US4160841A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Heterocyclic derivatives of 1-(1,3-dioxolan-2-ylmethyl)-1H-imidazoles
Assignee: Janssen Pharmaceutica NV
•
Filing: 1977-11-21
•
Granted: 1979-07-10
•
Expires: 1997-11-21
Abstract
Abstract Heterocyclic derivatives of 1-(1,3-dioxolan-2-ylmethyl)-1H-imidazoles, 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
2026-10-31 18:07
CPC Classifications
C; C07; C07D; C07D231/00; C07D231/02; C07D231/10; C07D231/12; A; A61; A61P; A61P31/00; A61P31/04; A61P31/10; C07D233/00; C07D233/54; C07D233/56; C07D233/64; C07D233/66; C07D233/84; C07D249/00; C07D249/02; C07D249/08; C07D249/10; C07D249/12; C07D317/00; C07D317/08; C07D317/10; C07D317/14; C07D317/18; C07D317/20; C07D317/24
Claims Analysis
Total Claims: 10
Claim 1
Independent Claim
183 words
A chemical compound selected from the group consisting of an azole derivative having the formula: ##STR100## 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 having from 1 to 3 substituents independently selected from the group consisting of halo, lower alkyl and lower alkyloxy; and the radical Y is a member selected from the group consisting of: a 1H-pyrrol-1-yl radical of the formula ##STR101## a 1H-pyrazol-1-yl radical of the formula ##STR102## wherein R 1 is selected from the group consisting of hydrogen, lower alkyl, lower alkylthio and phenyl, and, R 2 is selected from the group consisting of hydrogen, lower alkyl and phenyl; and a 1H-imidazol-1-yl radical of the formula ##STR103## wherein R 3 is selected from the group consisting of hydrogen, lower alkyl, phenyl, lower alkylthio, lower alkylsulfinyl and lower alkylsulfonyl, R 4 is selected from the group consisting of hydrogen, lower alkyl and phenyl, and, R 5 is selected from the group consisting of hydrogen and phenyl.
Claim 2
Dependent Claim
183 words
A chemical compound selected from the group consisting of an azole derivative having the formula: ##STR100## 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 having from 1 to 3 substituents independently selected from the group consisting of halo, lower alkyl and lower alkyloxy; and the radical Y is a member selected from the group consisting of: a 1H-pyrrol-1-yl radical of the formula ##STR101## a 1H-pyrazol-1-yl radical of the formula ##STR102## wherein R 1 is selected from the group consisting of hydrogen, lower alkyl, lower alkylthio and phenyl, and, R 2 is selected from the group consisting of hydrogen, lower alkyl and phenyl; and a 1H-imidazol-1-yl radical of the formula ##STR103## wherein R 3 is selected from the group consisting of hydrogen, lower alkyl, phenyl, lower alkylthio, lower alkylsulfinyl and lower alkylsulfonyl, R 4 is selected from the group consisting of hydrogen, lower alkyl and phenyl, and, R 5 is selected from the group consisting of hydrogen and phenyl.
Claim 3
Dependent Claim
23 words
A chemical compound selected from the group consisting of 1-{4-[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-ylmethoxy]phenyl} -1H-imidazole 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 1-{4-[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-ylmethoxy]phenyl} -1H-imidazole 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 1-{4-[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-ylmethoxy]phenyl}-1H-pyrazole and the pharmaceutically acceptable acid additions salts and stereochemically isomeric forms thereof.
Claim 6
Dependent Claim
22 words
A chemical compound selected from the group consisting of 1-{4-[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-ylmethoxy]phenyl}-1H-pyrazole and the pharmaceutically acceptable acid additions salts and stereochemically isomeric forms thereof.
Claim 7
Dependent Claim
18 words
A chemical compound selected from the group consisting of cis-1-{4-[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-ylmethoxy]phenyl}-1H-imidazole and the pharmaceutically acceptable acid addition salts thereof.
Claim 8
Dependent Claim
18 words
A chemical compound selected from the group consisting of cis-1-{4-[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-ylmethoxy]phenyl}-1H-imidazole and the pharmaceutically acceptable acid addition salts thereof.
Claim 9
Dependent Claim
214 words
A composition for combatting the growth of 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: ##STR104## 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 having from 1 to 3 substituents independently selected from the group consisting of halo, lower alkyl and lower alkyloxy; and the radical Y is a member selected from the group consisting of: a 1H-pyrrol-1-yl radical of the formula ##STR105## a 1H-pyrazol-1-yl radical of the formula ##STR106## wherein R 1 is selected from the group consisting of hydrogen, lower alkyl, lower alkylthio and phenyl, and, R 2 is selected from the group consisting of hydrogen, lower alkyl and phenyl; and a 1H-imidazol-1-yl radical of the formula ##STR107## wherein R 3 is selected from the group consisting of hydrogen, lower alkyl, phenyl, lower alkylthio, lower alkylsulfinyl and lower alkylsulfonyl, R 4 is selected from the group consisting of hydrogen, lower alkyl and phenyl, and, R 5 is selected from the group consisting of hydrogen and phenyl.
Claim 10
Dependent Claim
214 words
A composition for combatting the growth of 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: ##STR104## 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 having from 1 to 3 substituents independently selected from the group consisting of halo, lower alkyl and lower alkyloxy; and the radical Y is a member selected from the group consisting of: a 1H-pyrrol-1-yl radical of the formula ##STR105## a 1H-pyrazol-1-yl radical of the formula ##STR106## wherein R 1 is selected from the group consisting of hydrogen, lower alkyl, lower alkylthio and phenyl, and, R 2 is selected from the group consisting of hydrogen, lower alkyl and phenyl; and a 1H-imidazol-1-yl radical of the formula ##STR107## wherein R 3 is selected from the group consisting of hydrogen, lower alkyl, phenyl, lower alkylthio, lower alkylsulfinyl and lower alkylsulfonyl, R 4 is selected from the group consisting of hydrogen, lower alkyl and phenyl, and, R 5 is selected from the group consisting of hydrogen and phenyl.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1982-07-09 | 1983-01-08 | 1983-07-10 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1986-07-09 | 1987-01-08 | 1987-07-10 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1990-07-09 | 1991-01-08 | 1991-07-10 | $7700.00 | Window Closed / Lapsed |