P2Y 12-receptor antagonist – Novel antagonists of the P2Y12-receptor with antithrombotic effect

Purinergic receptors have been in the focus of drug

discovery for many years. Modulation of P2 receptors in platelets is of paramount importance in regulating platelet function, and, as a consequence, in controlling thrombotic diseases, which are the most common cause of morbidity and mortality in the Western world. The P2Y12-receptor on blood platelets is the target of known antithrombotic drugs (e.g. clopidogrel). The receptor is therefore validated for this therapeutic use. Furthermore, the P2Y12-receptor is expressed in certain parts of the brain, which opens new routes for the treatment of neuroinflammatory and neurodegenerative diseases. This invention provides novel antagonists of the P2Y12- receptor. The disclosed novel compounds show reversible and selective binding to the P2Y12-receptor. The molecules do not require bioactivation. Further the patent application discloses synthesis of the compounds with optimised product yield.

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