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Claims for Patent: 5,661,151

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Claims for Patent: 5,661,151

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 hydroxy moieties, an ether or ester thereof (e.g., a polyether ester amino acid ester or phosphate ester) 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)
Application Number:08/460,752
Patent Claims: 1. A compound represented by the formula ##STR100## or an ester group thereof convertible in vivo into OH; or a pharmaceutically acceptable salt thereof.

2. A compound of claim 1 wherein the ester group convertible in vivo into OH is a polyether ester, a phosphate ester, a sulfate ester, a heterocyclic ester, an alkanoate ester, an alkenoate ester, an amino acid ester or an acid ester.

3. A compound of claim 1 wherein the ester group convertible in vivo into OH is a polyether ester represented by the formula ##STR101## wherein R.sub.7 is a (C.sub.1 -C.sub.6) straight or branched chain alkyl group or H, s is an integer from 1 to 6, t is an integer from 1 to 6, and R.sub.8 is R.sub.7 or --CHR.sub.7).sub.s --CO.sub.2 R.sub.7.

4. A compound of claim 1 wherein the ester group convertible in vivo into OH is a phosphate ester represented by the formula ##STR102## wherein z is 0 or 1, R.sub.7 is a (C.sub.1 -C.sub.6) straight or branched chain alkyl group or H, f and n are independently an integer from 0 to 6, m is zero or 1 and W is H, CH.sub.2 Ar or and Ar is phenyl, phenyl substituted by halo, nitro, cyano or trihalomethyl.

5. A compound of claim 1 wherein the ester group convertible in vivo into OH is a heterocyclic ester represented by the formula ##STR103## wherein R.sub.7 is a (C.sub.1 -C.sub.6) straight or branched chain alkyl group or H; w is an integer of from 1 to 5; q and q' are independently 1 to 4 and Y is CHR.sub.7,--O--, NH, NR.sub.7, S, SO or SO.sub.2.

6. A compound of claim 1 wherein the ester group convertible in vivo into OH is an .alpha.-amine acid ester.

7. A compound of claim 1 wherein the esters of the compound represented by the formula of claim 1 have a solubility in a pharmaceutically acceptable aqueous medium of at least about 1 to about 50 mg/mL.

8. 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.

9. 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.

10. The pharmaceutical composition of claim 8 wherein the mode of administration is oral or parenteral.

11. A compound represented by the formula ##STR104## or a pharmaceutically acceptable salt thereof.

12. A pharmaceutically composition for treating or preventing a fungal infection comprising an antifungally effective amount of the compound of claim 11 together with a pharmaceutically acceptable carrier therefor.

13. A method of treating and/or preventing a fungal infection in a mammal afflicted with same which comprises administering an antifungally effective amount of the compound of claim 11 sufficient for such treating or preventing.
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