Novel bromodomain and extraterminal domain (BET) inhibitors and to therapeutic methods of treating conditions and diseases using these novel BET inhibitors are provided.
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(2021/01/23)
Compound with BRD4 inhibitory activity, preparation method and application thereof
The invention discloses a compound with BRD4 inhibitory activity, a preparation method and application thereof. The structure of the compound with the BRD4 inhibitory activity is shown as a formula I, and definitions of substituent groups are shown in the specification and claims. The compound provided by the invention has very high bromodomain protein inhibition activity, especially BRD4 targeted inhibition activity, and can be used for treating or/and preventing related diseases mediated by bromodomain protein.
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Paragraph 0848-0853
(2021/04/10)
COMPOUNDS AND USES THEREOF
The present invention relates to compositions and methods for the treatment of BAF-related disorders, such as cancers and viral infections.
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Page/Page column 227
(2020/08/22)
Design, synthesis and SAR of thienopyridines as potent CHK1 inhibitors
A novel series of CHK1 inhibitors based on thienopyridine template has been designed and synthesized. These inhibitors maintain critical hydrogen bonding with the hinge and conserved water in the ATP binding site. Several compounds show single digit nanomolar CHK1 activities. Compound 70 shows excellent enzymatic activity of 1 nM.