Janssen Pharmaceutica Nv

Janssen Pharmacuetica N.v.

Leo J Backx

Jan Heeres

Joseph H Mostmans

Raymond A Stokbroekx

Didier Robert De Chaffoy De Courcelles

Luc Alfons Van Der Eycken

Adolf Hubele

Elmar Sturm

Willy Joannes Van Laerhoven

Robert Jozef Hendrickx

Robert Nyfeler

Jean Louis Mesens

Frank Christopher Odds

Jean P Van Wauwe

Louis J Van Der Veken

Alfonsus G Knaeps

Paul August Luyts

Joseph A Mostmans

Jozef B Thijssen

Apolipoprotein-B synthesis inhibitors

Triazolones as apolipoprotein-B synthesis inhibitors

Watersoluble azole antifungals

The present invention provides novel compounds of formula ##STR1## the stereochemically isomeric forms thereof, and the pharmaceutically acceptable acid addition salts thereof, wherein A and B taken together form a bivalent radical of formula: --N.dbd.CH-- (a), --CH.dbd.N-- (b), --CH.sub.2 --CH.sub.2 -- (c), --CH.dbd.CH-- (d) --C(.dbd.O)--CH.sub.2 -- (e), --CH.sub.2 --C(.dbd.O)-- (f); R.sup.1 is hydrogen, C.sub.1-6 alkyl, or halo; R.sup.2 is hydrogen or halo; R.sup.3 is hydrogen; C.sub.1-8 alkyl; C.sub.3-6 cycloalkyl or C.sub.1-8 alkyl substituted with hydroxy, oxo, C.sub.3-6 cycloalkyl or aryl. Het is five- or six-membered optionally substituted heterocyclic ring. The use as a medicine, especially as a lipid lowering agent is disclosed as well as pharmaceutical compositions and processes for preparing compounds and compositions.

Apolipoprotein-.beta. synthesis inhibitors

4-[4-[4-[4-[[2-(2,4-difluorophenyl)-2-(1H-azolylmethyl)-1,3-dioxolan-4-yl]m ethoxy]phenyl]-1-piperazinyl]phenyl]triazolones and imidazolones, their pharmaceutically acceptable acid addition salts and stereoisomeric forms having improved antifungal properties, compositions containing the same, and methods of inhibiting and/or preventing the growth or the development of fungi, or of destroying fungi, in warm-blooded animals suffering from diseases caused by these fungi.

Antifungal

Novel 1-(2-aryl-1,3-dioxan-2-ylmethyl)-1H-imidazoles and 1H-1,2,4-triazoles wherein the 1,3-dioxane ring is optionally substituted with 1 to 3 substituents.

1-(2-aryl-1,3-dioxon-2-ylmethyl)-1H-imidazoles and 1H-1,2,4-triazoles

4-(4-phenyl-1-piperazinyl)phenols for use as 5-lipoxygenase inhibitors and a method of treating warm-blooded animals suffering from leukotriene mediated diseases and disorders using the same. Pharmaceutical compositions containing the same as active ingredient. Novel compounds used in said method and processes for preparing said novel compounds.

5-lipoxygenase inhibiting 4-(4-phenyl-1-piperazinyl)phenols

4-[4-[4-[4-[[2-(2,4-difluorophenyl)-2-(1H-azolylmethyl)-1,3-dioxolan-4-yl]m ethoxy]phenyl]-1-piperazinyl]phenyl]triazolones, their pharmaceutically acceptable acid addition salts and stereoisomeric forms having improved antimicrobial properties, compositions containing the same, and methods of inhibiting and/or eliminating the development of fungi and bacteria in warm-blooded animals suffering from diseases caused by these fungi and/or bacteria.

4-[4-[4-[4-[[2-(2,4-difluoro

Substituted [[4-[4-(4-phenyl-1-piperazinyl)phenoxymethyl]-1,3-dioxolan-2-yl]methyl]-1H -imidazoles and 1H-1,2,4-triazoles having antimicrobial properties and being particularly useful in the treatment of vaginal candidosis.

Novel [[4-[4-(4-phenyl-1-piperazinyl)phenoxymethyl]-1,3-dioxolan-2-yl]methyl]-1H -imidazoles and 1H-1,2,4-triazoles, having anti-microbial activity, compositions containing the same, and methods of inhibiting and/or eliminating the development of fungi and bacteria in warm-blooded animals suffering from diseases caused by these fungi and/or bacteria.

[[4-[4-(4-phenyl-1-piperazinyl)phenoxymethyl]-

Substituted [[4-[4-(4-phenyl-1-piperazinyl)phenoxymethyl]-1,3 dioxolan-2-yl]methyl]-1H-imidazoles and 1H-1,2,4-triazoles having antimicrobial properties and being particularly useful in the treatment of vaginal candidosis.

[[4-[4-(4-phenyl-1-piperazinyl)phenoxymethyl]-1,3-diox

Novel 1-(1,3-dioxolan-2-ylmethyl)-1H-imidazoles and 1H-1,2,4-triazoles wherein the 1,3-dioxolane ring is substituted in the 4- and in the 5-positions, said compounds having useful antimicrobial properties.

Fungicidal

Novel compounds of the class of 1-(2-aryl-2-R-ethyl)-1H-1,2,4-triazoles having fungicidal and plant-growth regulating properties.

Fungicidal 1-(2-aryl-2-R-ethyl)-1H-1,2,4-triazoles

The invention is concerned with novel dithioketal derivatives of 1-(2-aryl-2-oxoethyl)-1H-imidazoles and sulfones and sulfoxides derived therefrom, said compounds being useful as antimicrobial agents.

Growing community of inventors

Arendonk, Belgium

Leo J Backx