Hoechst Aktiengesellschaft

Walter Dittmar

Wolfgang Raether

Klaus-Dieter Kampe

Gerhard Lohaus

Burkhard Sachse

Herbert Siegel

Heinz Hanel

Ernst Blume

Eberhard Futterer

Wolfgang Schaper

Hermann J Gerhards

Ulrich Schacht

Patricia Usinger

Margret Leven

Manfred Bohn

Karl Theodor Kraemer

Heinz Ehrhardt

Hans-Georg Alpermann

Heinz G Peil

Dieter Bernd Reuschling

Hans G Alpermann

Bengt-Thomas Grobel

Klaus D Kampe

A nail lacquer containing at least one film-former which is insoluble in water and at least one substance which has antimycotic activity and is from the group comprising tioconazole, econazole, oxiconazole, miconazole, tolnaftate and naftifine hydrochloride.

Nail lacquer with antimycotic activity, and a process for the

Arylmethylazoles of the formula I ##STR1## in which Aryl is (substituted) phenyl or naphthyl;

Arylmethylazoles and their salts, agents which contain these compounds,

Arylmethylazole preparation processes

A nail varnish comprising a water-insoluble film-forming substance and an antimycotic compound which is a 1-hydroxy-2-pyridone I of the general formula ##STR1## in which R.sup.1 is a hydrocarbon group which contains from 6 to 9 carbon atoms, but is free from olefinic and acetylenic bonds, one of the groups R.sup.2 and R.sup.4 is hydrogen and the other is hydrogen, methyl or ethyl and R.sup.3 is alkyl having up to two carbon atoms, said antimycotic ingredient being present in free form or in the form of a salt.

Antimycotic nail varnish

Compounds of the formula I ##STR1## and the acid-addition salts thereof, where A=CH or N; Ar=naphthyl, thienyl or phenyl; Z=oxygen or sulfur; R.sup.1 =alkyl, F or Cl; g=0-2; L=0 or 1; m=0-4; p=0 or 1; X=O, S or N-R.sup.3 ; R.sup.2 =alkyl, alkoxy, halogen, SCH.sub.3, COC.sub.6 H.sub.5, CF.sub.3, COOCH.sub.3, COOC.sub.2 H.sub.5, or NO.sub.2 ; n=0-2; R.sup.2, under certain circumstances, is alternatively --CH.dbd.CH--CH.dbd.CH-- or phenoxy are described. Processes for the preparation thereof are also described. ##STR2## are valuable intermediates for the preparation of I. The compounds I serve as antimycotics.

2-azolylmethyl-2-aryl-1,3-dioxolanes and the salts thereof, processes

Arylmethylazoles and their salts, processes for their preparation,

Compounds I ##STR1## where A equals t-butyl or a large number of (substituted) aromatics; Y equals azolyl; or Y equals --X--R.sup.1 where X=oxygen or sulfur and R.sup.1 equals (cyclo)alkyl or (heterocyclic) aryl; or Y equals ##STR2## where R.sup.2 equals (cyclo)alkyl, acetyl or aryl; or Y equals --NR.sup.3 R.sup.4 where R.sup.3 /R.sup.4 is alkyl; or Y equals several nitrogen-containing heterocyclic rings; Z equals OH, alkylcarbonyloxy, hal, alkoxy or benzyloxy; and the salts thereof are effective antimycotics or fungicides. They are obtained by reaction of II ##STR3## with (CH.sub.3).sub.2 ##STR4## and further reaction of the compound IV ##STR5## obtained from this with a nucleophile YM (M=hydrogen or a metal equivalent). The compounds I (where Z=OH) resulting from this can be acylated or alkylated, or converted into I where Z=hal.

1-[1-aryl-1-hydroxy-2-azolyl-ethyl]-1-aryl-cyclopropane derivatives, and

Compounds of the formula I ##STR1## in which A equals CH or N, Ar equals phenyl, naphthyl or thienyl, R.sup.1 equals alkyl or halogen, and Y is a number of nitrogen-containing heterocyclic rings, have an excellent antimycotic action. The compounds IIIa ##STR2## are valuable intermediates for the preparation thereof.

