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

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

C - Chemistry, Metallurgy

07

D

C07D 213/74 (2006.01) A61K 31/4427 (2006.01) A61K 31/455 (2006.01) A61P 25/00 (2006.01) A61P 29/02 (2006.01) C07D 213/75 (2006.01) C07D 213/79 (2006.01) C07D 213/82 (2006.01) C07D 401/04 (2006.01) C07D 401/06 (2006.01) C07D 401/12 (2006.01) C07D 409/04 (2006.01) C07D 413/04 (2006.01) C07D 417/04 (2006.01) C07D 521/00 (2006.01)

Patent

CA 2418868

The present invention relates to compounds of the general formula (I) wherein a.o. 5 R is hydrogen or halogen; R and R2 or R4 and R4' may be together -CH=CH- CH=CH-, optionally substituted by one or two substituents selected from lower alkyl, halogen or lower alkoxy; X is -C(O)N(R8)-, (CH2)pO-, -(CH2)pN(R8)-, - N(R8)C(O)- or -N(R8)-(CH2)p-; wherein R8 is hydrogen or lower alkyl; n is 1 or 2; m is 0, 1, 2, 3, or 4; O is 1 or 2; and p is 1 or 2; and to pharmaceutically acceptable acid addition salts thereof. It has been found that the compounds of the present invention are antagonists of the Neurokinin 1 (NK-1, substance P) receptor, and they are therefore useful in the treatment of diseases, related to this receptor.

L'invention concerne des composés de formule générale (I) dans laquelle 5 R désigne hydrogène ou halogène ; R et R?2¿ ou R?4¿ et R?4'¿ peuvent désigner conjointement -CH=CH-CH=CH-, éventuellement substitué par un ou deux substituants sélectionnés parmi alkyle inférieur, halogène ou alcoxy inférieur ; X désigne -C(O)N(R?8¿)-, (CH¿2?)¿p?O-, -(CH¿2?)¿p?N(R?8¿)-, -N(R?8¿)C(O)- ou N(R?8¿)-(CH¿2?)¿p?- ; où R?8¿ désigne hydrogène ou alkyle inférieur ; n vaut 1 ou 2 ; m vaut 0,1,2,3 ou 4 ; o vaut 1 ou 2 ; et p vaut 1 ou 2. L'invention concerne également des sels d'addition d'acide pharmaceutiquement tolérables desdits dérivés. Il a été démontré que les composés de l'invention sont des antagonistes du récepteur de neurokinine 1 (NK-1, substance P) et s'utilisent de ce fait dans le traitement d'affections apparentées audit récepteur.

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