US4871741A
Expired / Lapsed
US
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Method of controlling mycotic infections and compositions therefor
Assignee: Merck and Co Inc
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Filing: 1987-02-02
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Granted: 1989-10-03
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Expires: 2007-02-02
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
2026-10-23 14:42
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/495
Claims Analysis
Total Claims: 12
Claim 1
Independent Claim
66 words
A fungicidal composition suitable for treating mycotic infections comprising a fungicidal amount in combination of: (1) from 200 to 400 milligrams of a compound having 14α-methyldemethylase inhibitor activity and which is named cis-1-acetyl-4-[4-[[2-(2,4-dichlorophenyl-2-(1H-imidazol e-1-yllmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]-piperazine(ketoconazole), and (b 2) from 200 to 400 milligrams of a compound having HmG-CoA reductase inhibitor activity and which is a water-soluble salt of mevinolinic acid in admixture with a pharmaceutically effective carrier.
Claim 2
Dependent Claim
66 words
A fungicidal composition suitable for treating mycotic infections comprising a fungicidal amount in combination of: (1) from 200 to 400 milligrams of a compound having 14α-methyldemethylase inhibitor activity and which is named cis-1-acetyl-4-[4-[[2-(2,4-dichlorophenyl-2-(1H-imidazol e-1-yllmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]-piperazine(ketoconazole), and (b 2) from 200 to 400 milligrams of a compound having HmG-CoA reductase inhibitor activity and which is a water-soluble salt of mevinolinic acid in admixture with a pharmaceutically effective carrier.
Claim 3
Dependent Claim
17 words
A composition according to claim 1 wherein the water-soluble salt of mevinolinic acid is the ammonium salt.
Claim 4
Dependent Claim
11 words
A composition according to claim 1 which is an oral composition.
Claim 5
Dependent Claim
11 words
A composition according to claim 1 which is a parenteral composition.
Claim 6
Independent Claim
80 words
A method for killing fungi causing mycotic infections comprising administering to the site infected with fungi, a fungicidally effective amount of a composition comprising: (1) 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) in an amount of from 2.85 to 4.75 mg/kg of body weight and (2) a compound having HmG-CoA reductase inhibitor activity and is a water-soluble salt of 7-[1,2,6,7,8,8a(R) hexahydro-2(S),6(R)-dimethyl-8(S)-(2(S)-methylbutyryloxy) naphthyl-1(S)]-3(R),5(R)dihydroxypheptanoic acid (mevinolinic acid) in an amount of from 2.85 to 4.75 mg/kg of body weight.
Claim 7
Independent Claim
80 words
A method for killing fungi causing mycotic infections comprising administering to the site infected with fungi, a fungicidally effective amount of a composition comprising: (1) 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) in an amount of from 2.85 to 4.75 mg/kg of body weight and (2) a compound having HmG-CoA reductase inhibitor activity and is a water-soluble salt of 7-[1,2,6,7,8,8a(R) hexahydro-2(S),6(R)-dimethyl-8(S)-(2(S)-methylbutyryloxy) naphthyl-1(S)]-3(R),5(R)dihydroxypheptanoic acid (mevinolinic acid) in an amount of from 2.85 to 4.75 mg/kg of body weight.
Claim 8
Independent Claim
77 words
A method for treating mycotic infections comprising directing to the site where control is desired, a fungicidally effective amount of: (1) a compound having 14α-methyldemethylase inhibitor activity and named cis-1-acetyl-4-[4-[[2-(2,4-dichlorophpenyl)2-(1H-imidazole-1ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]piperazine (ketoconazole) in an amount of from about 2.85 to 4.75 mg/kg of body weight and (2) a compound having HmG-CoA reductase inhibitor activity and is a water soluble salt of 7-[1,2,6,7,8,8a(R)-hexahydro-2(S),6(R)-dimethyl-8(S)-(2(S)-methylbutyryloxy)naphthyl-1(S)]-3(R),5(R)-dihydroxyheptanoic acid (mevinolinic acid) in an amount of from about 2.85 to 4.75 mg/kg of body weight.
Claim 9
Independent Claim
77 words
A method for treating mycotic infections comprising directing to the site where control is desired, a fungicidally effective amount of: (1) a compound having 14α-methyldemethylase inhibitor activity and named cis-1-acetyl-4-[4-[[2-(2,4-dichlorophpenyl)2-(1H-imidazole-1ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]piperazine (ketoconazole) in an amount of from about 2.85 to 4.75 mg/kg of body weight and (2) a compound having HmG-CoA reductase inhibitor activity and is a water soluble salt of 7-[1,2,6,7,8,8a(R)-hexahydro-2(S),6(R)-dimethyl-8(S)-(2(S)-methylbutyryloxy)naphthyl-1(S)]-3(R),5(R)-dihydroxyheptanoic acid (mevinolinic acid) in an amount of from about 2.85 to 4.75 mg/kg of body weight.
Claim 10
Dependent Claim
13 words
A method according to claim 6 wherein the water-soluble salt is ammonium mevinolinate.
Claim 11
Dependent Claim
13 words
A method according to claim 6 wherein the treatment is by parenteral administration.
Claim 12
Dependent Claim
13 words
A method according to claim 6 wherein the treatment is by oral administration.
References Cited (Backward Citations)
US4319039A
Cited
US4342767A
Cited
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