US4844902A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Topically applicable formulations of gyrase inhibitors in combination with corticosteroids
Assignee: Bayer AG
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Filing: 1988-02-11
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Granted: 1989-07-04
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Expires: 2008-02-11
Abstract
Abstract Topically applicable formulations comprising known ciprofloxacin-type antibacterials of the formula ##STR1## in which A is N or C-R.sup.9, and corticosteroids are especially effective in therapy, particularly in the oral cavity. The formulations can be used in the form of plasters, gels, suspensions, emulsions and solutions.
Inventors
- 👤 Klaus Grohe
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 14:30
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/435; A61K31/47; A61K31/56; A61K31/57; A61P; A61P17/00; A61P31/00; A61P31/04
Claims Analysis
Total Claims: 14
Claim 1
Independent Claim
190 words
A topically applicable formulation comprising by weight about 0.05 to 30% of an antibacterially active compound of the formula ##STR6## in which R 1 represents methyl, ethyl, propyl, isopropyl, cyclopropyl, vinyl, 2-hydroxyethyl, 2-fluoroethyl, methoxy, amino, methylamino, dimethylamino, ethylamino, phenyl, 4-fluorophenyl or 2,4-difluorophenyl, R 2 represents hydrogen, alkyl with 1 to 4 carbon atoms or (5-methyl-2-oxo-1,3-dioxol-4-yl)-methyl, R 3 represents methyl or a cyclic amino group of the formula ##STR7## wherein R 4 represents hydrogen, alkyl with 1 to 4 carbon atoms, 2-hydroxyethyl, allyl, propargyl, 2-oxopropyl, 3-oxobutyl, phenacyl, formyl, CFCL 2 -S-, CFCL 2 -SO 2 -, CH 3 O-CO-S-, benzyl, 4-aminobenzyl or ##STR8## R 5 represents hydrogen or methyl, R 6 represents hydrogen, alkyl with 1 to 4 carbon atoms, phenyl or benzyloxymethyl, R 7 represents hydrogen, amino, methylamino, ethylamino, aminomethyl, methylaminomethyl, ethylaminomethyl, dimethylaminomethyl, hydroxyl or hydroxymethyl and R 8 represents hydrogen, methyl, ethyl or chlorine, X represents hydrogen, fluorine, chlorine or nitro and A represents N or C-R 9 , wherein R 9 represents hydrogen, halogen, such as fluorine or chlorine, methyl or nitro, or A, together with R 1 , can also form a bridge with the structure ##STR9##
Claim 2
Dependent Claim
190 words
A topically applicable formulation comprising by weight about 0.05 to 30% of an antibacterially active compound of the formula ##STR6## in which R 1 represents methyl, ethyl, propyl, isopropyl, cyclopropyl, vinyl, 2-hydroxyethyl, 2-fluoroethyl, methoxy, amino, methylamino, dimethylamino, ethylamino, phenyl, 4-fluorophenyl or 2,4-difluorophenyl, R 2 represents hydrogen, alkyl with 1 to 4 carbon atoms or (5-methyl-2-oxo-1,3-dioxol-4-yl)-methyl, R 3 represents methyl or a cyclic amino group of the formula ##STR7## wherein R 4 represents hydrogen, alkyl with 1 to 4 carbon atoms, 2-hydroxyethyl, allyl, propargyl, 2-oxopropyl, 3-oxobutyl, phenacyl, formyl, CFCL 2 -S-, CFCL 2 -SO 2 -, CH 3 O-CO-S-, benzyl, 4-aminobenzyl or ##STR8## R 5 represents hydrogen or methyl, R 6 represents hydrogen, alkyl with 1 to 4 carbon atoms, phenyl or benzyloxymethyl, R 7 represents hydrogen, amino, methylamino, ethylamino, aminomethyl, methylaminomethyl, ethylaminomethyl, dimethylaminomethyl, hydroxyl or hydroxymethyl and R 8 represents hydrogen, methyl, ethyl or chlorine, X represents hydrogen, fluorine, chlorine or nitro and A represents N or C-R 9 , wherein R 9 represents hydrogen, halogen, such as fluorine or chlorine, methyl or nitro, or A, together with R 1 , can also form a bridge with the structure ##STR9##
Claim 3
Dependent Claim
9 words
01 to 10% of a corticosteroid, and a carrier.
