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44 results about "Wee1" patented technology
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Wee1 is a nuclear kinase belonging to the Ser/Thr family of protein kinases in the fission yeast Schizosaccharomyces pombe (S. pombe). Wee1 has a molecular mass of 96 kDa and it is a key regulator of cell cycle progression. It influences cell size by inhibiting the entry into mitosis, through inhibiting Cdk1. Wee1 has homologues in many other organisms, including mammals.
Therapeutic Compounds
The present invention relates to pyrazolopyridines and imidazopyridines which are inhibitors of the kinase PDK1 and are thus useful for the treatment of myeloproliferative disorders or cancer. The compounds are also useful as inhibitors of other kinases such as FGFR3, NTRK3, RP-S6K and WEE1. Furthermore, the present compounds also selectively inhibit microtubule affinity regulating kinase (MARK) and are therefore useful for the treatment or prevention of Alzheimer's disease.
Owner:MERCK SHARP & DOHME CORP +1
Therapeutic compounds
The present invention relates to pyrazolopyridines and imidazopyridines which are inhibitors of the kinase PDK1 and are thus useful for the treatment of myeloproliferative disorders or cancer. The compounds are also useful as inhibitors of other kinases such as FGFR3, NTRK3, RP-S6K and WEE1. Furthermore, the present compounds also selectively inhibit microtubule affinity regulating kinase (MARK) and are therefore useful for the treatment or prevention of Alzheimer's disease.
Owner:MERCK SHARP & DOHME CORP +1
Compositions and methods for treating cancer
The instant invention provides a method of treating a cancer, selected from the group consisting of breast cancer, melanoma, colorectal cancer, non-small cell lung cancer and ovarian cancer, by administering a combination of a WEE1 inhibitor and a CHK1 inhibitor, wherein the WEE1 inhibitor is MK-1775 or a pharmaceutically acceptable salt thereof, or MK-3652 or a pharmaceutically acceptable salt thereof, and the CHK1 inhibitor is MK-8776 or a pharmaceutically acceptable salt thereof, or SCH900444 or a pharmaceutically acceptable salt thereof.
Owner:MERCK SHARP & DOHME LLC
Pyrazolo[3,4-d]pyrimidine-3-ketone derivative as well as drug composition and application thereof
The invention relates to a pyrazolo[3,4-d]pyrimidine-3-ketone derivative as shown in formula (I) or (I') and / or a pharmaceutically-acceptable salt as well as a composition comprising a compound as shown in formula (I) or (I') and / or pharmaceutically-acceptable salt, a preparation method and a use thereof as a Wee1 inhibitor and a use as a sensitizer in a cancer chemical therapy or a cancer radioactive therapy. The pyrazolo[3.4-d]pyrimidine-3-ketone derivative of the invention can effectively inhibit Wee-1 as well as relevant signal channels and has good effect for treating and / or alleviating the cancer. (Shown in the description).
![Pyrazolo[3,4-d]pyrimidine-3-ketone derivative as well as drug composition and application thereof](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/fcbd1225-442f-4736-8c00-49c4e9458a62/HDA0001770064090000011.png "Pyrazolo[3,4-d]pyrimidine-3-ketone derivative as well as drug composition and application thereof")
![Pyrazolo[3,4-d]pyrimidine-3-ketone derivative as well as drug composition and application thereof](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/fcbd1225-442f-4736-8c00-49c4e9458a62/BDA0001770064080000021.png "Pyrazolo[3,4-d]pyrimidine-3-ketone derivative as well as drug composition and application thereof")
![Pyrazolo[3,4-d]pyrimidine-3-ketone derivative as well as drug composition and application thereof](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/fcbd1225-442f-4736-8c00-49c4e9458a62/BDA0001770064080000041.png "Pyrazolo[3,4-d]pyrimidine-3-ketone derivative as well as drug composition and application thereof")
Owner:SHANGHAI DE NOVO PHARMA
Heterocyclic compounds and uses thereof
Heterocyclic compounds as Wee1 inhibitors are provided. The compounds may find use as therapeutic agents for the treatment of diseases and may find particular use in oncology.
Owner:NUVATION BIO INC
Pyrazolone pyrimidine compound as well as preparation method and application thereof
PendingCN109810111AStrong inhibitory activityOrganic chemistryAntineoplastic agentsMetaboliteEnantiomer
The invention discloses a pyrazolone pyrimidine compound as well as a preparation method and application thereof. The invention provides the pyrazolone pyrimidine compound shown as a formula I, and anenantiomer, a diastereomer, a tautomer, a crystal form, a medically acceptable salt, a solvent compound, a metabolite or a prodrug thereof. The inhibition activity of the compound on WEE1 kinase is high. The formula I is shown in the description.
