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Claims for Patent: 4,335,125

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Claims for Patent: 4,335,125

Title: 1-(1,3-Dioxolan-2-ylmethyl)-1H-imidazoles
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)
Application Number:06/001,613
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 CH;

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)aminothiocarbonyl, (lower alkylthio)thiocarbonyl 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 an azole derivative having the formula: ##STR59## and the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof, wherein:

Q is CH;

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 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)aminothiocarbonyl, (lower alkylthio)thiocarbonyl, 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.

3. A chemical compound selected from the group consisting of 1-acetyl-4-{4-[2-(2,4-dichlorophenyl)-2-(1H-imidazol-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 4-{4-[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-ylm ethoxy]phenyl}-morpholine 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-imidazol-1-ylmethyl)-1,3-dioxolan-4-ylm ethoxy]phenyl}-N-methyl-1-piperazinecarboxamide and the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof.

6. A chemical compound selected from the group consisting of ethyl 4-{4-[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-ylm ethoxy]phenyl}-1-piperazinecarboxylate and the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof.

7. A chemical compound selected from the group consisting of methyl 4-{4-[2-(2,4-dichlorophenyl-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-ylme thoxy]phenyl}-1-piperazinecarboxylate and the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof.

8. A chemical compound selected from the group consisting of cis-1-acetyl-4-{4-[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-yl-methyl)-1,3- dioxolan-4-ylmethoxy]-phenyl}piperazine and the pharmaceutically acceptable acid addition salts thereof.

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

10. 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: ##STR61## and the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof, wherein:

Q is CH;

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 ##STR62## 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) aminothiocarbonyl, (lower alkylthio)thiocarbonyl, 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.

11. 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: ##STR63## and the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof, wherein:

Q is CH;

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 ##STR64## wherein Z is 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)aminothiocarbonyl, (lower alkylthio)thiocarbonyl, 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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