Patent Number: 6,251,893

Title: Bicyclic piperidine and piperazine compounds having 5-HT6 receptor affinity

Abstract: Described herein are compounds with affinity for the 5-HT.sub.6 receptor, which have the general formula: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are independently selected from the group consisting of H, halo, OH, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-7 cycloalkyl and others; R.sup.5 is selected from the group consisting of SO.sub.2 Ar, C(O)Ar, Ar and CH.sub.2 Ar; R.sup.6 and R.sup.7 are independently selected from the group consisting of H, C.sub.1-6 alkyl, optionally substituted phenyl and optionally substituted benzyl; ---------- represents a single or double bond; n is selected from an integer of from 1-3; X is selected from the group consisting of CR.sup.17 and N; Z is selected from the group consisting of C, CH and N, provided that when ---------- is a double bond, Z is C and when ---------- is a single bond, Z is selected from CH and N; Ar is an optionally substituted aromatic group selected from the group consisting of phenyl, pyridyl, thienyl, furanyl, naphthyl, quinolyl and isoquinolyl; R.sup.16 is selected from the group consisting of H, C.sub.1-6 alkyl and benzyl. Also described is the use of these compounds as pharmaceuticals to treat indications where inhibition of the 5-HT.sub.6 receptor is implicated, such as schizophrenia.

Inventors: Maddaford; Shawn (Mississauga, CA), Xin; Tao (North York, CA), Slassi; Abdelmalik (Mississauga, CA), Tehim; Ashok (Mississauga, CA), Qiao; Qi (Nutley, NJ)

Assignee: NPS Allelix Corp.

International Classification: C07D 471/00 (20060101); C07D 471/04 (20060101); C07D 487/00 (20060101); C07D 487/04 (20060101); A61K 031/55 (); A61K 031/44 (); A61P 025/18 (); C07D 221/02 (); C07D 241/36 ()

Expiration Date: 06/26/2018