955369-56-9Relevant academic research and scientific papers
A new method for the chemical synthesis of the Wee1 protein kinase inhibitor adavosertib
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, (2022/01/12)
The present invention relates to a New Method for the Chemical Synthesis of a Weather1 protein kinase inhibitor adavosertib. The method of the present invention, using an intermediate compound that is commercially readily available, which undergoes a micr
WEE1 Protein degradation agent
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, (2021/09/21)
WEE1 Protein degradation agents are provided. , The invention provides a compound as shown V, or a pharmaceutically acceptable salt thereof, or a stereoisomer, Y-L-M thereof. WEE1 (V) Wherein M. WEE1 A WEE1 binding moiety capable of binding to WEE1 protein kinase is provided. Y Is E3 ubiquitin ligase ligand moiety, and L Is a linking group.
Indoline -1H- pyrazolo [3,4-d] pyrimidinone compound, as well as preparation method and application thereof
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, (2020/03/17)
The present invention relates to a compound of Formula (I), or a pharmaceutically acceptable salt, thereof, which may be better selective Wee1 as a new generation, selective inhibitor Wee1 with respect to the existing, inhibitor Wee1 for, Kinase more safe
DEGRADERS OF WEE1 KINASE
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Paragraph 00127; 00130-00131, (2020/05/12)
Disclosed are bifunctional compounds (degraders) that target Wee1 tyrosine kinase for degradation. Also disclosed are pharmaceutical compositions containing the degraders and methods of using the compounds to treat disease.
HETEROCYCLIC COMPOUNDS AND USES THEREOF
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, (2019/04/25)
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.
1,2-DIHYDRO-3H-PYRAZOLO[3,4-D]PYRIMIDINE-3-ONE COMPOUNDS AS INHIBITORS OF WEE-1 KINASE
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, (2019/09/12)
The disclosure includes compounds of Formula (I) wherein Q, R1, R2, and m are defined herein. Also disclosed is a method for treating a neoplastic disease with these compounds.
WEE1 KINASE INHIBITORS AND METHODS OF TREATING CANCER USING THE SAME
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Page/Page column 43-44; 45, (2019/09/18)
A compound, or a pharmaceutically acceptable salts or prodrugs thereof, having the chemical structure (I) and methods of using these compounds to inhibit WEE1 kinase and treat cancer in a subject.
1,2-DIHYDRO-3H-PYRAZOLO[3,4-D]PYRIMIDIN-3-ONE DERIVATIVE AS WEE1 INHIBITOR
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Paragraph 0117-0119; 0208-0210, (2019/12/09)
The present invention provides a 1,2-dihydro-3H-pyrazolo[3,4-d]pyrimidin-3-one compound having an inhibitory effect on Wee 1, and includes an application of the compound in treating various types of tumors.
Development of Potent Pyrazolopyrimidinone-Based WEE1 Inhibitors with Limited Single-Agent Cytotoxicity for Cancer Therapy
Matheson, Christopher J.,Casalvieri, Kimberly A.,Backos, Donald S.,Reigan, Philip
, p. 1681 - 1694 (2018/08/01)
WEE1 kinase regulates the G2/M cell-cycle checkpoint, a critical mechanism for DNA repair in cancer cells that can confer resistance to DNA-damaging agents. We previously reported a series of pyrazolopyrimidinones based on AZD1775, a known WEE1 inhibitor, as an initial investigation into the structural requirements for WEE1 inhibition. Our lead inhibitor demonstrated WEE1 inhibition in the same nanomolar range as AZD1775, and potentiated the effects of cisplatin in medulloblastoma cells, but had reduced single-agent cytotoxicity. These results prompted the development of a more comprehensive series of WEE1 inhibitors. Herein we report a series of pyrazolopyrimidinones and identify a more potent WEE1 inhibitor than AZD1775 and additional compounds that demonstrate that WEE1 inhibition can be achieved with reduced single-agent cytotoxicity. These studies support that WEE1 inhibition can be uncoupled from the potent cytotoxic effects observed with AZD1775, and this may have important ramifications in the clinical setting where WEE1 inhibitors are used as chemosensitizers for DNA-targeted chemotherapy.
WEE 1 KINASE INHIBITORS AND METHODS OF MAKING AND USING THE SAME
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, (2017/05/17)
A compound, or a pharmaceutically acceptable salt thereof, having a chemical structure of formula (I) or formula (II), and methods of using these compounds to treat cancer in an individual.
