Discovery of novel tetrahydroisoquinoline derivatives as potent and selective factor Xa inhibitors

…, M Hayashi, I Uchida, K Aisaka, Y Hase, S Katoh…

Index: Ueno, Hiroshi; Yokota, Katsuyuki; Hoshi, Jun-Ichi; Yasue, Katsutaka; Hayashi, Mikio; Uchida, Itsuo; Aisaka, Kazuo; Hase, Yasunori; Katoh, Susumu; Cho, Hidetsura Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 1 p. 185 - 189

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Citation Number: 6

Abstract

A series of novel 2, 7-disubstituted tetrahydroisoquinoline derivatives were designed and synthesized. Among these derivatives, compounds 1 and 2 (JTV-803) exhibited potent inhibitory activity against FXa and good selectivity with respect to other serine proteases (thrombin, plasmin, and trypsin). In addition, compound 2 exhibited potent anti-FXa activity after intravenous and oral administration to cynomolgus monkey, and showed a dose- ...

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