Thrombosis remains the major cause of cardiovascular disorders in the Western countries. The continued impact of thrombotic diseases on morbidity and mortality has led to extensive efforts to discover and develop novel antithrombotic agents. Preclinical data suggests that P2Y1 and P2Y12 inhibition provide similar antithrombotic efficacy, while targeting P2Y1 may have the potential for reduced bleeding liability. In this presentation, the synthesis and SAR of a series of 4-benzothiazole-7-hydroxy indolinyl based P2Y1 antagonists (I) will be disclosed. In particular, several analogs were potent in the in vitro platelet aggregation assay (PA IC50< 0.5 �M) and showed low clearance and small volume of distribution in rat pharmacokinectic studies.

Synthesis and SAR of 4-benzothiazole-7-hydroxy indolinyl diaryl urea analogs as P2Y<sub>1</sub> antagonists

246th National Meeting (2013)

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Synthesis and SAR of 4-benzothiazole-7-hydroxy indolinyl diaryl urea analogs as P2Y1 antagonists

Synthesis and SAR of 4-benzothiazole-7-hydroxy indolinyl diaryl urea analogs as P2Y₁ antagonists