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Patent US4301166A successfully refreshed from Google Patents.
US4301166A
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Hydroxyethyl-azole compounds, their production and their medicinal use
Assignee: Bayer AG
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Filing: 1979-11-09
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Granted: 1981-11-17
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Expires: 1999-11-09
Abstract
Abstract The invention relates to hydroxyethyl-azole compounds and methods for their preparation. Also included in the invention are compositions containing said hydroxyethyl-azole compounds and methods for the use of said compounds and compositions as antimycotic agents.
Inventors
- 👤 Erik Regel
- 👤 Karl H. Buchel
- 👤 Ingo Haller
- 👤 Manfred Plempel
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-29 21:58
CPC Classifications
C; C07; C07D; C07D231/00; C07D231/02; C07D231/10; C07D231/12; A; A61; A61P; A61P31/00; A61P31/04; C07C; C07C29/00; C07C29/36; C07C29/38; C07C29/40; C07C45/00; C07C45/45; C07C45/46; C07D249/00; C07D249/02; C07D249/08
Claims Analysis
Total Claims: 12
Claim 1
Independent Claim
160 words
A hydroxyethyl-azole of the formula ##STR147## or a salt thereof in which Az represents imidazol-1-yl, 1,2,4-triazol-1-yl or 1,2,4-triazol-4-yl, R denotes optionally substituted phenyl, naphthyl or tetrahydronaphthyl which is unsubstituted or substituted by halogen, C 1 -C 4 -alkyl, C 1 -C 4 -alkoxy or halogenoalkyl with 1 to 4 carbon atoms and up to 5 halogen atoms, R 1 represents phenyl which is unsubstituted or substituted by halogen or C 1 -C 4 -alkyl and R 2 represents hydrogen, or R 1 and R 2 together, in the o-position relative to one another, represent an optionally halogen or C 1 -C 4 -alkyl substituted methylene bridge with 3 to 5 methylene groups, or, together with the phenyl ring, represent naphthyl, R 3 represents halogen, an alkyl, or alkoxy group with in each case 1 to 4 carbon atoms or halogenoalkyl with 1 to 4 carbon atoms and up to 5 halogen atoms and n is 0, 1, 2 or 3.
Claim 2
Dependent Claim
160 words
A hydroxyethyl-azole of the formula ##STR147## or a salt thereof in which Az represents imidazol-1-yl, 1,2,4-triazol-1-yl or 1,2,4-triazol-4-yl, R denotes optionally substituted phenyl, naphthyl or tetrahydronaphthyl which is unsubstituted or substituted by halogen, C 1 -C 4 -alkyl, C 1 -C 4 -alkoxy or halogenoalkyl with 1 to 4 carbon atoms and up to 5 halogen atoms, R 1 represents phenyl which is unsubstituted or substituted by halogen or C 1 -C 4 -alkyl and R 2 represents hydrogen, or R 1 and R 2 together, in the o-position relative to one another, represent an optionally halogen or C 1 -C 4 -alkyl substituted methylene bridge with 3 to 5 methylene groups, or, together with the phenyl ring, represent naphthyl, R 3 represents halogen, an alkyl, or alkoxy group with in each case 1 to 4 carbon atoms or halogenoalkyl with 1 to 4 carbon atoms and up to 5 halogen atoms and n is 0, 1, 2 or 3.
Claim 3
Dependent Claim
172 words
A compound according to claim 1 in which Az denotes an imidazol-1-yl, 1,2,4-triazol-1-yl or 1,3,4-triazole-1-yl radical, R denotes an optionally substituted phenyl, naphthyl or tetrahydronaphthyl radical which is unsubstituted or substituted by halogen, C 1 -C 4 -alkyl, C 1 -C 4 -alkoxy or halogenoalkyl, with 1 to 4 carbon atoms and up to 5 halogen atoms, R 1 denotes an optionally substituted phenyl and R 2 denotes a hydrogen atom, or R 1 and R 2 together, in the ortho-position relative to one another, denote a methylene bridge which has 3 to 5 methylene groups and is optionally monosubstituted or polysubstituted by halogen or C 1 -C 4 -alkyl, or R 1 and R 2 , together with the phenyl ring, complete a naphthyl radical; R 3 denotes a halogen atom, a straight-chain or branched alkyl or alkoxy group with in each case 1 to 4 carbon atoms, or a halogenoalkyl group with 1 to 4 carbon atoms and up to 5 halogen atoms, and n is 0, 1 or 2.
Claim 4
Dependent Claim
121 words
A compound according to claim 1 in which Az denotes an imidazol -1-yl or 1,2,4-triazol-1-yl radical, R denotes a phenyl radical, which is optionally monosubstituted or disubstituted by chlorine, fluorine or methyl, or denotes a naphthyl or tetrahydronaphthyl radical, R 1 denotes a phenyl radical, which is optionally monosubstituted or disubstituted by chlorine, bromine, fluorine or methyl, and R 2 denotes a hydrogen atom, or R 1 and R 2 together, in the ortho-position relative to one another, denote a trimethylene, tetramethylene or pentamethylene bridge, which is optionally substituted by chlorine or methyl, or, together with the phenyl ring, complete a naphthyl radical, R 3 denotes a chlorine or fluorine atom or a methyl group, and n is 0 or 1.
Claim 5
Dependent Claim
24 words
A pharmaceutical composition containing as an active ingredient an antimycotically effective amount of a compound according to claim 1 in admixture with a diluent.
Claim 6
Dependent Claim
17 words
A pharmaceutical composition of claim 4 in the form of a sterile or physiologically isotonic aqueous solution.
Claim 7
Dependent Claim
20 words
A composition according to claim 4 or 5 containing from 0.5 to 95% by weight of the said active ingredient.
Claim 8
Dependent Claim
24 words
A medicament in dosage unit form comprising an antimycotically effective amount of a compound according to claim 1 together with an inert pharmaceutical carrier.
Claim 9
Dependent Claim
16 words
A medicament of claim 7 in the form of tablets, pills, dragees, capsules, ampoules or suppositories.
Claim 10
Dependent Claim
41 words
A method of combating mycoses in warm-blooded animals which comprises administering to the animals an antimycotically effective amount of an active compound according to claim 1 either alone or in admixture with a diluent or in the form of a medicament.
Claim 11
Dependent Claim
27 words
A method according to claim 9 in which the active compound is administered in an amount of 50 to 200 mg per kg body weight per day.
Claim 12
Dependent Claim
16 words
A method according to claim 9 or 10 in which the active compound is administered parenterally.
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) | 1984-11-16 | 1985-05-18 | 1985-11-17 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1988-11-16 | 1989-05-18 | 1989-11-17 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1992-11-16 | 1993-05-18 | 1993-11-17 | $7700.00 | Window Closed / Lapsed |