Phenyl- and pyridinyl derivatives

Details Phenyl- and pyridinyl derivatives Phenyl- and pyridinyl derivatives

C - Chemistry, Metallurgy

07

D

C07D 413/04 (2006.01) A61K 31/167 (2006.01) A61K 31/495 (2006.01) A61K 31/496 (2006.01) A61K 31/5377 (2006.01) C07C 233/88 (2006.01) C07D 295/155 (2006.01) C07D 401/04 (2006.01)

Patent

CA 2364665

The invention relates to compounds of general formula (I), wherein R is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl; R1 is hydrogen or halogen; or R and R1 may be together -CH=CH-CH=CH-; R2 is hydrogen, halogen, trifluoromethyl, lower alkoxy or cyano; R3 is independently from each other hydrogen, lower alkyl or form a cycloalkyl group; R4 is hydrogen, halogen, lower alkyl, lower alkoxy, -N(R5)2, -N(R5)S(O)2-lower alkyl, -N(R5)C(O)R5 or a cyclic tertiary amine of the group (a); R5 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)m O-, -(CH2)m N(R5)-, -N(R5) C(O)-, C(O)O- or -N(R5)(CH2)m-; Y is -(CH2)n-, -O-, -S-, SO2-, -C(O)- or -N(R5)-; Z is =N-, -CH= or -C(C1)=; n is 0 - 4; and, is 1 or 2; and to pharmaceutically acceptable acid addition salts thereof. It has been shown that the compounds of formula (I) have a high affinity to the NK-1 receptor.

Cette invention porte sur les composants de la formule générale (I), dans laquelle R est hydrogène, alkyle inférieur, alkoxy inférieur, halogène ou trifluorométhyl; R<1> est hydrogène ou halogène; ou R et R<1> peuvent former ensemble -CH=CH-CH=CH-; R<2> est hydrogène, halogène, trifluorométhyl, alkoxy inférieur ou cyano; R<3> est, indépendamment l'un de l'autre, hydrogène, alkyle inférieur ou constitue un groupe cycloalkyle; R<4> est hydrogène, halogène, alkyle inférieur, alkoxy inférieur, -N(R<5>)2, -N(R<5>)S(O)2-alkyle inférieur, -N(R<5>)C(O)R<5> ou un aminé tertiaire cyclique du groupe (a) R<5> est, indépendamment l'un de l'autre, hydrogène, C3-6-cycloalkyle, benzyle ou alkyle inférieur; R<6> est hydrogène, hydroxy, alkyle inférieur, -N(R<5>)CO-alkyle, inférieur, hydroxy-alkyle inférieur, cyano, -CHO ou un groupe hétérocyclique de cinq ou six composants, éventuellement lié par un groupe alcoylène, X est -C(O)N(R<5>)-, -(CH2)mO-, -(CH2)mN(R<5>)-, -N(R<5>) C(O)-, C(O)O- ou -N(R<5>)(CH2)m-; Y est -(CH2)n-, -O-, -S-, SO2-, -C(O)- ou -N(R<5>)-; Z est =N-, -CH= ou -C(C1)=; n est 0 - 4; et, m est 1 ou 2; et pour des sels d'addition acides pharmaceutiquement acceptables. Dans la présente invention, on constate que les composants de la formule (1) ont une haute affinité avec le récepteur NK-1.

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