:SHANGHAI HAOYUAN MEDCHEMEXPRESS CO LTD +1
Combinations of (a) an atp-competitive inhibitor of c-abl kinase activity with (b) two or more other antineoplastic agents
InactiveUS20090239878A1Strong synergyRemarkable effectOrganic active ingredientsAntineoplastic agentsDiseaseKinase activity
Owner:AVRAMIS IOANNIS ALEXANDER +1
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
Combinations of (a) an ATP-competitive inhibitor of c-acl kinase activity with (b) two or more other antineoplastic agents
InactiveCN1713922AReduce deteriorationReduce incidenceOrganic active ingredientsAntineoplastic agentsKinase activityCompetitive inhibitor
The invention relates to combinations of (a) an ATP-competitive inhibitor of c-abl kinase activity with (b) two or more other antineoplastic agents for simultaneous, separate or sequential use, in particular for the delay of progression or treatment of a proliferative disease
Owner:NOVARTIS AG +1
Use of a kinase inhibitor for the treatment of particular resistant tumors
Owner:NERVIANO MEDICAL SERVICES SRL
A kind of non-ATP competitive FGFR1 inhibitor and its application
The invention belongs to the field of pharmacy and particularly relates to application of a specific non-ATP-competiveness FGFR1 (fibroblast growth factor receptor 1) inhibitor in preparing anticancer medicine and medicine for treating cancer-related diseases. The invention further relates to a small molecule compound L16H50 which can inhibit FGFR1 and activation of a signal channel of the FGFR1 in a non-ATP-dependent mode. Therefore, multiplication and survival of cancer cells are inhibited, and good in-vitro and in-vivo anticancer effects are further given to play.
Owner:WENZHOU MEDICAL UNIV
Treatment of hematological neoplasms
Hematological neoplasms resistant to treatment with an ATP-competitive inhibitor of BCR-ABL are treated by administration of N6-benzyladenosine, N6-benzyladenosine-5′-monophosphate, or pharmaceutically acceptable salts thereof.
Owner:THOMAS JEFFERSON 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
![Applications of 2,3-dihydro[1,5] benzothiazepine compounds or salts thereof in preparation of GSK-3beta inhibitor](https://images-eureka.patsnap.com/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/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/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
Use of kinase inhibitor for the treatment of thymoma
ActiveUS8580793B2Reduce lesionsOrganic active ingredientsOrganic chemistryRho kinase inhibitorKinase inhibition
Owner:NERVIANO MEDICAL SERVICES SRL
Use of a kinase inhibitor for the treatment of particular resistant tumors
Owner:NERVIANO MEDICAL SERVICES SRL
Use of a Kinase Inhibitor for the Treatment of Particular Resistant Tumors
The invention provides low molecular weight compounds, namely tetrahydropyrrolo[3,4-c]pyrazoles, showing a high affinity for the ATP pocket of ABL tyrosine kinase. These compounds are thus ATP-competitive tyrosine kinase inhibitors displaying a significant inhibitory potency also, and in particular, towards BCR-ABL inhibitor-resistant T315I ABL mutants. The compounds of the invention find a useful application in the treatment of BCR-ABL inhibitor-resistant ABL-mediated diseases, such as Imatinib-resistant chronic myelogenous leukemia. Moreover, the invention provides a screening method for the identification of compounds capable of binding the ATP pocket of a kinase protein, in particular of the T315I mutant ABL kinase.
Owner:NERVIANO MEDICAL SERVICES SRL
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
Synthesis method of ATP competitive small-molecule AKT inhibitor A443654
ActiveCN104610229AReduce usageReduced reaction time for preparationOrganic chemistryBulk chemical productionSuzuki reactionSynthesis methods
The invention discloses a synthesis method of an ATP competitive small-molecule AKT inhibitor A443654. According to the method, a compound 1 is used as a starting raw material, and the compound 6 (A-443654) is obtained through amino group protection, Suzuki reaction and protecting group removal. Usage of poisonous reagent hexamethylditin is avoided, the method is high in safety, environment-friendly, high in reaction yield and suitable for industrial large-scale production, the reaction time is shortened, and the process cost is reduced. The flow chart of the synthesis method is shown in the specification.
Owner:SHANGHAI HAOYUAN MEDCHEMEXPRESS CO LTD +1
Use of kinase inhibitor for the treatment of thymoma
ActiveUS20120077819A1Reduce lesionsOrganic active ingredientsOrganic chemistryCDK inhibitorKinase inhibition
The invention provides a low molecular weight ATP-competitive CDK inhibitor and TRKA inhibitor of formula (I) for use in the treatment of thymoma and thymic carcinoma. The compound can be administered together with one or more cytotoxic or cytostatic agents.
Owner:NERVIANO MEDICAL SERVICES SRL
![3,4-dihydrobenzo[f][1,4]thiazepine compound or salts of same and medical use of same](https://images-eureka.patsnap.com/patent_img/fce3fd91-3d53-4f4f-8b40-0b65a6697063/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/patent_img/fce3fd91-3d53-4f4f-8b40-0b65a6697063/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/patent_img/fce3fd91-3d53-4f4f-8b40-0b65a6697063/FDA00002933329500012.PNG "3,4-dihydrobenzo[f][1,4]thiazepine compound or salts of same and medical use of same")
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