Novel derivatives of 4-phenylpyridine, method of obtaining them, application of such novel derivatives in production of a pharmaceutic agent and method of obtaining such pharmaceutic agent

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: GALLEY GUIDO, SCHNIDER PATRICK, GODEL THIERRY, HOFFMANN TORSTEN, BRANCA QUIRICO, BÖS MICHAEL, STADLER HEINZ, HUNKELER WALTER
Format: Patent
Sprache:eng ; pol
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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.