137685-81-5Relevant articles and documents
The discovery of new human coagulation factor XIa (FXIa) inhibitors by synthesis, biological evaluation, and structure-based modeling
Lee, Myeong Hwi,Song, Ho Young,Kim, Hyoungrae,Park, Kyung Eun,Kim, Jinyeong,Park, Tae Kyo,Kim, Yong Ju,Kang, Nam Sook
, p. 1105 - 1113 (2016/07/15)
Factor XIa (FXIa) is an enzyme that is activated during the earliest stage of initiation of the intrinsic pathway of the blood coagulation mechanism. In this study, we attempted to discover a new FXIa inhibitor based on structure-based molecular modeling. We found that compound 16 exhibits satisfactory predicted properties while maintaining important binding interactions with FX1a.
New Compound Having Inhibition Activity to Factor XIa
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Paragraph 0179-0183, (2021/05/17)
The present invention relates to a pharmacologically active amount of a novel compound, represented by chemical formula 1, having inhibition activity against factor XIa, a producing method thereof, and a pharmaceutical composition comprising: a pharmaceut
SERINE/THREONINE KINASE INHIBITORS
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Paragraph 00210; 00211, (2015/06/18)
Compounds having the formula I wherein R1, X1, X2, X3 and X4 as defined herein are inhibitors of ERK kinase. Also disclosed are compositions and methods for treating hyperproliferative disorders.
XANTHINE DERIVATIVES AS ADENOSINE A1 RECEPTOR ANTAGONISTS
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, (2008/06/13)
A method of attenuating a cognitive deficit in a patient in need thereof comprising administering to the patient a xanthine derivative.
Xanthines with C8 chiral substituents as potent and selective adenosine A1 antagonists.
Peet,Lentz,Dudley,Ogden,McCarty,Racke
, p. 4015 - 4020 (2007/10/02)
Several 8-substituted 1,3-dipropylxanthines were synthesized, and their receptor binding affinities at adenosine A1 and A2 receptors were measured. When enantiomeric pairs of compounds were examined, the R enantiomers were significantly more potent than the corresponding S enantiomers. The most potent compound at the A1 receptor was (R)-3,7-dihydro-8-(1-methyl-2-phenylethyl)-1,3-dipropyl-1H-purine-2,6-di one (5a; MDL 102,503), whose Ki value at the A1 receptor was 6.9 nM. However, a more selective compound was (R)-3,7-dihydro-8-(1-phenylpropyl)-1,3-dipropyl-1H-purine-2,6-dione (5d; MDL 102,234), which had a Ki value of 23.2 nM at the A1 receptor and an A2/A1 ratio of 153.
Selective adenosine receptor agents
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, (2008/06/13)
Xanthine derivative which act selectively at adenosine receptors and which act in general as adenosine antagonists are disclosed. From in vitro studies it is known that specific physiological effects can be distinguished as a result of this selectively and that adenosine receptor activity in vitro correlates with adenosine receptor activity in vivo.Pharmaceutical preparations of the subject compounds can be prepared on the basis of the selective binding activity of the compounds disclosed herein which will enhance certain physiological effects while minimizing others, such as decreasing blood pressure without decreasing heart rate.