Fungicidal compositions and method

Claim 1

A synergistic antifungal composition suitable for treating mycotic infections in unit dosage form comprising a mycotic infection controlling amount in combination of: (1) from about 200 to 400 milligrams of a 14α-methyldemethylase inhibiting azole compound selected from the group consisting of (a) cis-1-acetyl-4-[4-[[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-yl-methyl)-1,3-dioxolan-4-yl]-methoxyl]phenyl]piperazine (ketoconazole), (b) α-(2,4-difluorophenyl)-α-(1H-1,2,4-triazol-1-yl-methyl)-1H-1,2-4-triazol-1-ethanol (fluconazole), (c) cis-4-[4-[4-[4-[[2-(2,4-dichlorophenyl)-2-(1H-1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]-methoxy]-phenyl]1-piperazinyl]phenyl-2,4-dihydro-2-(1-methylpropyl)-3H-1,2,4-triazol-3-one (itraconazole) and (d) 1-[2,4-dichloro-β-(2,4-dichlorobenzyloxy)-phenethyl]imidazole nitrate (miconazole); and (2) from about 200 to 400 milligrams of a β-lactone compound having the formula ##STR2## or a salt thereof wherein said compounds are in admixture with a pharmaceutically acceptable carrier.

Claim 11

A method for treating mycotic infections in a patient having such an infection comprising directing to the site in said patient where control is desired, a fungicidally effective amount of: (1) a 14α-methyldemethylase inhibiting azole compound selected from the group consisting of (a) cis-1-acetyl-4-[4-[[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-yl-methyl)-1,3-dioxolan-4-yl]-methoxyl]phenyl]piperazine (ketoconazole), (b) α-(2,4-difluorophenyl)-α-(1H-1,2,4-triazol-1-yl-methyl)-1H-1,2-4-triazole-1-ethanol (fluconazole), (c) cis-4-[4-[4-[4-[[2-(2,4-dichlorophenyl)-2-(1H-1,2,4-triazol-1-yl-methyl)-1,3-dioxolan-4-yl]-methoxy]-phenyl]-1-piperazinyl]phenyl-2,4-dihydro-2-(1-methylpropyl)-3H-1,2,4-triazol-3-one (itraconazole) and (d) 1-[2,4-dichloro-β-(2,4-dichlorobenzyloxy)phenethyl]imidazole nitrate (miconazole); and (2) from about 200 to 400 milligrams of a β-lactone compound having the formula ##STR3## or a salt thereof wherein the azole compound is employed in an amount of from about 2.85 to 4.75 mg/kg of body weight and the β-lactone compound or salt thereof is employed in an amount of from about 2.85 to 4.75 mg/kg of body weight.

Claim 12

A method for treating mycotic infections in a patient having such an infection comprising directing to the site in said patient where control is desired, a fungicidally effective amount of: (1) a 14α-methyldemethylase inhibiting azole compound selected from the group consisting of (a) cis-1-acetyl-4-[4-[[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-yl-methyl)-1,3-dioxolan-4-yl]-methoxyl]phenyl]piperazine (ketoconazole), (b) α-(2,4-difluorophenyl)-α-(1H-1,2,4-triazol-1-yl-methyl)-1H-1,2-4-triazole-1-ethanol (fluconazole), (c) cis-4-[4-[4-[4-[[2-(2,4-dichlorophenyl)-2-(1H-1,2,4-triazol-1-yl-methyl)-1,3-dioxolan-4-yl]-methoxy]-phenyl]-1-piperazinyl]phenyl-2,4-dihydro-2-(1-methylpropyl)-3H-1,2,4-triazol-3-one (itraconazole) and (d) 1-[2,4-dichloro-β-(2,4-dichlorobenzyloxy)phenethyl]imidazole nitrate (miconazole); and (2) from about 200 to 400 milligrams of a β-lactone compound having the formula ##STR3## or a salt thereof wherein the azole compound is employed in an amount of from about 2.85 to 4.75 mg/kg of body weight and the β-lactone compound or salt thereof is employed in an amount of from about 2.85 to 4.75 mg/kg of body weight.

Claim 18

A method for killing fungi causing mycotic infections comprising administering to the site infected with fungi (1) a β-lactone compound having the formula ##STR4## or a salt thereof, and (2) cis-1-acetyl-4-[4-[[2-(2,4-dichlorophenyl)-2-(1H-imidazole-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]-phenyl]piperazine (ketoconazole), wherein the β-lactone compound or salt thereof is employed in an amount of from about 2.85 to 4.75 mg/kg of body weight and ketoconazole is employed in an amount of from about 2.85 to 4.75 mg/kg of body weight.

Claim 19

A method for killing fungi causing mycotic infections comprising administering to the site infected with fungi (1) a β-lactone compound having the formula ##STR4## or a salt thereof, and (2) cis-1-acetyl-4-[4-[[2-(2,4-dichlorophenyl)-2-(1H-imidazole-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]-phenyl]piperazine (ketoconazole), wherein the β-lactone compound or salt thereof is employed in an amount of from about 2.85 to 4.75 mg/kg of body weight and ketoconazole is employed in an amount of from about 2.85 to 4.75 mg/kg of body weight.