Improved isoxazoline fibrinogen receptor antagonists

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 261/10 (2006.01) A61K 31/42 (2006.01) A61K 31/535 (2006.01) C07D 413/14 (2006.01)

Patent

CA 2222050

This invention relates to improved isoxazoline compounds including, but not limited to N2-(3,5-dimethylisoxazole-4-sulfonyl)-N3- [3-(4-amidinophenyl)isoxazolin-5(R)-ylacetyl]-(S)-2,3-diaminopropionic acid, which are useful as antagonists of the platelet glycoprotein IIb/IIIa fibronogen receptor complex, to pharmaceutical compositions containing 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.

La présente invention concerne des composés d'isoxazoline améliorés contenant, sans toutefois s'y limiter, l'acide N2-(3,5-diméthylisoxazole-4-sulfonyl)-N3- [3-(4-amidinophényl)isoxazolin-5(R)-ylacétyl]-(S)-2,3-diaminopropionique, qui sont utiles comme antagonistes du récepteur du fibronogène de la membrane plaquettaire (c.-à-d. le complexe GPIIb/IIIa), des compositions pharmaceutiques contenant ces composés et des méthodes pour utiliser ces composés, seul ou en association avec d'autres agents thérapeutiques, pour l'inhibition de l'agrégation plaquettaire, comme thrombolytiques et/ou pour le traitement des troubles thrombo-emboliques.

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