Owner:SHANGAI PHARMA GRP CO LTD
Heterocyclic compounds and uses thereof
Heterocyclic compounds as Wee1 inhibitors are provided. The compounds may find use as therapeutic agents for the treatment of diseases and may find particular use in oncology.
Owner:NUVATION BIO INC
Dihydroisoindole-1H-pyrazolo[3,4-d]pyrimidone compound, and preparation method and application thereof
ActiveCN110872296AGood choiceGood blood-brain barrier permeabilityOrganic chemistryMetabolism disorderIsoindolesDepressant
The invention relates to a series of compounds represented as the formula (I), or pharmaceutically acceptable salts thereof, which can be used as new-generation Wee1 selective inhibitor. Compared withexisting Wee1 inhibitor, the compound has a higher selectivity on Wee1 kinase, so that the compound is safer and is higher in treatment index, and also has higher blood brain barrier permeability. The compound has better safety and a larger applicable range, and can be applied to treatment on various tumors, including brain tumor.
![Dihydroisoindole-1H-pyrazolo[3,4-d]pyrimidone compound, and preparation method and application thereof](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/21cf7138-1159-4bb1-8979-ccebc699e72a/FDA0001785167610000011.png "Dihydroisoindole-1H-pyrazolo[3,4-d]pyrimidone compound, and preparation method and application thereof")
![Dihydroisoindole-1H-pyrazolo[3,4-d]pyrimidone compound, and preparation method and application thereof](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/21cf7138-1159-4bb1-8979-ccebc699e72a/FDA0001785167610000031.png "Dihydroisoindole-1H-pyrazolo[3,4-d]pyrimidone compound, and preparation method and application thereof")
![Dihydroisoindole-1H-pyrazolo[3,4-d]pyrimidone compound, and preparation method and application thereof](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/21cf7138-1159-4bb1-8979-ccebc699e72a/FDA0001785167610000041.png "Dihydroisoindole-1H-pyrazolo[3,4-d]pyrimidone compound, and preparation method and application thereof")
Owner:上海弘翊生物科技有限公司 +1
Chemical Compounds
The present invention relates to dianilinopyrimidine derivatives, compositions and medicaments containing the same, as well as processes for the preparation and use of such compounds, compositions and medicaments. Such dianilinopyrimidine derivatives are useful in the treatment of diseases associated with inappropriate Wee1 kinase activity.
Owner:SMITHKLINE BECKMAN CORP
Bicycloaniline derivative
InactiveCN101784551AExcellent Wee1 Kinase InhibitionOrganic chemistryAntineoplastic agentsAnticarcinogenAniline
Disclosed are: a compound represented by the general formula (I); and others. (I) wherein A1 and A2 independently represent a nitrogen atom or a methine group which may be substituted; the ring B represents a 5- to 7-membered aliphatic ring or a spiro or bicyclo ring formed by the aliphatic ring and a 3- to 7-membered aliphatic ring which is different from the aforementioned aliphatic ring; R1 represents a hydrogen atom, a C1-C6 alkyl group which may be substituted or an aryl, aralkyl or heteroaryl group which may be substituted; R2 represents an aryl, aralkyl or heteroaryl group which may be substituted; and X represents a group represented by the formula =NH or =O. The compound has an excellent cell proliferation inhibition activity relying on a Wee1 kinase inhibition activity and an additive / synergistic effect with other anti-cancer agent, and is therefore useful in the medical field.
Owner:บันยิว ฟาร์มาซูติคัล โค แอลทีดี
Pyrimidine derivative used as Wee1 inhibitor
InactiveCN112442049AOrganic active ingredientsOrganic chemistryCombinatorial chemistryPharmaceutical medicine
The invention discloses a pyrimidine derivative used as a Weel inhibitor. The invention relates to a novel compound shown as a formula (1A) or a formula (1B) and / or pharmaceutically acceptable salt thereof, a composition containing the compound shown as the formula (1A) or the formula (1B) and / or pharmaceutically acceptable salt thereof, a preparation method and application of the compound servingas a Wee1 inhibitor in preparation of antitumor drugs.
