Details for Patent: 5,703,079
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Title: | Tetrahydrofuran antifungals |
Abstract: | A compound represented by the formula I ##STR1## wherein X is independently both F or both Cl or one X is independently F and the other is independently Cl; R.sub.1 is a straight or branched chain (C.sub.3 to C.sub.8) 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): | Saksena; Anil K. (Upper Montclair, NJ), Girijavallabhan; Viyyoor M. (Parsippany, NJ), Lovey; Raymond G. (West Caldwell, NJ), Pike; Russell E. (Stanhope, NJ), Wang; Haiyan (Dayton, NJ), Liu; Yi-Tsung (Morris Township, NJ), Ganguly; Ashit K. (Upper Montclair, NJ), Bennett; Frank (Piscataway, NJ) |
Assignee: | Schering Corporation (Kenilworth, NJ) |
Filing Date: | Jun 02, 1995 |
Application Number: | 08/460,400 |
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; R.sub.1 is a straight or branched chain (C.sub.4 to C.sub.5) alkyl group substituted by a hydroxy group or a pharmaceutically acceptable salt thereof. 2. A compound of claim 1 wherein R.sub.1 is a hydroxy-substituted C.sub.4 - or C.sub.5 -alkyl group selected from: --*CH(C.sub.2 H.sub.5)*CH(R.sub.4)CH.sub.3, --*CH(C.sub.2 H.sub.5)CH.sub.2 CH.sub.2 R.sub.4, --(CH.sub.2).sub.2 --*CH(R.sub.4)C.sub.2 H.sub.5, --*CH(CH.sub.3)*CH(R.sub.4)CH.sub.3, --*CH(C.sub.2 H.sub.5)CH.sub.2 R.sub.4 and --*CH(CH.sub.3)CH.sub.2 CH.sub.2 R.sub.4 wherein R.sub.4 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 R.sub.1 is a C.sub.4 alkyl group substituted by a hydroxy group. 4. The compound of claim 1 wherein R.sub.1 is a C.sub.5 alkyl group substituted by a hydroxy group. 5. A compound represented by formula III ##STR110## wherein R.sub.5 is ##STR111## wherein R.sub.13 is a hydroxy group, or a pharmaceutically acceptable salt thereof. 6. A compound represented by the formula IV ##STR112## wherein R.sub.9 =--*CH(C.sub.2 H.sub.5)CH(R.sub.6)CH.sub.3 or --*CH(CH.sub.3)CH(R.sub.6)CH.sub.3 wherein R.sub.6 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. |