4-PHENYL-PIRIDINE DERIVATIVES, PROCESS FOR PRODUCING THEM AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

The present invention relates to compounds of the general formula wherein R is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl; R    is hydrogen or halogen; or R and R    may be together -CH=CH-CH=CH-; R and R   may be together -CH=CH-CH=CH-, optionally substituted by one or two subs...

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Hauptverfasser: HOFFMANN TORSTEN HOFFMANN TORSTEN, HUNKELER WALTER HUNKELER WALTER, GALLEY GUIDO GALLEY GUIDO, BRANCA QUIRICO BRANCA QUIRICO, BOES MICHAEL BOES MICHAEL, GODEL THIERRY GODEL THIERRY, STADLER HEINZ STADLER HEINZ, SCHNIDER PATRICK SCHNIDER PATRICK
Format: Patent
Sprache:eng
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Zusammenfassung:The present invention relates to compounds of the general formula wherein R is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl; R    is hydrogen or halogen; or R and R    may be together -CH=CH-CH=CH-; R and R   may be together -CH=CH-CH=CH-, optionally substituted by one or two substituents selected from lower alkyl or lower alkoxy; R    is hydrogen, lower alkyl or form a cycloalkyl group; R    is hydrogen, -N(R )2, -N(R )(CH2)nOH, -N(R )S(O)2-lower alkyl, -N(R )S(O)2-phenyl, -N=CH-N(R )2, -N(R )C(O)R or a cyclic tertiary amine of the group R    is, independently from each other, hydrogen, C3-6-cycloalkyl, benzyl or lower alkyl; R    is hydrogen, hydroxy, lower alkyl, -(CH2)nCOO-lower alkyl, -N(R )CO-lower alkyl, hydroxy-lower alkyl, cyano, -(CH2)nO(CH2)nOH, -CHO or a 5-or 6 membered heterocyclic group, optionally bonded via an alkylene group, X is -C(O)N(R )-, -(CH2)mO-, -(CH2)mN(R )-, -N(R )C(O)-, or -N(R )(CH2)m-; n is 0 - 4; and m is 1 or 2; and to pharmaceutically acceptable acid addition salts thereof. The compounds of formula I show a high affinity to the NK-1 receptor. They may be used for the treatment of diseases, which relate to NK-1 receptor antagonists.