1-(1,2-Disubstituted piperidinyl)-4-substituted piperidine derivatives as thachykinin receptor antagonists

The present invention concerns compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof, wherein n is 0, 1 or 2; m is 1 or 2, provided that if m is 2, then n is 1; p is 0, 1 or 2; =Q is =O or =NR3; X is a covalent bond or...

Ausführliche Beschreibung

Gespeichert in:
Bibliographische Detailangaben
Hauptverfasser: VAN ROOSBROECK YVES EMIEL MARIA, SOMMEN FRANCOIS MARIA, SURLERAUX DOMINIQUE LOUIS NESTOR GHISLAINE, JANSSENS FRANS EDUARD
Format: Patent
Sprache:eng ; slo
Schlagworte:
Online-Zugang:Volltext bestellen
Tags: Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
Beschreibung
Zusammenfassung:The present invention concerns compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof, wherein n is 0, 1 or 2; m is 1 or 2, provided that if m is 2, then n is 1; p is 0, 1 or 2; =Q is =O or =NR3; X is a covalent bond or a bivalent radical of formula -O-, -S-, -NR3-; R1 is Ar1; Ar1C1-6alkyl or di(Ar1)C1-6alkyl, wherein each C1-6alkyl group is optionally substituted with hydroxy, C1-4alkyloxy, oxo or a ketalised oxo substituent of formula -O-CH2-CH2-O- or -O-CH2-CH2-CH2-O-; R2 is Ar2; Ar2C1-6alkyl; Het or HetC1-6alkyl; R3 is hydrogen or C1-6alkyl; R4 is hydrogen; C1-4alkyl; C1-4alkyloxyC1-4alkyl; hydroxyC1-4alkyl; carboxyl; C1-4alkyloxycarbonyl or Ar3; R5 is hydrogen; hydroxy; Ar3; Ar3C1-6alkyloxy; di(Ar3)C1-6alkyloxy; Ar3C1-6alkylthio; di(Ar3)C1-6alkylthio; Ar3C1-6alkylsulfoxy; di(Ar3)C1-6alkylsulfoxy; Ar3C1-6alkylsulfonyl; di(Ar3)C1-6alkylsufonyl; -NR7R8; C1-6alkyl substituted with -NR7R8; or a radical of formula (a-1) or (a-2); R4 and R5 may also be taken together; R6 is hydrogen; hydroxy; C1-6alkyloxy; C1-6alkyl or Ar3C1-6alkyl; Ar1, Ar2 and Ar3 are phenyl or substituted phenyl; Ar2 is also naphthalenyl; and Het is an optionally substituted monocyclic or bicyclic heterocycle; as substance P antagonists; their preparation, compositions containing them and their use as a medicine. Opísané sú deriváty piperidínu vzorca (I), ich N-oxidové formy, farmaceuticky prijateľné adičné soli a stereochemicky izomérne formy, kde n je 0, 1 alebo 2; m je 1 alebo 2 s tým, že keď m je 2, potom n je 1; p je 0, 1 alebo 2; =Q je =O alebo =NR3-; X je kovalentná väzba alebo -O-, -S-, NR3-; R1 je Ar1C1-6alkyl; R2 je Ar2; Ar2C1-6alkyl; Het alebo HetC1-6alkyl; R3 je vodík alebo C1-6alkyl; R4 je vodík; C1-4alkyl; C1-4alkyloxyC1- 4alkyl; hydroxyC1-4alkyl; karboxyl; C1-4alkyloxykarbonyl alebo Ar3; R5 je vodík; hydroxyskupina; Ar3; Ar3C1-6alkyloxyskupina; di(Ar3)C1-6alkyloxyskupina; Ar3C1-6alkyltioskupina; di(Ar3)C1-6alkyltioskupina; Ar3C1-6alkylsulfoxyskupina; di(Ar3)C1-6alkylsulfoxyskupina; Ar3C1-6alkylsulfonyl; di(Ar3)C1-6alkylsulfonyl; -NR7R8; C1-6alkyl substituovaný -NR7R8; alebo radikál vzorca (a-1) alebo (a-2); R6 je vodík, hydroxyskupina; C1-6alkyloxyskupina; C1-6alkyl alebo Ar3C1-6alkyl; Ar1, Ar2 a Ar3 sú fenyl alebo substituovaný fenyl; Ar2 je tiež naftalenyl; a Het je prípadne substituovaný monocyklický alebo bicyklický heterocyklus; ich príprava, farmaceutické prostriedky, ktoré ich obsahujú,