# US 5,707,976 A · Substituted propane-2-OL derivatives

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- Number: US 5,707,976 A
- Document ID: US5707976A
- Status: Granted
- Kind: A
- Application number: 08/605,052
- Filed: 1996-03-04
- Granted: 1998-01-13
- Earliest claimed: 1993-09-23
- Assignees: Richter Gedeon Vegyeszeti Gyar Rt.
- Inventors: Janos Kreidl; Csaba Szantay; Laszlo Czibula; Maria nee Kirjak Farkas; Ida nee Juhasz Deutsch; Mihaly Szegedi; Istvan Hegedus
- Web page: https://patentgrep.com/patent/US5707976A

## CPC

- C07F 7/1804: {Compounds having Si-O-C linkages (Si-O-acyl linkages C07F7/1896)}
- A61P 31/04: Antibacterial agents
- A61P 31/10: Antimycotics
- C07F: ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM (metal-containing porphyrins C07D487/22)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

Anti-Fungal compounds are disclosed of the Formula (I) ##STR1## wherein R.sup.1 is C.sub.1 to C.sub.10 alkyl, phenyl, or phenyl-C.sub.1 to C.sub.6 alkyl, and the phenyl moiety of the two latter groups may carry at least one substituent selected from the group consisting of a halogen atom, C.sub.1 to C.sub.6 alkoxy group, phenyl group, phenoxy group, and trifluorome thyl group; R.sup.2 is a hydrogen atom, a C.sub.1 to C.sub.10 alkyl group or a phenyl group; R.sup.3 and R.sup.4 are independently from each other a C.sub.1 to C.sub.10 alkyl group or a phenyl group; X is a hydrogen atom, halogen atom or a group of the formula (A) ##STR2## and in this formula Y.sup.1 and Y.sup.2 are independently from each other, a --N.dbd. atom or a group of the formula --CH.dbd., or an optical antipode thereof.

## Claims

### Claim 1

A compound of the formula (I) ##STR15## wherein R.sup.1 is C.sub.1-10 alkyl group, a phenyl group or a phenyl-C.sub.1-6 alkyl group, and the phenyl moiety of the two latter groups may carry at least one substituent selected from the group consisting of a halogen atom, C.sub.1-6 alkoxy group, phenyl group, phenoxy group and trifluoromethyl group;
R.sup.2 is a C.sub.1-10 alkyl group or a;
R.sup.3 and R.sup.4 are, independently from each other, a C.sub.1-10 alkyl group;
X is a halogen atom or a group of the formula (A) ##STR16## and in this formulae Y.sup.1 and Y.sup.2 are, independently from each other, a --N.dbd. atom or a group of the formula --CH.dbd., or an optical antipode thereof.

### Claim 2 (depends on 1)

2-(2,4-Difluoro phenyl)-1,3-bis(1,2,4-triazol-1-yl)-2-(trimethylsilyloxy)propane defined in claim 1.

### Claim 3 (depends on 1)

1-(Imi dazol-1-yl)-2-(2,4-difluorophenyl)-3-(1,2,4-triazol-1-yl)-2-(trimethylsilyl oxy) propane defined in claim 1.

### Claim 4 (depends on 1)

2-(2,4-Difluorophenyl)-1,3-bis(imidazol-1-yl)-2-(trimethylsilyloxy) propane defined in claim 1.

### Claim 5 (depends on 1)

1-Chloro-2-(2,4-difluorop henyl)-3-(1,2,4-triazol-1-yl)-2-(trimethylsilyloxy) propane defined in claim 1.

### Claim 6 (depends on 1)

1-Chloro-2-(2,4-difluorophenyl)-3-(imidazol-1-yl)-2-(trimethylsilyloxy) propane defined in claim 1.

### Claim 7 (depends on 1)

2-(2,4-Dichlorophenyl)-1- (1,2,4-triazol-1-yl)-3-(imidazol-1-yl)-2-(trimethylsilyloxy) propane defined in claim 1.

### Claim 8 (depends on 1)

A pharmaceutical composition of fungicidal action which comprises a fungicidally effective amount of a compound of the formula (I), as defined in claim 1, or an optical antipode thereof, together with a pharmaceutically acceptable inert carrier.

### Claim 9 (depends on 1)

A method of treating a fungicidal infection in a mammal which comprises the steps of administering to said mammal, a fungicidally effective amount of a compound of the formula (I) as defined in claim 1, or an optical antipode thereof, alone or in the form of a pharmaceutical composition.