Patent Number: 6,169,097

Title: 1-(1,2-Disubstituted piperidinyl)-4-substituted piperidine derivatives

Abstract: The present invention concerns compounds of formula ##STR1## 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; .dbd.Q is .dbd.O or .dbd.NR.sup.3 ; X is a covalent bond or a bivalent radical of formula --O--, --S--, --NR.sup.3 --; R.sup.1 is Ar.sup.1 ; Ar.sup.1 C.sub.1-6 alkyl or di(Ar.sup.1)C.sub.1-6 alkyl, wherein each C.sub.1-6 alkyl group is optionally substituted with hydroxy, C.sub.1-4 alkyloxy, oxo or a ketalized oxo substituent of formula --O--CH.sub.2 --CH.sub.2 --O-- or --O--CH.sub.2 --CH.sub.2 --CH.sub.2 --O--; R.sup.2 is Ar.sup.2 ; Ar.sup.2 C.sub.1-6 alkyl; Het or HetC.sub.1-6 alkyl; R.sup.3 is hydrogen or C.sub.1-6 alkyl; R.sup.4 is hydrogen; C.sub.1-4 alkyl; C.sub.1-4 aklyloxyC.sub.1-4 alkyl; hydroxyC.sub.1-4 alkyl; carboxyl; C.sub.1-4 aklyloxycarbonyl or Ar.sup.3 ; R.sup.5 is hydrogen; hydroxy; Ar.sup.3 ; Ar.sup.3 C.sub.1-6 alkyloxy; di(Ar.sup.3)C.sub.1-6 alkyloxy; Ar.sup.3 C.sub.1-6 alkylthio; di(Ar.sup.3)C.sub.1-6 alkylthio; Ar.sup.3 C.sub.1-6 alkylsulfoxy; di(Ar.sup.3)C.sub.1-6 alkylsulfoxy; Ar.sup.3 C.sub.1-6 alkylsulfonyl; di(Ar.sup.3)C.sub.1-6 alkylsulfonyl; --NR.sup.7 R.sup.8 ; C.sub.1-6 alkyl substituted with --NR.sup.7 R.sup.8 ; or a radical of formula (a-1) or (a-2); R.sup.4 and R.sup.5 may also be taken together; R.sup.6 is hydrogen; hydroxy; C.sub.1-6 alkyloxy; C.sub.1-6 alkyl or Ar.sup.3 C.sub.1-6 alkyl; Ar.sup.1, Ar.sup.2 and Ar.sup.3 are phenyl or substituted phenyl; Ar.sup.2 is also naphtalenyl; 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.

Inventors: Janssens; Frans Eduard (Bonheiden, BE), Sommen; Fran.cedilla.ois Maria (Wortel, BE), Surleraux; Dominique Louis Nestor Ghislaine (Machelen, BE), Van Roosbroeck; Yves Emiel Maria (Heist-op den-Berg, BE)

Assignee: Janssen Pharmaceutica N.V.

International Classification: C07D 211/44 (20060101); C07D 211/46 (20060101); C07D 405/14 (20060101); C07D 405/00 (20060101); C07D 211/00 (20060101); C07D 211/52 (20060101); C07D 409/14 (20060101); C07D 211/58 (20060101); C07D 417/00 (20060101); C07D 401/14 (20060101); C07D 471/00 (20060101); C07D 409/00 (20060101); C07D 401/00 (20060101); C07D 417/14 (20060101); C07D 401/06 (20060101); C07D 491/10 (20060101); C07D 471/10 (20060101); C07D 491/00 (20060101); A61K 031/445 (); C07D 401/04 ()

Expiration Date: 01/02/2018