- Design, synthesis and biological evaluation of novel 2,3-dihydroquinazolin- 4(1H)-one derivatives as potential fXa inhibitors
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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.
- Xing, Junhao,Yang, Lingyun,Yang, Yifei,Zhao, Leilei,Wei, Qiangqiang,Zhang, Jian,Zhou, Jinpei,Zhang, Huibin
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- Preparation method for 1-(4-aminophenyl)-1H-pyridin-2-one
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The invention relates to a preparation method for 1-(4-aminophenyl)-1H-pyridin-2-one. The preparation method comprises the steps that reflux reaction is carried out on paraiodoaniline and 2-hydroxypyridine under the presence of 8-hydroxyquinoline, potassi
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Paragraph 0021; 0022
(2018/03/13)
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- INHIBITORS OF BRUTON'S TYROSINE KINASE
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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
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Paragraph 1127; 1128
(2015/06/17)
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- ANTIVIRAL COMPOUNDS
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The present invention discloses compounds of Formula (I): wherein the variables in Formula (I) are defined as described herein. Also disclosed are pharmaceutical compositions containing such compounds and methods for using the compounds of Formula (I) in the prevention or treatment of HCV infection.
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- NOVEL PYRIMIDINE AND PYRIDINE COMPOUNDS AND USAGE THEREOF
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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
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Page/Page column 37
(2014/09/29)
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- NOVEL PYRIMIDINE AND PYRIDINE COMPOUNDS AND THEIR USAGE
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The present invention relates to novel pyrimidine and pyridine compounds of formula (I) or a pharmaceutical acceptable salt thereof, wherein R1, R2, R3, R4, R5, X, Y and G are as defined in the description, to pharmaceutical compositions containing them, a process for preparing them, and their use in therapy of a disease responsive to inhibition of FGFR, for example, cancer.
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Page/Page column 38
(2014/09/29)
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- NOVEL PIPERAZINE DERIVATIVES AS INHIBITORS OF STEAROYL-CoA DESATURASE
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The present invention relates to piperazine derivatives that act as inhibitors of stearoyl-CoA desaturase. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.
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Page/Page column 31
(2009/10/01)
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- FACTOR XA INHIBITORS
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The present invention is directed to compounds represented by Formula (I) or a pharmaceutically acceptable salt, ester, or prodrug thereof which are inhibitors of Factor Xa. The present invention is also directed to intermediates used in making such compounds, pharmaceutical compositions containing such compounds, methods to prevent or treat certain conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.
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Page/Page column 123-124
(2008/12/07)
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- TETRAHYDROISOQUINOLINES AS FACTOR XA INHIBITORS
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The present invention is directed to compounds represented by Formula I and pharmaceutically acceptable salts, solvates, hydrates, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to and intermediates used in making such compounds, pharmaceutical compositions containing such compounds, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.
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Page/Page column 59
(2008/06/13)
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- UREAS AS FACTOR XA INHIBITORS
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The present invention is directed to compounds represented by Formula (I) and pharmaceutically acceptable salts, solvates, hydrates, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to and intermediates used in making such compounds, pharmaceutical compositions containing such compounds, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.
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Page/Page column 118
(2010/11/08)
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- THIOUREAS AS FACTOR Xa INHIBITORS
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The present invention is directed to compounds represented by Formula (I) and pharmaceutically acceptable salts, solvates, hydrates, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to and intermediates used in making such compounds, pharmaceutical compositions containing such compounds, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.
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Page/Page column 48-49
(2010/11/08)
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- Cyclic beta-amino acid derivatives as factor Xa inhibitors
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The present application describes cyclic β-amino acid derivatives or pharmaceutically acceptable salt forms thereof, wherein the central core is a non-aromatic carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.
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Page/Page column 64
(2010/10/20)
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- PROLINE DERIVATIVES
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The invention relates to novel compounds of formula (I), wherein X, Y, R1, R2, R3, R4 and n have the meaning cited in claim 1, are inhibitors of the coagulation factor Xa and can be used for the prophylaxis and/or therapy of thromboembolic diseases and for the treatment of tumours.
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Page/Page column 41
(2008/06/13)
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- MONOCYCLIC AND BICYCLIC LACTAMS AS FACTOR XA INHIBITORS
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The present application describes monocyclic and bicyclic lactams and derivatives thereof of Formulae (Ia-e); wherein one of one of T and T is carbonyl, thiocarbonyl, or sulfonyl or pharmaceutically acceptable salt forms thereof. Compounds of the pr
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Page/Page column 158
(2008/06/13)
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- CARBONYL COMPOUNDS
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The invention relates to the novel compounds of formula (I), wherein D, E, G, W, X, Y, T, R and R are defined as in claim 1. The inventive compounds inhibit coagulation factor Xa and can be used in the prophylaxis and/or therapy of thrombo-embolic diseases and for treating tumors.
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Page/Page column 112
(2008/06/13)
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