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Details for Patent: 4,223,036

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Details for Patent: 4,223,036

Title: 1-(1,3-Dioxolan-2-ylmethyl)-1H-1,2,4-triazoles
Abstract:Novel 1-(1,3-dioxolan-2-ylmethyl)-1H-imidazoles and 1H-1,2,4-triazoles useful as antifungal and antibacterial agents.
Inventor(s): Heeres; Jan (Vosselaar, BE), Backx; Leo J. J. (Arendonk, BE), Mostmans; Joseph H. (Antwerp, BE)
Assignee: Janssen Pharmaceutica N.V. (Beerse, BE)
Filing Date:Jan 08, 1979
Application Number:06/001,612
Claims:1. A chemical compound selected from the group consisting of an azole derivative having the formula: ##STR57## and the pharmaceutically acceptable acid addition salts and stereochemical optical isomeric forms thereof, wherein:

Q is N;

Ar is a member selected from the group consisting of phenyl and substituted phenyl, said substituted phenyl being phenyl having from 1 to 3 substituents independently selected from the group consisting of halo, lower alkyl and lower alkyloxy;

the radical A is a member selected from the group consisting of:

(a) an isothiocyanato group --N.dbd.C.dbd.S;

(b) an amino radical of the formula ##STR58## wherein R.sub.1 and R.sub.2 are each independently selected from the group consisting of hydrogen and lower alkyl;

(c) a radical of the formula ##STR59## wherein X is selected from the group consisting of O and S, Y is selected from the group consisting of O and NH, m is the integer 0 or 1, and R.sub.3 is selected from the group consisting of hydrogen, lower alkyl, mono- and dihalo(lower alkyl), phenyl and substituted phenyl, said substituted phenyl having from 1 to 2 substituents independently selected from the group consisting of halo, lower alkyl and lower alkyloxy, provided that:

(i) when said X is S, then said Y is NH and said m is 1, and

(ii) when said Y is O and said m is 1, then said R.sub.3 is other than hydrogen; and

R is a member selected from the group consisting of hydrogen and nitro, provided that when said R is nitro, then said A is amino.

2. A composition for combatting a microorganism selected from the group consisting of fungus and bacterium comprising an inert carrier material and as an active ingredient an effective amount of a compound selected from the group consisting of an azole derivative having the formula: ##STR60## and the pharmaceutically acceptable acid addition salts and stereochemical optical isomeric forms thereof, wherein:

Q is N;

Ar is a member selected from the group consisting of phenyl and substituted phenyl, said substituted phenyl being phenyl having from 1 to 3 substituents independently selected from the group consisting of halo, lower alkyl and lower alkyloxy;

the radical A is a member selected from the group consisting of

(a) an isothiocyanato group --N.dbd.C.dbd.S;

(b) an amino radical of the formula ##STR61## wherein R.sub.1 and R.sub.2 are each independently selected from the group consisting of hydrogen and lower alkyl;

(c) a radical of the formula ##STR62## wherein X is selected from the group consisting of O and S, Y is selected from the group consisting of O and NH, m is the integer 0 or 1, and R.sub.3 is selected from the group consisting of hydrogen, lower alkyl, mono- and dihalo(lower alkyl), phenyl and substituted phenyl, said substituted phenyl having from 1 to 2 substituents independently selected from the group consisting of halo, lower alkyl and lower alkyloxy, provided that:

(i) when said X is S, then said Y is NH and said m is 1, and

(ii) when said Y is O and said m is 1, then said R.sub.3 is other than hydrogen; and

R is a member selected from the group consisting of hydrogen and nitro, provided that when said R is nitro, then said A is amino.

3. A chemical compound selected from the group consisting of N-{4-[2-(2,4-dichlorophenyl)-2-(1H-1,2,4-triazol-1-ylmethyl)-1,3-dioxolan- 4-ylmethoxy]phenyl}acetamide and the pharmaceutically acceptable acid addition salts and stereochemical optical isomeric forms thereof.
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