170229-13-7Relevant articles and documents
Isoxazoline and isoxazole fibrinogen receptor antagonists
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, (2008/06/13)
This invention relates to novel isoxazolines and isoxazoles which are useful as antagonists of the platelet glycoprotein IIb/IIIa fibrinogen receptor complex or the vitronectin receptor, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of platelet aggregation, as thrombolytics, and/or for the treatment of thromboembolic disorders.
Bisbenzamidine isoxazoline derivatives as factor Xa inhibitors
Quan,Pruitt,Ellis,Liauw,Galemmo Jr.,Stouten,Wityak,Knabb,Thoolen,Wong,Wexler
, p. 2813 - 2818 (2007/10/03)
Factor Xa is an important serine protease in the blood coagulation cascade. It generates thrombin and holds the central position that links the intrinsic and extrinsic activation mechanism in the final common pathway of coagulation. Therefore, inhibition
Discovery of potent isoxazoline glycoprotein IIb/IIIa receptor antagonists
Wityak, John,Sielecki, Thais M.,Pinto, Donald J.,Emmett, George,Sze, Jean Y.,Liu, Jie,Tobin, A. Ewa,Wang, Shuaige,Jiang, Biao,Ma, Philip,Mousa, Shaker A.,Wexler, Ruth R.,Olson, Richard E.
, p. 50 - 60 (2007/10/03)
Using the isoxazoline as a common structural feature, three series of glycoprotein IIb/IIIa receptor antagonists were evaluated, culminating in the discovery of XR299 (30). In an in vitro assay of platelet inhibition, XR299 had an IC50 of 0.24 μM and was a potent antiplatelet agent when dosed intravenously in a canine model. It was shown through X-ray studies of the cinchonidine salt 49 that the receptor required the 5(R)-stereochemistry for high potency. The ethyl ester prodrug of XR299, XR300 (29), was orally active in the dog.