Claims for Patent: 5,703,079

Summary for Patent: 5,703,079

Title:	Tetrahydrofuran antifungals
Abstract:	A compound represented by the formula I [I] wherein X is independently both F or both Cl or one X is independently F and the other is independently Cl; R1 is a straight or branched chain (C3 to C8) alkyl group substituted by one or two polyetyher ester groups (e.g., a polyether ester convertible in vivo into a hydroxy group) thereof or a pharmaceutically acceptable salt thereof and pharmaceutical compositions thereof useful for treating and/or preventing fungal infections are disclosed.
Inventor(s):	Anil K. Saksena, Viyyoor M. Girijavallabhan, Raymond G. Lovey, Russell E. Pike, Haiyan Wang, Yi-Tsung Liu, Ashit K. Ganguly, Frank Bennett
Assignee:	Merck Sharp and Dohme LLC
Application Number:	US08/460,400
Patent Claims:	1. A compound represented by the formula I ##STR109## wherein X is independently both F or both Cl or one X is independently F and the other is independently Cl;R1 is a straight or branched chain (C4 to C5) alkyl group substituted by a hydroxy group or a pharmaceutically acceptable salt thereof. 2. A compound of claim 1 wherein R1 is a hydroxy-substituted C4 - or C5 -alkyl group selected from:--*CH(C2 H5)*CH(R4)CH3, --*CH(C2 H5)CH2 CH2 R4, --(CH2)2 --*CH(R4)C2 H5, --*CH(CH3)*CH(R4)CH3, --*CH(C2 H5)CH2 R4 and --*CH(CH3)CH2 CH2 R4 wherein R4 is OH and the carbons with the asterisk(*) have the R or S absolute configuration or a pharmaceutically acceptable salt thereof. 3. The compound of claim 1 wherein R1 is a C4 alkyl group substituted by a hydroxy group. 4. The compound of claim 1 wherein R1 is a C5 alkyl group substituted by a hydroxy group. 5. A compound represented by formula III ##STR110## wherein R5 is ##STR111## wherein R13 is a hydroxy group, or a pharmaceutically acceptable salt thereof. 6. A compound represented by the formula IV ##STR112## wherein R9 =--*CH(C2 H5)CH(R6)CH3 or --*CH(CH3)CH(R6)CH3 wherein R6 is OH or a pharmaceutically acceptable salt thereof. 7. A pharmaceutical composition for treating or preventing fungal infection comprising an antifungally effective amount of a compound of claim 1 together with a pharmaceutically acceptable carrier therefor. 8. A method of treating and/or preventing fungal infections in a mammal afflicted with same which comprises administering an antifungally effective amount of a compound of claim 1 sufficient for such treating or preventing. 9. The pharmaceutical composition of claim 1 wherein the mode of administration is oral or parenteral.