C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 213/75 (2006.01) A61K 31/44 (2006.01) A61P 25/00 (2006.01) A61P 29/00 (2006.01) C07D 213/30 (2006.01) C07D 213/38 (2006.01) C07D 213/81 (2006.01)
Patent
CA 2364662
The invention relates to compounds of 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 hydrogen, lower alkyl or form a cycloalkyl group; R4 is hydrogen, -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)-, or -N(R5)(CH2)m-; n is 0-4; and m is 1 or 2; and to pharmaceutically acceptable acid addition salts thereof. It has been shown that the above mentioned compounds have a good affinity to the NK-1 receptor.
L'invention concerne des composés de la formule (I) dans laquelle R est hydrogène, alkyl inférieur, alkoxy inférieur, halogène ou trifluorométhyle; R<1> est hydrogène ou halogène; ou R et R<1> peuvent être ensemble -CH=CH-CH=CH-; R<2> est hydrogène, halogène, trifluorométhyle, alkoxy inférieur ou cyano; R<3> est hydrogène, alkyle inférieur ou forme un groupe cycloalkyle; R<4> est hydrogène, -N(R<5>)2, -N(R<5>)S(O)2- alkylène inférieur, -N(R<5>)C(O)R<5> ou un amine tertiaire cyclique du groupe (a); R<5> est, indépendamment l'un de l'autre, hydrogène, C3-6-cycloalkyle, benzyle ou alkyl inférieur; R<6> est hydrogène, hydroxy, alkyle inférieur, -N(R<5>)CO-alkyle inférieur, hydroxy-alkyle inférieur, cyano, -CHO ou un groupe hétérocyclique de 5 ou 6 membres, éventuellement lié par un groupe alkylène, X est C(O)N(R<5>)-, -(CH2)mO-, -(CH2)mN(R<5>)-, -N(R<5>)C(O)-, ou N(R<5>)(CH2)m-; n est 0-4; et m est 1 ou 2 ; l'invention concerne également des sels d'addition acides pharmaceutiquement acceptables. On a montré que les composés susmentionnés présentaient une bonne affinité avec le recepteur NK-1.
Boes Michael
Galley Guido
Godel Thierry
Hoffmann Torsten
Hunkeler Walter
Borden Ladner Gervais Llp
F. Hoffmann-La Roche Ag
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