Claim 4
Dependent Claim
9 words
01 to 10% of a corticosteroid, and a carrier.
Claim 5
Dependent Claim
134 words
A topically applicable formulation according to claim 1, wherein the antibacterially active compound is selected from the group consisting of ciprofloxacin, norfloxacin, perfloxacin, amifloxacin, pirfloxacin, ofloxacin and enoxacin, and the corticosteroid is selected from the group consisting of A beclomethasone dipropionate B clobetasol propionate C diflucortolone valerate D fluocinolone acetonide E beclomethasone dipropionate F betamethasone benzoate G betamethasone dipropionate H betamethasone valerate I desonide J desoxymethasone K diflorasone diacetate L diflucortolone valerate M fluclorolone acetonide N fluocinolone acetonide O fluocinonide P fluocortolone Q fluprednidene (fluprednylidene) acetate R flurandrenolone S halcinonide T hydrocortisone butyrate X triamcinolone acetonide Y clobetasone butyrate Z flumethasone pivalate A 1 fluocinolone acetonide B 1 fluocortine butyl ester C 1 fluocortolone D 1 flurandrenalone E 1 hydrocortisone (urea) F 1 dexamethasone G 1 hydrocortisone (alcohol or acetate) and H 1 methylprednisolone.
Claim 6
Dependent Claim
27 words
A topically applicable formulation according to claim 1, in the form of a solution, spray, lotion, gel, ointment, cream, powder, dusting powder spray, paste, suspension, emulsion, foam.
Claim 7
Dependent Claim
87 words
A topically applicable formulation according to claim 1, comprising by weight about (a 1 ) 0.1 to 20% of an active compound of the formula I, (a 2 ) 0.01 to 10% of a corticosteroid, (b) 1 to 40% of a water-soluble gel- or lacquer-forming polymer, (c) 40 to 98% of an organic water-miscible solvent which evaporates faster than water and in which the polymer does not dissolve, and (d) 0.1 to 10% of at least one of a plasticizer, suspending auxiliary, antioxidant, spreading agent or dyestuff.
Claim 8
Dependent Claim
87 words
A topically applicable formulation according to claim 1, comprising by weight about (a 1 ) 0.1 to 5% of an active compound of the formula I, (a 2 ) 0.02 to 5% of a corticosteroid, (b) 1 to 20% of a water-soluble gel- or lacquer-forming polymer, (c) 60 to 90% of an organic water-miscible solvent which evaporates faster than water and in which the polymer does not dissolve, and (d) 0.1 to 10% of at least one of a plasticizer, suspending auxiliary, antioxidant, spreading agent or dyestuff.
Claim 9
Dependent Claim
13 words
A topically applicable formulation according to claim 1, further containing a spreading agent.
Claim 10
Dependent Claim
41 words
A composition according to claim 1 in the form of a gel, the carrier including as a gel-forming agent, cellulose ether, polyacrylic acid, polymethacrylic acid, sodium alginate or propylene glycol alginate, sodium amylopectin semiglycolate, alginic acid, gum arabic or guar gum.
Claim 11
Dependent Claim
19 words
A composition according to claim 7 further containing a linear high molecular weight polysaccharide as a stabilizing gel-forming agent.
Claim 12
Dependent Claim
31 words
A composition according to claim 1 in the form of a suspension having solid particles of 0.1 to 100 μm and a solids content of about 0.5 to 40% by weight.
Claim 13
Dependent Claim
12 words
A composition according to claim 1 in the form of an emulsion.
Claim 14
Dependent Claim
43 words
A composition according to claim 1 in the form of a solution, the carrier comprising at least one solvent selected from the group consisting of ethanol, isopropyl alcohol, propylene glycol, polyethylene glycol, glycerol, methylcellosolve, cellosolve, an ester, morpholine, dioxane, dimethylsulphoxide, water and cyclohexanone.
References Cited (Backward Citations)
US4659603A
Cited
US4681876A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1992-07-03 | 1993-01-02 | 1993-07-04 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1996-07-03 | 1997-01-02 | 1997-07-04 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2000-07-03 | 2001-01-02 | 2001-07-04 | $7700.00 | Window Closed / Lapsed |