Owner:WIGEN BIOMEDICINE TECH SHANGHAI CO LTD
Novel compounds
InactiveUS20190210996A1Organic active ingredientsOrganic chemistryProtein-Tyrosine KinasesBruton's tyrosine kinase
A method of treating disorders associated with aberrant kinase activity, wherein the kinase is. Adaptor-associated protein kinase 1 (AAK1), Aurora Kinase A (AURKA), Aurora Kinase B (AURKB), Bruton's Tyrosine Kinase (BTK), Interleukin-1 receptor-associated kinase 3 (IRAK3), Protein tyrosine kinase 2 beta (PTK2B), Tyrosine-protein kinase Tec (TEC), Serine / threonine-protein kinase Wee1 (WEE1), Cyclin G-associated kinase (GAK), Large Tumour suppressor 1 Kinase (LATS1), Focal Adhesion Kinase (PTK2), Ribosomal protein S6 kinase alpha-1 (RPS6KA1) said method comprising degrading said kinase.
Owner:GLAXOSMITHKLINE INTPROP DEV LTD
WEE1 protein degradation agent
InactiveCN113402520ANo degradationGood choiceOrganic active ingredientsOrganic chemistryUbiquitin ligasePharmaceutical medicine
The invention provides a WEE1 protein degradation agent. Specifically, the invention provides a compound as shown in a formula V, or a pharmaceutically acceptable salt thereof, or a stereoisomer thereof, Y-L-MWEE1 (V), in which MWEE1 is a WEE1 binding part capable of being bound with WEE1 protein kinase; the Y is an E3 ubiquitin ligase ligand part; and L is a linking group.
Owner:SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
Combination of checkpoint kinase i inhibitors and wee i kinase inhibitors
Owner:ARRAY BIOPHARMA
Application of tetrahydropyrido[4,5-]thieno[2,3-]pyrimidin-4(3)-one compound in pharmacy
The invention provides a pharmaceutical composition using tetrahydropyrido[4,5-]thieno[2,3-]pyrimidin-4(3)-one compound as an active ingredient, and application thereof in the preparation of Wee1 small-molecular inhibitor. Wee1 kinase serves as a candidate drug target for tumor treatment; it is possible to enhance the antitumor activity of the Wee1 kinase by the joint use of its inhibitors with certain chemotherapy drugs. Up to now, and there is only one Wee1 small-molecular inhibitor is under clinical test phase; in-vitro antitumor activity screening shows that the compound of the invention shows good inhibitory activity for five different tumor strains. The compound is applicable to the development of novel Wee1 small-molecular inhibitors, a new choice is provided for the field of tumor treatment, and the compound has good applicable value.
![Application of tetrahydropyrido[4,5-]thieno[2,3-]pyrimidin-4(3)-one compound in pharmacy](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/213858d3-b5d1-42f1-aba4-5d91cc8335d4/HDA0001366546330000011.png "Application of tetrahydropyrido[4,5-]thieno[2,3-]pyrimidin-4(3)-one compound in pharmacy")
![Application of tetrahydropyrido[4,5-]thieno[2,3-]pyrimidin-4(3)-one compound in pharmacy](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/213858d3-b5d1-42f1-aba4-5d91cc8335d4/BDA0001366546320000021.png "Application of tetrahydropyrido[4,5-]thieno[2,3-]pyrimidin-4(3)-one compound in pharmacy")
![Application of tetrahydropyrido[4,5-]thieno[2,3-]pyrimidin-4(3)-one compound in pharmacy](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/213858d3-b5d1-42f1-aba4-5d91cc8335d4/BDA0001366546320000042.png "Application of tetrahydropyrido[4,5-]thieno[2,3-]pyrimidin-4(3)-one compound in pharmacy")
Owner:KUNMING INST OF BOTANY - CHINESE ACAD OF SCI +1
Pyrazolone-fused pyrimidine compound as well as preparation method and application thereof
PendingCN112142748AStrong inhibitory activityImprove bioavailabilityOrganic active ingredientsOrganic chemistryWee1Pyrimidine
The invention discloses a pyrazolone-fused pyrimidine compound as well as a preparation method and application thereof. The invention provides a pyrazolone-fused pyrimidine compound as shown in a formula I which is described in the specification. The pyrazolone-fused pyrimidine compound has better inhibitory activity on WEE1 kinase.
Owner:SHANGAI PHARMA GRP CO LTD
Pyrazolone-fused pyrimidine compound as well as preparation method and application thereof
PendingCN112142747AStrong inhibitory activityImprove bioavailabilityOrganic active ingredientsOrganic chemistryCombinatorial chemistryKinase
The invention discloses a pyrazolone-fused pyrimidine compound as well as a preparation method and application thereof. The invention provides a pyrazolone-fused pyrimidine compound as shown in a formula II which is described in the specification. The pyrazolone-fused pyrimidine compound has better inhibitory activity on WEE1 kinase.
