US 4,060,623 AGranted

1,2,4-Triazole antimycotic compositions and use thereof

AssigneeBayer Aktiengesellschaft

InventorsWerner Meiser, Wolfgang Kramer, Karl Heinz Buchel, Manfred Plempel

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Abstract

Antimycotic compositions are produced which comprise an antimycotically effective amount of a 1,2,4-triazole of the formula: ##STR1## or a pharmaceutically acceptable non-toxic salt thereof wherein X.sup.1 is hydrogen or alkyl; X.sup.2 is hydrogen or alkyl; R.sup.1 is alkyl, unsubstituted or substituted aryl or unsubstituted or substituted aralkyl; R.sup.2 is hydrogen, alkyl or unsubstituted or substituted aryl; R.sup.3 is alkyl, cycloalkyl, unsubstituted or substituted aryl or unsubstituted or substituted aralkyl; and Y is a keto group or a functional derivative of a keto group, in combination with a pharmaceutically acceptable non-toxic, inert diluent or carrier.

Claims28

Dependent claims

An antimycotic composition for treating mycotic infections in humans and animals which comprises an antimycotically effective amount of a 1,2,4-triazole of the formula:

##STR72## wherein X.sup.1 is hydrogen or alkyl of 1 to 3 carbon atoms;
X.sup.2 is hydrogen or alkyl of 1 to 3 carbon atoms;
R.sup.1 is phenyl unsubstituted or substituted by one to five substituents selected from the group consisting of alkyl of 1 to 4 carbon atoms, the same or different halogen, the same or different haloalkyl of 1 or 2 carbon atoms and 2 to 5 halogen atoms, alkoxy of 1 or 2 carbon atoms, the same or different haloalkoxy of 1 or 2 carbon atoms and 2 to 5 halogen atoms, and nitro, or by one substituent selected from the group consisting of phenyl, halophenyl or amino;
R.sup.2 is hydrogen or alkyl of 1 to 6 carbon atoms;
R.sup.3 is phenyl unsubstituted or substituted by one to five substituents selected from the group consisting of alkyl of 1 to 4 carbon atoms, the same or different halogen, the same or different haloalkyl of 1 or 2 carbon atoms and 2 to 5 halogen atoms, alkoxy of 1 or 2 carbon atoms, the same or different haloalkoxy of 1 or 2 carbon atoms and 2 to 5 halogen atoms, alkoxy of 1 or 2 carbon atoms, the same or different haloalkoxy of 1 or 2 carbon atoms and 2 to 5 halogen atoms, and nitro, or by one substituent selected from the group consisting of phenyl, halophenyl or amino;
and
Y is CO;
in combination with a pharmaceutically acceptable non-toxic, inert carrier.

5 more elements

A method for treating mycotic infections in humans and animals which comprises administering to a human or animal in need thereof an antimycotically effective amount of a 1,2,4-triazole of the formula:

##STR77## wherein X.sup.1 is hydrogen or alkyl of 1 to 3 carbon atoms;
X.sup.2 is hydrogen or alkyl of 1 to 3 carbon atoms;
R.sup.1 is phenyl unsubstituted or substituted by one to five substituents selected from the group consisting of alkyl of 1 to 4 carbon atoms, the same or different halogen, the same or different haloalkyl of 1 to 2 carbon atoms and 2 to 5 halogen atoms, alkoxy of 1 or 2 carbon atoms, the same or different haloalkoxy of 1 or 2 atoms and 2 to 5 halogen atoms, and nitro, or by one substituent selected from the group consisting of phenyl, halophenyl or amino;
R.sup.2 is hydrogen or alkyl of 1 to 6 carbon atoms;
R.sup.3 is phenyl unsubstituted or substituted by one to five substituents selected from the group consisting of alkyl of 1 to 4 carbon atoms, the same or different halogen, the same or different haloalkyl of 1 or 2 carbon atoms and 2 to 5 halogen atoms, alkoxy of 1 or 2 carbon atoms, the same or different haloalkoxy of 1 or 2 carbon atoms and 2 to 5 halogen atoms, alkoxy of 1 or 2 carbon atoms, the same or different haloalkoxy of 1 or 2 carbon atoms and 2 to 5 halogen atoms, and nitro, or by one substitutent selected from the group consisting of phenyl, halophenyl or amino;
and
Y is CO;
in combination with a pharmaceutically acceptable non-toxic, inert carrier.

5 more elements

Dependencies are inferred from the claim text.

Facts

Application: 05/646,019Filed 2 Jan 1976 · division
Priority: DT 224718626 Sep 1972
Granted: 29 Nov 1977
Term ends: Not estimatedThe source records don’t support an estimate.

Classification7 codes

C07C 45/71
By reaction with functional groups containing oxygen only in singly bound form: being hydroxy groups
C07C 45/004
Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds: by reaction with…
C07C 45/63
By reactions not involving the formation of >C = O groups: by introduction of halogen; by substitution of halogen atoms by other halogen atoms
C07C 45/70
By increase in the number of carbon atoms: by reaction with functional groups containing oxygen only in singly bound form

Family

Serial396,202Parent of this division · filed 11 Sep 1973
Serial532,191Parent of this division · filed 12 Dec 1974
US 4,002,763 AParent of this division
3890442Parent of this division
US 4,060,623 AThis patent

From the US filing history. Foreign family members aren’t listed.