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US4358449A
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1-(1,3-Dioxolan-2-ylmethyl)-1H-1,2,4-triazoles and compositions
Assignee: Janssen Pharmaceutica NV
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Filing: 1980-02-15
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Granted: 1982-11-09
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Expires: 2000-02-15
Abstract
Abstract 1-(1,3,-Dioxolan-2-ylmethyl)-1H-imidazoles and 1H-1,2,4-triazoles useful as antifungal and antibacterial agents.
Inventors
- 👤 Jan Heeres
- 👤 Leo J. J. Backx
- 👤 Joseph H. Mostmans
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-28 23:07
CPC Classifications
C; C07; C07D; C07D405/00; C07D405/02; C07D405/06; A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/41; A61K31/415; A61K31/435; A61K31/44; A61K31/445; A61K31/495; A61K31/535; A61P; A61P31/00; A61P31/04; A61P31/10; C07D231/00; C07D231/02; C07D231/10; C07D231/12; C07D233/00; C07D233/54; C07D233/56; C07D249/00; C07D249/02; C07D249/08; C07D295/00; C07D295/02; C07D295/027; C07D295/03; C07D295/04; C07D295/08; C07D295/096; C07D295/16; C07D295/18; C07D295/182; C07D295/185; C07D295/22; C07D295/26
Claims Analysis
Total Claims: 14
Claim 1
Independent Claim
175 words
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 2 , O and N-R 4 , wherein R 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.
Claim 2
Dependent Claim
175 words
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 2 , O and N-R 4 , wherein R 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.
Claim 3
Dependent Claim
23 words
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.
Claim 4
Dependent Claim
23 words
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.
Claim 5
Dependent Claim
22 words
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-dioxolan-4-ylmethoxy]-phenyl}piperazine and the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof.
Claim 6
Dependent Claim
22 words
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-dioxolan-4-ylmethoxy]-phenyl}piperazine and the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof.
Claim 7
Dependent Claim
22 words
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-dioxolan-4-ylmethoxy]phenyl}-1-piperazinecarboxaldehyde and the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof.
Claim 8
Dependent Claim
22 words
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-dioxolan-4-ylmethoxy]phenyl}-1-piperazinecarboxaldehyde and the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof.
Claim 9
Dependent Claim
22 words
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.
Claim 10
Dependent Claim
22 words
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.
Claim 11
Dependent Claim
22 words
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-dioxolan-4-ylmethoxy]phenyl}-4-(1-methylethyl)piperazine and the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof.
Claim 12
Dependent Claim
22 words
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-dioxolan-4-ylmethoxy]phenyl}-4-(1-methylethyl)piperazine and the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof.
Claim 13
Dependent Claim
203 words
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 2 , O and N-R 4 wherein R 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.
Claim 14
Dependent Claim
203 words
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 2 , O and N-R 4 wherein R 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.
References Cited (Backward Citations)
No citation records indexed.
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1985-11-08 | 1986-05-10 | 1986-11-09 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1989-11-08 | 1990-05-10 | 1990-11-09 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1993-11-08 | 1994-05-10 | 1994-11-09 | $7700.00 | Window Closed / Lapsed |