Substituted 1,2,3,4-tetrahydronaphthalene derivatives

C - Chemistry – Metallurgy – 07 – D

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C07D 295/155 (2006.01) A61K 31/445 (2006.01) A61K 31/495 (2006.01) A61K 31/496 (2006.01) A61K 31/535 (2006.01) A61K 31/54 (2006.01) C07D 207/337 (2006.01) C07D 211/26 (2006.01) C07D 211/34 (2006.01) C07D 211/76 (2006.01) C07D 241/00 (2006.01) C07D 295/096 (2006.01) C07D 295/135 (2006.01) C07D 295/215 (2006.01)

Patent

CA 2247940

New piperidinyl- or piperazinyl-substituted-1,2,3,4-tetrahydronaphthalene derivatives having formula (I) wherein X is N or CH; Y is NR2CH2, CH2-NR2, NR2- CO, CO-NR2 or NR2SO2; R1 is H, C1-C6 alkyl or C3-C6 cycloalkyl; R3 is C1-C6 alkyl, C3-C6 cycloalkyl or (CH2)n-aryl, where aryl is phenyl or a heteroaromatic ring containing one or two heteroatoms selected from N, O and S and which may be mono- or di-substituted; n is 0-4; as (R)-enantiomer, (S)- enantiomer or a racemate in the form of the free base or a pharmaceutically acceptable salt or hydrate thereof; a pharmaceutical formulation containing the compounds, use of the compounds in the treatment of 5-hydroxytryptamine mediated disorders, processes for the preparation of the compounds and intermediates for the preparation of the compounds.

Nouveaux dérivés de 1,2,3,4-tétrahydronaphthalène substitués par pipéridinyle ou pipérazinyle, de la formule (I). Dans cette formule, X est N ou CH; Y est NR¿2?CH¿2?, CH¿2?-NR¿2?, NR¿2?-CO, CO-NR¿2? ou NR¿2?SO¿2?; R¿1? est H, C¿1?-C¿6? alkyle ou C¿3?-C¿6? cycloalkyle; R¿3? est C¿1?-C¿6? alkyle, C¿3?-C¿6? cycloalkyle ou (CH¿2?)¿n?-aryle, où aryle est phényle ou un cycle hétéroaromatique renfermant un ou deux hétéroatomes choisis parmi N, O et S et pouvant être mono- ou di-substitués; n est un nombre de 0 à 4; en tant qu'énantiomère (R), énantiomère (S) ou mélange racémique sous forme de base libre, de sel pharmaceutiquement acceptable ou d'hydrate de ce sel; formulation pharmaceutique renfermant ces composés, utilisation de ces composés pour le traitement des désordres à médiation de 5-hydroxytryptamine, procédés d'élaboration de ces composés et intermédiaires de ceux-ci.

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