发明名称 3-Phenylpyridine derivatives and their use as NK-1 receptor antagonist.
摘要 The invention relates to compounds of the formulawhereinR is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl;R1 is hydrogen or halogen; orR and R1 may be together -CH=CH-CH=CH-;R2 is hydrogen, halogen, trifluoromethyl, lower alkoxy or cyano;R3 is hydrogen, lower alkyl or form a cycloalkyl group;R4 is hydrogen, -N(R5)2, -N(R5)S(O)2-lower alkyl, -N(R5)C(O)R5 or a cyclic tertiary amine of the groupR5 is, independently from each other, hydrogen, C3-6-cycloalkyl, benzyl or lower alkyl;R6 is hydrogen, hydroxy, lower alkyl, -N(R5)CO-lower alkyl, hydroxy-lower alkyl, cyano, -CHO or a 5- or 6 membered heterocyclic group, optionally bonded via an alkylene group,X is -C(O)N(R5)-, -(CH2)mO-, -(CH2)mN(R5)-, -N(R5)C(O)-, or -N(R5)(CH2)m-;n is 0-4; andm is 1 or 2;and to pharmaceutically acceptable acid addition salts thereof.It has been shown that the above mentioned compounds have a good affinity to the NK-1 receptor.
申请公布号 ZA200106371(B) 申请公布日期 2002.11.04
申请号 ZA20010006371 申请日期 2001.08.02
申请人 F. HOFFMANN-LA ROCHE AG. 发明人 MICHAEL BOES;GUIDO GALLEY;THIERRY GODEL;TORSTEN HOFFMANN;WALTER HUNKELER;PATRICK SCHNIDER;HEINZ STADLER
分类号 A61K31/44;A61P25/00;A61P29/00;C07D213/30;C07D213/38;C07D213/75;C07D213/81;C07D401/04 主分类号 A61K31/44
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