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US4782059A Expired / Lapsed US ⏱️ 0.0 years remaining

Method of controlling mycotic infections and compositions therefor

Assignee: Merck and Co Inc
•
Filing: 1986-09-29
•
Granted: 1988-11-01
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Expires: 2006-09-29
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Abstract

Abstract Certain fungistats when employed in combination have been found to exhibit synergistic antifungal properties and further exhibit fungicidal properties.

Inventors

  • 👤 Hans H. Gadebusch
  • 👤 Mary E. Valiant

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-24 21:11
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/495

Claims Analysis

Total Claims: 10
Claim 1
Independent Claim 94 words
A method for treating subjects with mycotic infecions comprising directing to the site where control is desired by administering a fungicidally effective amount of: (1) a compound having 14α-methyldemethylase inhibitor activity and named cis-1-acetyl-4-[4-[[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]-methoxy]phenyl]piperazine(ketoconazole); and (2) a compound having squalene epoxidase inhibitor activity and named N-methyl-N-(3-phenylpropenyl)-1-naphthalenemethamine hydrochloride (naftifine); wherein the compound having 14α-methyldemethylase inhibitor activity is employed in an amount of from about 2.85 to 4.75 mg/kg of body weight, and wherein the compound having squalene epoxidase inhibitor activity is employed in an amount of from about 2.85 to 4.75 mg/kg of body weight.
Claim 2
Independent Claim 94 words
A method for treating subjects with mycotic infecions comprising directing to the site where control is desired by administering a fungicidally effective amount of: (1) a compound having 14α-methyldemethylase inhibitor activity and named cis-1-acetyl-4-[4-[[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]-methoxy]phenyl]piperazine(ketoconazole); and (2) a compound having squalene epoxidase inhibitor activity and named N-methyl-N-(3-phenylpropenyl)-1-naphthalenemethamine hydrochloride (naftifine); wherein the compound having 14α-methyldemethylase inhibitor activity is employed in an amount of from about 2.85 to 4.75 mg/kg of body weight, and wherein the compound having squalene epoxidase inhibitor activity is employed in an amount of from about 2.85 to 4.75 mg/kg of body weight.
Claim 3
Dependent Claim 13 words
A method according to claim 1 wherein the treatment is by parenteral administration.
Claim 4
Dependent Claim 13 words
A method according to claim 1 wherein the treatment is by oral administration.
Claim 5
Dependent Claim 68 words
An oral pharmaceutical composition suitable for treating mycotic infections in unit dosage form comprising per dosage unit of: (1) from about 200 to 400 milligrams of a compound having 14α-methyldemethylase inhibitor activity and named cis-1-acetyl-4-[4-[[2-(2,4-dichlorophenyl)-2-(1H-imidazole-1-ylmethyl)-1,3-dioxolan-4-yl]-methoxy]-phenyl]piperazine (ketoconazole); and (2) from about 200 to 400 milligrams of a compound having squalene epoxidase inhibitor activity and named N-methyl-N-(3-phenylpropenyl-1-naphthalenemethamine hydrochloride (naftifine); wherein said compounds are in admixture with a pharmaceutically acceptable carrier.
Claim 6
Dependent Claim 68 words
An oral pharmaceutical composition suitable for treating mycotic infections in unit dosage form comprising per dosage unit of: (1) from about 200 to 400 milligrams of a compound having 14α-methyldemethylase inhibitor activity and named cis-1-acetyl-4-[4-[[2-(2,4-dichlorophenyl)-2-(1H-imidazole-1-ylmethyl)-1,3-dioxolan-4-yl]-methoxy]-phenyl]piperazine (ketoconazole); and (2) from about 200 to 400 milligrams of a compound having squalene epoxidase inhibitor activity and named N-methyl-N-(3-phenylpropenyl-1-naphthalenemethamine hydrochloride (naftifine); wherein said compounds are in admixture with a pharmaceutically acceptable carrier.
Claim 7
Dependent Claim 15 words
A composition according to claim 4 in which the unit dosage form is a tablet.
Claim 8
Dependent Claim 15 words
A composition according to claim 4 in which the unit dosage form is a capsule.
Claim 9
Dependent Claim 66 words
A parenteral pharmaceutical composition suitable for treating mycotic infection in unit dosage form: comprising per dosage unit of: from about 200 to 400 milligrams of a compound having 14α-methyldemethylase inhibitor activity and named cis-1-acetyl-4-[4-[[2-(2,4-dichlorophenyl)-2-(1H-imidazol-ylmethyl)-1,3-dioxolan-4-yl] -methoxy]phenyl]piperazine (ketoconazole); and from about 200 to 400 milligrams of a compound having squalene epoxidase inhibitor activity and named N-methyl-N-(3-phenylpropenyl)-1-naphthalenemethamine hydrochloride (naftifine); wherein said compounds are in admixture in aqueous parenteral compositions.
Claim 10
Dependent Claim 66 words
A parenteral pharmaceutical composition suitable for treating mycotic infection in unit dosage form: comprising per dosage unit of: from about 200 to 400 milligrams of a compound having 14α-methyldemethylase inhibitor activity and named cis-1-acetyl-4-[4-[[2-(2,4-dichlorophenyl)-2-(1H-imidazol-ylmethyl)-1,3-dioxolan-4-yl] -methoxy]phenyl]piperazine (ketoconazole); and from about 200 to 400 milligrams of a compound having squalene epoxidase inhibitor activity and named N-methyl-N-(3-phenylpropenyl)-1-naphthalenemethamine hydrochloride (naftifine); wherein said compounds are in admixture in aqueous parenteral compositions.

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) 1991-11-01 1992-05-02 1992-11-01 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1995-11-01 1996-05-02 1996-11-01 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1999-11-01 2000-05-02 2000-11-01 $7700.00 Window Closed / Lapsed

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