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Serving leading biopharmaceutical companies globally:

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McKinsey
Teva
US Department of Justice
US Army
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Generated: January 17, 2018

DrugPatentWatch Database Preview

Claims for Patent: 4,358,449

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Summary for Patent: 4,358,449
Title: 1-(1,3-Dioxolan-2-ylmethyl)-1H-1,2,4-triazoles and compositions
Abstract: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)
Application Number:06/351,671
Patent 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 stereochemically 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;

A is a radical of the formula ##STR58## wherein Z is a member selected from the group consisting of a direct bond, CH.sub.2, O and N-R.sub.4, wherein R.sub.4 is selected from the group consisting of hydrogen, lower alkyl, hydroxy(lower alkyl), (lower alkyloxy)lower alkyl, lower alkanoyl, lower alkylsulfonyl, phenylmethylsulfonyl, lower alkyloxycarbonyl, lower alkyloxycarbonylmethyl, phenoxycarbonyl, aminocarbonyl, mono- and di(lower alkyl)aminocarbonyl, aminocarbonylmethyl, (lower alkyl)aminocarbonylmethyl, (lower alkyl) aminothioxomethyl, (lower alkylthio)thioxomethyl, phenyl, phenylmethyl, benzoyl and substituted benzoyl, said substituted benzoyl being benzoyl having from 1 to 2 substituents independently selected from the group consisting of halo, lower alkyl and lower alkyloxy; and

R is hydrogen.

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

3. A chemical compound selected from the group consisting of cis-1-{4-[2-(2,4-dichlorophenyl)-2-(1H-1,2,4-triazol-1-ylmethyl)-1,3-dioxo lan-4-ylmethoxy]-phenyl}piperazine and the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof.

4. A chemical compound selected from the group consisting of cis-4-{4-[2-(2,4-dichlorophenyl)-2-(1H-1,2,4-triazol-1-ylmethyl)-1,3-dioxo lan-4-ylmethoxy]phenyl}-1-piperazinecarboxaldehyde and the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof.

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

6. A chemical compound selected from the group consisting of cis-1-{4-[2-(2,4-dichlorophenyl)-2-(1H-1,2,4-triazol-1-ylmethyl)-1,3-dioxo lan-4-ylmethoxy]phenyl}-4-(1-methylethyl)piperazine and the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof.

7. 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: ##STR59## and the pharmaceutically acceptable acid addition salts and stereochemically 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;

A is a radical of the formula ##STR60## wherein Z is a member selected from the group consisting of a direct bond, CH.sub.2, O and N-R.sub.4 wherein R.sub.4 is selected from the group consisting of hydrogen, lower alkyl, hydroxy(lower alkyl), (lower alkyloxy)lower alkyl, lower alkanoyl, lower alkylsulfonyl, phenylmethylsulfonyl, lower alkyloxycarbonyl, lower alkyloxycarbonylmethyl, phenoxycarbonyl, aminocarbonyl, mono- and di(lower alkyl)aminocarbonyl, aminocarbonylmethyl, (lower alkyl)aminocarbonylmethyl, (lower alkyl) aminothioxomethyl, (lower alkylthio) thioxomethyl, phenyl, phenylmethyl, benzoyl and substituted benzoyl, said substituted benzoyl being benzoyl having from 1 to 2 substituents independently selected from the group consisting of halo, lower alkyl and lower alkyloxy; and

R is hydrogen.

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Serving leading biopharmaceutical companies globally:

Julphar
Daiichi Sankyo
Colorcon
US Department of Justice
Federal Trade Commission
Queensland Health
Cerilliant
Dow
McKinsey

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