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Page 1
Dual neurokinin NK(1)/NK(2) antagonists: N-[(R,R)-(E)-1-arylmethyl-3-(2-oxo-azepan-3-yl)carbamoyl]allyl-N-methyl-3,5-bis(trifluoromethyl)benzamides and 3-[N'-3,5-bis(trifluoromethyl)benzoyl-N-arylmethyl-N'-methylhydrazino]-N-[(R)-2-oxo-azepan-3-yl]propionamides.
Gerspacher M, La Vecchia L, Mah R, von Sprecher A, Anderson GP, Subramanian N, Hauser K, Bammerlin H, Kimmel S, Pawelzik V, Ryffel K, Ball HA. Gerspacher M, et al. Bioorg Med Chem Lett. 2001 Dec 3;11(23):3081-4. doi: 10.1016/s0960-894x(01)00631-x. Bioorg Med Chem Lett. 2001. PMID: 11714615
Biphenyl derivatives as novel dual NK(1)/NK(2)-receptor antagonists.
Mah R, Gerspacher M, von Sprecher A, Stutz S, Tschinke V, Anderson GP, Bertrand C, Subramanian N, Ball HA. Mah R, et al. Among authors: gerspacher m. Bioorg Med Chem Lett. 2002 Aug 19;12(16):2065-8. doi: 10.1016/s0960-894x(02)00382-7. Bioorg Med Chem Lett. 2002. PMID: 12127505
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: gerspacher m. 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
1-Alkyl-4-phenyl-6-alkoxy-1H-quinazolin-2-ones: a novel series of potent calcium-sensing receptor antagonists.
Widler L, Altmann E, Beerli R, Breitenstein W, Bouhelal R, Buhl T, Gamse R, Gerspacher M, Halleux C, John MR, Lehmann H, Kalb O, Kneissel M, Missbach M, Müller IR, Reidemeister S, Renaud J, Taillardat A, Tommasi R, Weiler S, Wolf RM, Seuwen K. Widler L, et al. Among authors: gerspacher m. J Med Chem. 2010 Mar 11;53(5):2250-63. doi: 10.1021/jm901811v. J Med Chem. 2010. PMID: 20158186
Discovery and SAR of potent, orally available 2,8-diaryl-quinoxalines as a new class of JAK2 inhibitors.
Pissot-Soldermann C, Gerspacher M, Furet P, Gaul C, Holzer P, McCarthy C, Radimerski T, Regnier CH, Baffert F, Drueckes P, Tavares GA, Vangrevelinghe E, Blasco F, Ottaviani G, Ossola F, Scesa J, Reetz J. Pissot-Soldermann C, et al. Among authors: gerspacher m. Bioorg Med Chem Lett. 2010 Apr 15;20(8):2609-13. doi: 10.1016/j.bmcl.2010.02.056. Epub 2010 Feb 19. Bioorg Med Chem Lett. 2010. PMID: 20231096
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