4-phenyl-pyridine derivatives as neurokinin-1 receptor...

C - Chemistry – Metallurgy – 07 – D

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C07D 213/82 (2006.01) A61K 31/4427 (2006.01) A61K 31/465 (2006.01) A61P 25/00 (2006.01) A61P 29/00 (2006.01) C07D 213/75 (2006.01) C07D 401/04 (2006.01) C07D 413/04 (2006.01) C07D 521/00 (2006.01)

Patent

CA 2416874

The invention relates to compounds of general formulas (IA) or (IB) wherein R1 is (a), (b), (c), (d) or is -NH(CH2)2OH, -NR3C(O)CH3 or -NR3C(O)-cyclopropyl; R2 is methyl or chloro; R3 is hydrogen or methyl; R is hydrogen or -(CH2)2OH; and n is 1 or 2 and pharmaceutically acceptable acid addition salts thereof. These compounds have a good affinity of the NK-1 receptor and therefore they may be used in the treatment or prevention of diseases, related to this receptor.

Cette invention concerne des composés de formules générales (I) et (II), dans lesquelles : R?1¿ représente a), b), c), d), ou -NH(CH¿2?)¿2?OH, -NR?3¿C(O)CH¿3? ou -NR?3¿C(O)-cyclopropyle, R?2¿ représente méthyle ou chloro ; R?3¿ représente hydrogène ou méthyle ; R représente hydrogène ou (CH¿2?)¿2?OH et n vaut 1 ou 2 ; et des sels d'addition d'acide de ces derniers pharmaceutiquement acceptables. Ces composés présentent une bonne affinité pour le récepteur de NK-1 et peuvent, par conséquent, être utilisés pour le traitement ou la prévention des maladies liées à ce récepteur.

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