Janssen Pharmaceutica Nv

Marcel J Van Der Aa

Jan Vandenberk

Albert H Van Heertum

Ludo E Kennis

Raymond A Stokbroekx

Marcel G Luyckx

Jan Heeres

Marc Willems

Gilbert A Grauwels

Joannes J Willems

Lieven Meerpoel

Paul A Janssen

Joseph H Mostmans

Robert W Tuman

Frank Christopher Odds

Luc Alfons Van Der Eycken

G M Marcel

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.

Angiogenesis inhibiting pyridazinamines

Urea and thiourea derivatives of azolones

Substituted azolone derivatives

The invention is concerned with the compounds having the formula ##STR1## the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein X is O or S; Y is CH or N; R.sup.1, R.sup.2 and R.sup.3 each independently are hydrogen or C.sub.1-4 alkyl; R.sup.4 and R.sup.5 each independently are hydrogen, halo, C.sub.1-4 alkyl, C.sub.1-4 alkyloxy, hydroxy, trifluoromethyl, trifluoromethyloxy or difluoromethyloxy; R.sup.6 is C.sub.1-4 alkyl; C.sub.1-4 alkyl substituted with arylcyclohexyl; aryl or arylcarbonyl; wherein aryl is phenyl optionally substituted with one or two substituents selected from halo and C.sub.1-4 alkyl;

Anti-virally active pyridazinamines, compositions containing the same and methods of treating viral diseases in warm-blooded animals.

Anti-virally active pyridazinamines

Novel pyridazinamine derivatives having antiviral activity, compositions containing these compounds as active ingredient, and a method of destructing viruses or preventing the growth thereof in warm-blooded animals suffering from diseases caused by these viruses. Processes for preparing said compounds and compositions.

Pridazinamine derivatives

Novel pyridazinamines having antirhinoviral activity, compositions containing these compounds as active ingredient, and a method of inhibiting combating or preventing the growth of viruses in warm-blooded animals suffering from diseases caused by these viruses.

Antirhinoviral heteroamine-substituted pyridazines

Pyridzainamine derivatives

Novel (thio)morpholinyl and piperazinyl alkylphenol ethers having antirhinoviral activity, compositions containing these compounds as active ingredient, and a method of inhibiting, combating or preventing the growth of viruses in warm-blooded animals suffering from diseases caused by these viruses.

Antipicorpaviral herterocyclic-substituted morpholinyl alkylphenol ethers

Novel pyridazinamine derivatives

Novel quinazoline derivatives, comprising in the heterocyclic part of their quinazoline nucleus at least one carbonyl or thiocarbonyl group and a particularly substituted piperidinyl-alkyl side chain, said compounds being potent serotonin-antagonists.

(Piperidinylalkyl) quinazoline derivatives

Novel 1-substituted 4-(diarylmethyl)piperazine derivatives having antianaphylactic and antihistaminic properties.

Growing community of inventors

Vosselaar, Belgium

Marcel J Van Der Aa