N-oxides as nk1 receptor antagonist prodrugs of 4-phenyl-pyridine derivatives
作者： Patrick Schnider , Andrew Sleight , Sonia Maria Poli , Torsten Hoffmann
DOI:
关键词:
摘要: The invention relates to compounds of formula (I) wherein R is hydrogen, lower alkyl, alkoxy, or trifluoromethyl; R1 hydrogen halogen; and may be together with the ring carbon atoms which they are attached -CH=CH-CH=CH-; R?2 R2'? independently from each other halogen, trifluoromethyl, alkoxy cyano; -CH=CH-CH=CH-, optionally substituted by one two substituents selected alkyl alkoxy; R3, R3' cycloalkyl; R4, R4' -(CH?2)mOR?6 alkyl; R?4 R4'? form N-atom a cyclic tertiary amine group (II) R5 hydroxy, -lower -(CH?2?)mOH, -COOR?3?, -CON(R3)2,-N(R3)CO-lower -C(O)R3; R6 phenyl; X -C(O)N(R6)-, -N(R6)C(O)-, -(CH?2?)mO- -O(CH2)m-; n 0, 1, 2, 3 4 and; m 3; pharmaceutically acceptable acid addition salts thereof. It has been found that these uses as prodrugs for treatment prevention illnesses, related NK1 receptor.
lens.org 参考文章(3)
Yoshinori IKEURA, Toshimasa TANAKA, Yutaka KIYOTA, Shinji MORIMOTO, Masaki OGINO, Takenori ISHIMARU, Izumi KAMO, Takayuki DOI, Hideaki NATSUGARI, Potent NK1 receptor antagonists: synthesis and antagonistic activity of various heterocycles with an N-[3,5-bis(trifluoromethyl)benzyl]-N-methylcarbamoyl substituent. Chemical & Pharmaceutical Bulletin. ,vol. 45, pp. 1642- 1652 ,(1997) , 10.1248/CPB.45.1642
Andrew Sleight, Sonia Maria Poli, Theresa Maria Ballard, Torsten Hoffmann, Guy Andrew Higgins, 2-(3,5-bis-trifluoromethyl-phenyl)-n-methyl-n-(6-morpholin-4-yl-4-o-tolyl-pyridin-3-yl)-isobutyramide ,(2000)
Thierry Godel, Walter Hunkeler, Guido Galley, Michael Montreal Boes, Patrick Schnider, Heinz Stadler, Quirico Branca, Torsten Hoffmann, 4-Phenylpyridine derivatives and their use as NK-1 receptor antagonists ,(2000)