Owner:SHANGAI PHARMA GRP CO LTD
Cytidine deaminase inhibitors for the treatment of pancreatic cancer
InactiveUS20190076464A1High affinityStrong specificityCompound screeningOrganic active ingredientsAdenosine Deaminase InhibitorCancer cell
The present invention relates to methods and pharmaceutical compositions for use in the treatment of pancreatic cancer in a subject in need thereof. The inventors showed that targeting cytidine deaminase sensitizes cancer cells to chemotherapy (gemcitabine dFdC) both in vitro and in vivo in experimental models of PDA, with very high efficacy. To their surprise, CDA targeting in the absence of chemotherapy strongly alters cell proliferation and tumor progression. In particular, the present invention relates to a method for treating pancreatic cancer in a subject in need thereof comprising administering to the subject a therapeutically effective amount of a cytidine deaminase inhibitor in combination with an anti-pancreatic cancer treatment selected from the group consisting of CHK1 inhibitor, WEE1 inhibitor, ART inhibitor, DHODH inhibitor or gene therapy.
Owner:INST NAT DE LA SANTE & DE LA RECHERCHE MEDICALE (INSERM) +1
Heterocyclic compounds and uses thereof
Heterocyclic compounds as Wee1 inhibitors are provided. The compounds may find use as therapeutic agents for the treatment of diseases and may find particular use in oncology.
Owner:NUVATION BIO IN
Predictive biomarkers useful for cancer therapy mediated by a wee1 inhibitor
InactiveUS20120157342A1Microbiological testing/measurementLibrary screeningPredictive biomarkerCancer therapy
The present invention provides the identification of biomarker gene sets whose expression levels are useful for predicting a patient's response to a therapeutically effective dose of a Wee1 inhibitor as well the ability to predict said response prior to dosing with the Wee1 inhibitor. Additional uses are also disclosed in the specification.
Owner:MSD KK
Heterocyclic compounds and uses thereof
Heterocyclic compounds as Wee1 inhibitors are provided. The compounds may find use as therapeutic agents for the treatment of diseases and may find particular use in oncology.
Owner:NUVATION BIO INC
Application of tetrahydropyrido[4,5-]thieno[2,3-]pyrimidin-4(3)-ones in pharmacy
The invention provides a pharmaceutical composition using tetrahydropyrido[4,5-]thieno[2,3-]pyrimidin-4(3)-one compound as an active ingredient, and application thereof in the preparation of Wee1 small-molecular inhibitor. Wee1 kinase serves as a candidate drug target for tumor treatment; it is possible to enhance the antitumor activity of the Wee1 kinase by the joint use of its inhibitors with certain chemotherapy drugs. Up to now, and there is only one Wee1 small-molecular inhibitor is under clinical test phase; in-vitro antitumor activity screening shows that the compound of the invention shows good inhibitory activity for five different tumor strains. The compound is applicable to the development of novel Wee1 small-molecular inhibitors, a new choice is provided for the field of tumor treatment, and the compound has good applicable value.
![Application of tetrahydropyrido[4,5-]thieno[2,3-]pyrimidin-4(3)-ones in pharmacy](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/11748ccd-21ee-4d3d-af31-d57358d30a93/HDA0001366546330000011.png "Application of tetrahydropyrido[4,5-]thieno[2,3-]pyrimidin-4(3)-ones in pharmacy")
![Application of tetrahydropyrido[4,5-]thieno[2,3-]pyrimidin-4(3)-ones in pharmacy](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/11748ccd-21ee-4d3d-af31-d57358d30a93/BDA0001366546320000021.png "Application of tetrahydropyrido[4,5-]thieno[2,3-]pyrimidin-4(3)-ones in pharmacy")
![Application of tetrahydropyrido[4,5-]thieno[2,3-]pyrimidin-4(3)-ones in pharmacy](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/11748ccd-21ee-4d3d-af31-d57358d30a93/BDA0001366546320000042.png "Application of tetrahydropyrido[4,5-]thieno[2,3-]pyrimidin-4(3)-ones in pharmacy")
Owner:KUNMING INST OF BOTANY - CHINESE ACAD OF SCI +1
Combinations of chk1- and wee1- inhibitors
InactiveUS20200108074A1Reduce tumor volumeProlong survival timeAntineoplastic agentsHeterocyclic compound active ingredientsChemical compoundPharmaceutical drug
In one aspect, the present invention provides a method for preventing or treating cancer in a subject. In some embodiments, the method comprises administering a therapeutically effective amount of the Chk1 inhibitor Compound 1. In other embodiments, the method further comprises administering a therapeutically effective amount of a Wee1 inhibitor. Pharmaceutical compositions and kits are also provided herein.
