C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 243/08 (2006.01) A61K 31/551 (2006.01) A61K 31/5517 (2006.01) C07D 401/06 (2006.01) C07D 401/14 (2006.01) C07D 403/06 (2006.01) C07D 487/04 (2006.01)
Patent
CA 2409842
The invention relates to compounds of general formula (I) wherein R1, R2 are independently from each other aryl or heteroaryl, wherein the heteroaryl group contains one or two heteroatoms, selected from N, O or S, and wherein the aryl or heteroaryl groups are optionally substituted by 1 to 3 substituents, which are independently from each other halogen, CF3, lower alkoxy or lower alykl; R3 is hydrogen, lower alkyl, -(CH2)nN(R)2, -(CH2)n-heteroaryl or is a -(CH2)n- non aromatic heterocycle, which heterocycles are optionally substituted by halogen, CF3, lower alkoxy or lower alkyl; R4 is =O, =N(CH2)nCH3 or =N(CH2)nN(R)2; R3 and R4 may be together with the N and C atoms to which they are attached the group -CR5=N-N=; R5 is hydrogen, -(CH2)nN(R)2, -(CH2)n- heteroaryl or is a -(CH2)n-non aromatic heterocycle, which heterocycles are optionally substituted by halogen, CF3, lower alkoxy or lower alkyl; R is hydrogen or lower alkyl; n is 0, 1, 2 or 3; and pharmaceutically acceptable acid addition salts and enantiomeric forms thereof. The compounds are useful in the treatment of diseases, related to the NK-1 receptor.
L'invention porte sur des composés de formule générale (I) dans laquelle: R?1¿, R?2¿ sont indépendamment l'un de l'autre aryle ou hétéroaryle, le groupe hétéroaryle contenant un ou deux hétéroatomes choisis parmi N, O ou S, et les groupes aryle ou hétéroaryle étant facultativement substitué par 1 à 3 substituants qui sont indépendamment l'un de l'autre halogène, CF¿3?, alkoxy inférieur ou alkyle inférieur; R?3¿ est hydrogène, alkyle inférieur, -(CH¿2?)¿n?N(R)¿2?, hétéroaryle-(CH¿2?)¿n?-, ou un hétérocycle-(CH¿2?)¿n?- non aromatique, lesdits hétérocycles étant facultativement substitués par halogène, CF¿3?, alkoxy inférieur ou alkyle inférieur; R?4¿ est =O, =N(CH¿2?)¿n?CH¿3? ou =N(CH¿2?)¿n?N(R)¿2?; R?3¿ et R?4¿ peuvent former avec les atomes de N et C auxquels ils sont liés le groupe -CR5=N-N=; R?5¿ est hydrogène, -(CH¿2?)¿n?N(R¿)2?, hétéroaryle-(CH¿2?)¿n?-, ou un hétérocycle-(CH¿2?)¿n?- non aromatique, lesdits hétérocycles étant facultativement substitués par halogène, CF¿3?, alkoxy inférieur ou alkyle inférieur; R est hydrogène ou alkyle inférieur; n est 0, 1, 2 ou 3; et sur leurs sels d'addition d'acide et leurs énantiomères. Lesdits composés servent au traitement de maladies liées au récepteur de la NK-1.
Galley Guido
Godel Thierry
Goergler Annick
Heck Reinhard
Borden Ladner Gervais Llp
F. Hoffmann-La Roche Ag
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