- Novel 3-phenylpiperidine-4-carboxamides as highly potent and orally long-acting neurokinin-1 receptor antagonists with reduced CYP3A induction
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The synthesis and biological evaluation of a series of novel 3-phenylpiperidine-4-carboxamide derivatives are described. These compounds are generated by hybridization of the substructures from two types of tachykinin NK1 receptor antagonists.
- Shirai, Junya,Sugiyama, Hideyuki,Morimoto, Shinji,Maezaki, Hironobu,Yamamoto, Yasuharu,Okanishi, Satoshi,Kamo, Izumi,Matsumoto, Shiho,Ishigami, Keiko,Inatomi, Nobuhiro,Imanishi, Akio,Kawamoto, Makiko,Tarui, Naoki,Hashimoto, Tadatoshi,Ikeura, Yoshinori
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p. 962 - 977
(2012/03/26)
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- PIPERIDINE DERIVATIVE AND USE THEREOF
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The present invention provides a novel piperidine derivative and a tachykinin receptor antagonist containing same, as well as a compound represented by the formula:wherein R1 is carbamoylmethyl, methylsulfonylethylcarbonyl and the like; R2 is methyl or cyclopropyl; R3 is a hydrogen atom or methyl; R4 is a chlorine atom or trifluoromethyl; R5 is a chlorine atom or trifluoromethyl; and a group represented by the formula:is a group represented by the formula:wherein R6 is a hydrogen atom, methyl, ethyl or isopropyl; R7 is a hydrogen atom, methyl or a chlorine atom; and R8 is a hydrogen atom, a fluorine atom, a chlorine atom or methyl; or 3-methylthiophen-2-yl, and a salt thereof.
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Page/Page column 94
(2008/12/08)
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