US4652579A
Expired / Lapsed
US
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Antimicrobial azoles
Assignee: Bayer AG
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Filing: 1984-10-19
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Granted: 1987-03-24
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Expires: 2004-10-19
Abstract
Abstract The invention relates to 1-hydroxylethyl-azole derivatives of formula (I) in composition form and includes the use of such compositions as antimicrobial agents.
Inventors
- 👤 Graham Holmwood
- 👤 Karl H. Buchel
- 👤 Manfred Plempel
- 👤 Ingo Haller
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-30 02:18
CPC Classifications
C; C07; C07D; C07D231/00; C07D231/02; C07D231/10; C07D231/12; A; A61; A61P; A61P31/00; A61P31/04; C07D233/00; C07D233/54; C07D233/56; C07D249/00; C07D249/02; C07D249/08; C07D303/00; C07D303/02; C07D303/04; C07D303/08
Claims Analysis
Total Claims: 7
Claim 1
Independent Claim
227 words
A method of combating mycoses in warm-blooded animals which comprises administering to the animals an antimycotically effective amount of a compound which is a 1-hydroxyethyl-azole derivative of the formula ##STR157## or a physiologically acceptable acid addition salt thereof, in which R represents a C 1 -C 8 -alkyl radical, a C 3 -C 7 -cycloalkyl radical optionally substituted by C 1 -C 2 -alkyl or a phenyl radical optionally substituted by halogen, C 1 -C 4 -alkyl or halogenoalkyl with 1 or 2 carbon atoms and 1 to 5 halogen atoms, X represents a nitrogen atom or a CH group, Y represents a grouping --CH 2 CH 2 --, each Z independently represents a halogen atom, a C 1 -C 8 -alkyl, C 3 -C 7 -cycloalkyl, C 1 -C 8 -alkoxy, C 1 -C 8 -alkylthio, halogenoalkyl or halogenoalkoxy or halogenoalkylthio radical each of said halogen-atom-containing radicals having 1 to 2 carbon atoms and 1 to 5 halogen atoms, a phenyl radical, a phenoxy radical, a phenylalkyl radical or a phenylalkoxy radical, each of 7-8 C atoms and each being optionally substituted by halogen, C 1 -C 4 -alkyl or halogenoalkyl with 1 to 2 carbon atoms and 1 to 5 halogen atoms and m is 0, 1, 2 or 3 either alone or in admixture with a diluent or in the form of a medicament.
Claim 2
Independent Claim
227 words
A method of combating mycoses in warm-blooded animals which comprises administering to the animals an antimycotically effective amount of a compound which is a 1-hydroxyethyl-azole derivative of the formula ##STR157## or a physiologically acceptable acid addition salt thereof, in which R represents a C 1 -C 8 -alkyl radical, a C 3 -C 7 -cycloalkyl radical optionally substituted by C 1 -C 2 -alkyl or a phenyl radical optionally substituted by halogen, C 1 -C 4 -alkyl or halogenoalkyl with 1 or 2 carbon atoms and 1 to 5 halogen atoms, X represents a nitrogen atom or a CH group, Y represents a grouping --CH 2 CH 2 --, each Z independently represents a halogen atom, a C 1 -C 8 -alkyl, C 3 -C 7 -cycloalkyl, C 1 -C 8 -alkoxy, C 1 -C 8 -alkylthio, halogenoalkyl or halogenoalkoxy or halogenoalkylthio radical each of said halogen-atom-containing radicals having 1 to 2 carbon atoms and 1 to 5 halogen atoms, a phenyl radical, a phenoxy radical, a phenylalkyl radical or a phenylalkoxy radical, each of 7-8 C atoms and each being optionally substituted by halogen, C 1 -C 4 -alkyl or halogenoalkyl with 1 to 2 carbon atoms and 1 to 5 halogen atoms and m is 0, 1, 2 or 3 either alone or in admixture with a diluent or in the form of a medicament.
Claim 3
Dependent Claim
111 words
A method according to claim 1, in which the active ingredient is a compound as defined in claim 1 in which R represents a tert.-butyl, isopropyl or methyl radical; a cyclopropyl, cyclopentyl or cyclohexyl radical (in each case optionally methyl-substituted) or a phenyl radical which is optionally monosubstituted or disubstituted by fluorine, chlorine, methyl or trifluoromethyl; each Z independently represents a fluorine, chlorine or bromine atom or a methyl, tert.-butyl, cyclohexyl, methoxy, methylthio, trifluoromethyl, trifluoromethoxy or trifluoromethylthio radical, or a phenyl, phenoxy, benzyl or benzyloxy radical, (in each case optionally monosubstituted or disubstituted by fluorine, chlorine or methyl) and X, Y and m have the same meanings as in claim 1.
Claim 4
Dependent Claim
12 words
A method according to claim 1 wherein the 1-hydroxyethyl-azole derivative is 2-(4-chlorophenethyl)-3,3-dimethyl-1-(imidazol-1-yl)-butan-2-ol.
Claim 5
Dependent Claim
27 words
A method according to claim 1 in which the active compound is administered in an amount of 10 to 300 mg per kg body weight per day.
Claim 6
Dependent Claim
27 words
A method according to claim 1 in which the active compound is administered in an amount of 50 to 200 mg per kg body weight per day.
Claim 7
Dependent Claim
14 words
A method according to claim 1 in which the active compound is administered parenterally.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1990-03-23 | 1990-09-22 | 1991-03-24 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1994-03-23 | 1994-09-22 | 1995-03-24 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1998-03-23 | 1998-09-22 | 1999-03-24 | $7700.00 | Window Closed / Lapsed |