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2005
Isoquinoline derivatives
R 0420
Discovery of Novel Tetrahydroisoquinoline Derivatives as Potent and Selective
Xa Inhibitors. — A series of 17 novel tetrahydroisoquinoline derivatives, e.g.
18- 136 Factor
(I), is prepared. Among these derivatives, the 4-pyridinyl derivative (Ie) as well as its
mesylate salt possess the most promising anti-FXa activity. Importantly, the derivatives
not containing a carboxylate group at the piperidine ring show high acute toxicity. —
(UENO, H.; YOKOTA, K.; HOSHI, J.-I.; YASUE, K.; HAYASHI, M.; UCHIDA, I.;
AISAKA, K.; HASE, Y.; KATOH, S.; CHO*, H.; Bioorg. Med. Chem. Lett. 15 (2005)
1, 185-189; Cent. Pharm. Res. Inst., Japan Tobacco Inc., Takatsuki, Osaka 569, Japan;
Eng.) — Mischke
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