2-Azolylmethyl-2-aryl-1,3-dioxolanes and the salts thereof, agents

Compounds I ##STR1## where A equals t-butyl, phenyl, biphenylyl, phenoxyphenyl, benzylphenyl, benzyloxyphenyl, phenylthiophenyl, phenylsulfinylphenyl, phenylsulfonylphenyl, naphthyl, 1,2,3,4-tetrahydronaphthyl, indanyl, fluorenyl, thienyl, furyl, pyridyl, isoxazolyl, pyrazolyl, benzofuryl or benzothienyl,

Antimycotic 1,1-disubstituted cyclopropane derivatives

Compounds I ##STR1## where A equals CH or N; Ar equals naphthyl, thienyl or phenyl; R.sup.1 equals alkyl, F or Cl; g equals zero, 1 or 2; and Y equals various heterocyclic bases, and the acid-addition salts thereof, are described. Several preparation processes are described. The compounds IIIa ##STR2## where R.sup.1, g and Y are as specified in the case of the formula I, serve as intermediates for the preparation of these compounds. Processes are also specified for the preparation of IIIa. I represent valuable antimycotics.

Compounds of the formula I ##STR1## and the acid-addition salts thereof, where A=CH or N; Ar=naphthyl, thienyl or phenyl; Z=oxygen or sulfur; R.sup.1 =alkyl, F or Cl; g=0-2; L=0 or 1; m=0-4; p=0 or 1; X=O, S or N--R.sup.3 ; R.sup.2 =alkyl, alkoxy, halogen, SCH.sub.3, COC.sub.6 H.sub.5, CF.sub.3, COOCH.sub.3, COOC.sub.2 H.sub.5, or NO.sub.2 ; n=0-2; R.sup.2, under certain circumstances, is alternatively --CH.dbd.CH--CH.dbd.CH-- or phenoxy are described. Processes for the preparation thereof are also described. Compounds IIIa ##STR2## are valuable intermediates for the preparation of I. The compounds I serve as antimycotics.

2-azolylmethyl-2-phenyl-4-[benzazol-2-yloxy-or-thio-methyl]-1,3

Alkenylazoles of formula I a/b ##STR1## in which X/Y is H, alkyl, phenyl, Hal, alkoxy or alkylthio; Z is CH or N; R is alkyl or a bridged (CH.sub.2).sub.m chain; and A is alkylene or a bridged alkylene chain; and the salts of these alkenylazoles are antimycotic agents or fungicides. They are obtained by elimination of water from the compounds II ##STR2##

Alkenylazoles, a process for their preparation and their use

New 1-hydroxy-2-pyridones of the general formula I ##STR1## in which R.sup.1, R.sup.2 and R.sup.3, which are identical or different, denote hydrogen or lower alkyl having 1-4 carbon atoms, R.sup.1 and R.sup.3 preferably being hydrogen, and R.sup.2 preferably being methyl,

1-hydroxy-2-pyridones, a process for their preparation, and medicaments

New 1-(1,3-dioxolan-2-ylmethyl)azoles, their stereoisomers and their salts are described, as are processes for their preparation. The new compounds are chemotherapeutic agents. They are active against skin fungi, mold fungi and yeasts and against bacteria.

1-(1,3-dioxolan-2-ylmethyl)azoles, their salts and their use

A cosmetic composition comprising a content of an 1-hydroxy-2-pyridone of the general formula ##STR1## in which R.sub.1 stands for hydrogen, alkyl of 1 to 17 carbon atoms, alkenyl of 2 to 17 carbon atoms, cycloalkyl of 5 to 8 carbon atoms, bicycloalkyl of 7 to 9 carbon atoms, cycloalkyl-alkyl of 1 to 4 alkyl carbon atoms, the cycloalkyl groups being optionally substituted by alkyl groups of 1 to 4 carbon atoms, aryl, aralkyl of 1 to 4 alkyl carbon atoms, aryl-alkenyl of 2 to 4 alkenyl carbon atoms, aryloxy-alkyl or arylthio-alkyl of 1 to 4 alkyl carbon atoms, benzhydryl, phenylsulfonyl-alkyl of 1 to 4 alkyl carbon atoms, furyl or furyl-alkenyl of 2 to 4 alkenyl carbon atoms, the aryl groups being optionally substituted by alkyl of 1 to 4 carbon atoms, by alkoxy of 1 to 4 carbon atoms, by nitro, cyano or halogen atoms,

Growing community of inventors

Hofheim am Taunus, Germany

Walter Dittmar