Owner:SEATTLE GENETICS INC
Heterocyclic compounds and uses thereof
Heterocyclic compounds as Wee1 inhibitors are provided. The compounds may find use as therapeutic agents for the treatment of diseases and may find particular use in oncology.
Owner:NUVATION BIO INC
Pharmaceutical preparation composition containing WEE1 inhibitor and preparation method thereof
PendingCN114831993AOrganic active ingredientsPill deliveryCombinatorial chemistryPharmaceutical formulation
Owner:SHOUYAO HLDG BEIJING CO LTD
Combination of antibody-drug conjugate and kinase inhibitor
PendingUS20220040324A1ImmunoglobulinsPharmaceutical non-active ingredientsAntiendomysial antibodiesDrug conjugation
A pharmaceutical composition wherein an antibody-drug conjugate in which a drug-linker of the represented formula (wherein A represents a connecting position to an antibody) is conjugated to the antibody via a thioether bond and a kinase inhibitor (at least one selected from the group consisting of a CDK4 / 6 inhibitor, an mTOR inhibitor, a PI3K inhibitor, an AKT inhibitor, an ERK inhibitor, an MEK inhibitor, an RAF inhibitor, a CDK1 inhibitor, a CDK2 inhibitor, a CHK1 inhibitor, a WEE1 inhibitor, a PLK1 inhibitor, an Aurora kinase inhibitor, a Bcr-Abl inhibitor, an Src inhibitor, an EPH inhibitor, a VEGFR inhibitor, a KIT inhibitor, an RET inhibitor, a PDGFR inhibitor, an FGFR inhibitor, a BTK inhibitor, an FLT3 inhibitor, an ALK inhibitor, a JAK inhibitor, an MET inhibitor, a CSF-1R inhibitor, an NTRK inhibitor, an EGFR inhibitor, and an HER2 inhibitor) are administered in combination, and / or a method of treatment.
Owner:DAIICHI SANKYO CO LTD
Pyrazolone-fused pyrimidine compound as well as preparation method and application thereof
PendingCN112142763AStrong inhibitory activityImprove bioavailabilityOrganic active ingredientsOrganic chemistryCombinatorial chemistryKinase
The invention discloses a pyrazolone-fused pyrimidine compound as well as a preparation method and application thereof. The invention provides a pyrazolone-fused pyrimidine compound as shown in a formula A which is described in the specification. The pyrazolone-fused pyrimidine compound has better inhibitory activity on WEE1 kinase.
Owner:SHANGAI PHARMA GRP CO LTD
Heterocyclic compounds and uses thereof
Heterocyclic compounds as Wee1 inhibitors are provided. The compounds may find use as therapeutic agents for the treatment of diseases and may find particular use in oncology.
Owner:GIRAFPHARMA LLC
1,2-dihydro-3H-pyrazolo[3,4-d]pyrimidin-3-one derivative as Wee1 inhibitor
ActiveUS10954253B2Enhanced inhibitory effectHigh indexOrganic active ingredientsOrganic chemistryPerylene derivativesWee1
The present invention provides a 1,2-dihydro-3H-pyrazolo[3,4-d]pyrimidin-3-one compound having an inhibitory effect on Wee1, and includes an application of the compound in treating various types of tumors.
![1,2-dihydro-3H-pyrazolo[3,4-d]pyrimidin-3-one derivative as Wee1 inhibitor](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/6e786372-8274-4627-abe7-15de797626f0/US10954253-C00001.png "1,2-dihydro-3H-pyrazolo[3,4-d]pyrimidin-3-one derivative as Wee1 inhibitor")
![1,2-dihydro-3H-pyrazolo[3,4-d]pyrimidin-3-one derivative as Wee1 inhibitor](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/6e786372-8274-4627-abe7-15de797626f0/US10954253-C00002.png "1,2-dihydro-3H-pyrazolo[3,4-d]pyrimidin-3-one derivative as Wee1 inhibitor")
![1,2-dihydro-3H-pyrazolo[3,4-d]pyrimidin-3-one derivative as Wee1 inhibitor](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/6e786372-8274-4627-abe7-15de797626f0/US10954253-C00003.png "1,2-dihydro-3H-pyrazolo[3,4-d]pyrimidin-3-one derivative as Wee1 inhibitor")
Owner:WUXI BIOCITY BIOPHARMACEUTICS CO LTD
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