The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.
The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.
Patent No.:
Date of Patent:
Nov. 16, 1999
Filed:
Jul. 09, 1998
Raymond Antoine Stokbroekx, Beerse, BE;
Marcel Jozef Van der Aa, Turnhout, BE;
Marc Willems, Vosselaar, BE;
Lieven Meerpoel, Merksplas, BE;
Marcel Gerebernus Luyckx, Geel, BE;
Robert Tuman, Spring House, PA (US);
Janssen Pharmaceuticals, N.V., Beerse, BE;
Abstract
This invention concerns compounds of formula the N-oxide forms, the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof, wherein X is CH or N; m is 2 or 3 and n is 1, 2 or 3; wherein 1 or 2 C-atoms of the CH.sub.2 groups of the ##STR1## moiety which may also contain one double bond, may be substituted with C.sub.1-6 alkyl, amino, aminocarbonyl, mono- or di(C.sub.1-6 alkyl)amino, C.sub.1-6 alkyloxycarbony, C.sub.1-6 alkylcarbonylamino, hydroxy or C.sub.1-6 alkyloxy; and/or 2 C-atoms of said CH.sub.2 groups may be bridged with C.sub.2-4 alkanediyl; R.sup.1 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, C.sub.1-6 alkylthio, amino, mono- or di(C.sub.1-6 alkyl)amino, Ar, ArNH--, C.sub.3-6 cycloalkyl, hydroxymethyl or benzyloxymethyl; R.sup.2 and R.sup.3 are hydrogen, or taken together may form a bivalent radical of formula --CH.dbd.CH--CH.dbd.CH--; in case X represents CH then L is a radical L.sup.1, L.sup.2 or L.sup.3 ; or in case X represents N then L is a radical L.sup.2 or L.sup.3 ; L.sup.1 is Ar-C.sub.1-6 alkyloxy, Ar-oxy, Ar-thio, Ar-carbonylamino, di-Ar-methyloxy-, N-Ar-piperazinyl, N-Ar-homopiperazinyl, 2-benzimidazolinonyl, Ar--NR.sup.4 --, Ar-Alk-NR.sup.4 --, Ar--NR.sup.4 -Alk-NR.sup.5 -- or Het-NR.sup.4 --; L.sup.2 is Ar, Ar-carbonyl, Ar--CH.dbd.CH--CH.sub.2 --, naphtalenyl or Het; L.sup.3 is C.sub.1-6 alkyl substituted with one or two radicals selected from Ar, Ar-oxy, or Ar-thio, further optionally substituted with cyano or hydroxy; 2,2-dimethyl-1,2,3,4-tetrahydro-naphtalenyl; 2,2-dimethyl-1H-2,3-dihydroindenyl;Ar-piperidinyl or Ar--NR.sup.4 -Alk-; R.sup.4 and R.sup.5 are each independently selected from hydrogen or C.sub.1-6 alkyl; Alk is C.sub.1-6 alkanediyl; their preparation, compositions containing them and their use as a medicine.