43 results about "Wee1" patented technology

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).

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.

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.

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.

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.

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.

A combination of a CHK1 inhibitor and a WEE1 inhibitor are provided.

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.

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.

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.

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.

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.

The invention relates to a pharmaceutical preparation composition containing a WEE1 inhibitor and a preparation method of the pharmaceutical preparation composition. The WEE1 inhibitor is shown as a compound in a formula (I).

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.

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.

The invention relates to a novel chemical synthesis method of a Wee1 protein kinase inhibitor adavisertib. According to the method, the target compound adavisertib is synthesized by adopting the existing commercially easily available intermediate compound through four steps of reaction, namely one-time microwave reaction, two-time halogenation reaction and one-time substitution reaction, so that the total yield and industrial operability of the reaction are effectively improved.