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Discovery and SAR of potent, orally available and brain-penetrable 5,6-dihydro-4H-3-thia-1-aza-benzo[e]azulen- and 4,5-dihydro-6-oxa-3-thia-1-aza-benzo[e]azulen derivatives as neuropeptide Y Y5 receptor antagonists.
Rueeger H, Gerspacher M, Buehlmayer P, Rigollier P, Yamaguchi Y, Schmidlin T, Whitebread S, Nuesslein-Hildesheim B, Nick H, Cricione L. Rueeger H, et al. Among authors: yamaguchi y. Bioorg Med Chem Lett. 2004 May 17;14(10):2451-7. doi: 10.1016/j.bmcl.2004.03.014. Bioorg Med Chem Lett. 2004. PMID: 15109631
Structural modification of the P2' position of 2,7-dialkyl-substituted 5(S)-amino-4(S)-hydroxy-8-phenyl-octanecarboxamides: the discovery of aliskiren, a potent nonpeptide human renin inhibitor active after once daily dosing in marmosets.
Maibaum J, Stutz S, Göschke R, Rigollier P, Yamaguchi Y, Cumin F, Rahuel J, Baum HP, Cohen NC, Schnell CR, Fuhrer W, Gruetter MG, Schilling W, Wood JM. Maibaum J, et al. Among authors: yamaguchi y. J Med Chem. 2007 Oct 4;50(20):4832-44. doi: 10.1021/jm070316i. Epub 2007 Sep 8. J Med Chem. 2007. PMID: 17824680
Food intake in free-feeding and energy-deprived lean rats is mediated by the neuropeptide Y5 receptor.
Criscione L, Rigollier P, Batzl-Hartmann C, Rüeger H, Stricker-Krongrad A, Wyss P, Brunner L, Whitebread S, Yamaguchi Y, Gerald C, Heurich RO, Walker MW, Chiesi M, Schilling W, Hofbauer KG, Levens N. Criscione L, et al. Among authors: yamaguchi y. J Clin Invest. 1998 Dec 15;102(12):2136-45. doi: 10.1172/JCI4188. J Clin Invest. 1998. PMID: 9854049 Free PMC article.
Structure-based design of aliskiren, a novel orally effective renin inhibitor.
Wood JM, Maibaum J, Rahuel J, Grütter MG, Cohen NC, Rasetti V, Rüger H, Göschke R, Stutz S, Fuhrer W, Schilling W, Rigollier P, Yamaguchi Y, Cumin F, Baum HP, Schnell CR, Herold P, Mah R, Jensen C, O'Brien E, Stanton A, Bedigian MP. Wood JM, et al. Among authors: yamaguchi y. Biochem Biophys Res Commun. 2003 Sep 5;308(4):698-705. doi: 10.1016/s0006-291x(03)01451-7. Biochem Biophys Res Commun. 2003. PMID: 12927775
5,241 results