13143-47-0Relevant articles and documents
Design, synthesis and biological evaluation of novel 2,3-dihydroquinazolin- 4(1H)-one derivatives as potential fXa inhibitors
Xing, Junhao,Yang, Lingyun,Yang, Yifei,Zhao, Leilei,Wei, Qiangqiang,Zhang, Jian,Zhou, Jinpei,Zhang, Huibin
, p. 411 - 422 (2017)
Coagulation factor Xa (fXa) is a particularly attractive target for the development of effective and safe anticoagulants. In this study, novel 2,3-dihydroquinazolin-4(1H)-one derivatives were designed as potential fXa inhibitors based on anthranilamide structure which has been reported in our previous research. The experimental data showed that most of the designed compounds exhibited significant in?vitro potency against fXa. Among them, compound 8e displayed the strongest potency against fXa with the IC50value of 21?nM and highly selectivity versus thrombin (IC50?=?67?μM) and excellent in?vitro antithrombotic activity with its 2?×?PT value of 1.2?μM and 2?×?aPTT value of 0.6?μM. In addition, 8e also displayed excellent in?vivo antithrombotic activity in the rat arteriovenous shunt (AV-SHUNT) model. The bleeding risk evaluation showed that 8e had a similar safety profile as that of betrixaban. All results demonstrated that compound 8e could be considered as a potential fXa inhibitor for the prevention and treatment of thromboembolic diseases.
INHIBITORS OF BRUTON'S TYROSINE KINASE
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Paragraph 1127; 1128, (2015/06/17)
Disclosed herein are reversible and irreversible inhibitors of Bruton's tyrosine kinase (Btk). Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are described, alone or in combination with other
NOVEL PYRIMIDINE AND PYRIDINE COMPOUNDS AND USAGE THEREOF
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Page/Page column 37, (2014/09/29)
Provided are novel pyrimidine and pyridine compounds of formula (I) or a pharmaceutical acceptable salt thereof, pharmaceutical compositions containing them, a process for preparing them, and their use in therapy of a disease responsive to inhibition of F