Claims
- 1. A compound represented by the formula I ##STR107## 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 -C.sub.5) alkyl group substituted by an amino acid ester group convertible in vivo into a hydroxy moiety
- or a pharmaceutically acceptable salt thereof.
- 2. A compound of claim 1 wherein R.sub.1 is a C.sub.4 - or C.sub.5 -alkyl group selected from:
- --C.sup.* H(C.sub.2 H.sub.5)C.sup.* H(R.sub.4)CH.sub.3, --C.sup.* H(C.sub.2 H.sub.5)CH.sub.2 CH.sub.2 R.sub.4,
- --(CH.sub.2).sub.2 --C.sup.* H(R.sub.4)C.sub.2 H.sub.5, --C.sup.* H(CH.sub.3)CH(R.sub.4)CH.sub.3,
- --C.sup.* H(C.sub.2 H.sub.5)CH.sub.2 R.sub.4 and --C.sup.* H(CH.sub.3)CH.sub.2 CH.sub.2 R.sub.4
- wherein R.sub.4 is amino acid ester group convertible in vivo into OH and the carbons with the asterisk (*) have the R or S absolute configuration or a pharmaceutically acceptable salt thereof.
- 3. A compound represented by formula III ##STR108## wherein R.sub.5 is ##STR109## wherein R.sub.11 is an amino acid ester group convertible in vivo into a hydroxy group, or a pharmaceutically acceptible salt thereof.
- 4. A compound represented by the formula IV ##STR110## wherein R.sub.9 =--C.sup.* H(C.sub.2 H.sub.5)CH(R.sub.6)CH.sub.3 or --C.sup.* H(CH.sub.3)CH(R.sub.6)CH.sub.3
- wherein R.sub.6 is an amino acid ester group convertible in vivo into OH or a pharmaceutically acceptable salt thereof.
- 5. A compound of claim 4 wherein R.sub.6 is a dipeptide ester.
- 6. A compound of claim 5 wherein the dipeptide ester is the ester of glycylglycine, i.e. --OCOCH.sub.2 NHCOCH.sub.2 NH.sub.2.
- 7. A compound of claim 4 wherein R.sub.6 is the ester of L-glycine, i.e. --OCOCH.sub.2 NH.sub.2.
- 8. A compound of claim 4 wherein R.sub.6 is the ester of 2,4-diaminobutanoic acid, i.e., --COCH(NH.sub.2)CH.sub.2 CH.sub.2 NH.sub.2.
- 9. The compound of claim 4 wherein R.sub.6 is an ester of leucine., i.e., --OCOCH(NH.sub.2)CH.sub.2 CH(CH.sub.3).sub.2.
- 10. The compound of claim 4 wherein R.sub.6 is an ester of isoleucine, i.e., --OCOCH(NH.sub.2)(CH.sub.2)CHC.sub.2 H.sub.5.
- 11. The compound of claim 4 wherein R.sub.6 is an ester of valine, i.e., --OCOCH(NH.sub.2)CH(CH.sub.3).sub.2.
- 12. The compound of claim 4 wherein R.sub.6 is an ester of ##STR111##
- 13. 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.
- 14. 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.
- 15. The pharmaceutical composition of claim 13 wherein the mode of administration is oral or parenteral.
- 16. A compound represented by the formula ##STR112## wherein R.sub.11 is an amino ester group convertible in vivo into a hydroxy group;
- or a pharmaceutically acceptable salt thereof.
- 17. A compound of claim 16 wherein R.sub.11 is --OCOCH.sub.2 NH.sub.2 or a pharmaceutically acceptable salt thereof.
- 18. A compound of claim 16 wherein R.sub.11 is a natural (L) .alpha.-amino acid ester or a pharmaceutically acceptable salt thereof.
- 19. A pharmaceutical composition for treating or preventing a fungal infection comprising an antifungally effective amount of the compound of claim 16 together with a pharmceutically acceptable carrier therefor.
- 20. 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 16 sufficient for such treating or preventing.
CROSS-REFERENCE TO RELATED APPLICATIONS
This is a continuation-in-part application of International Application No. PCT/US94/14236, filed 20 Dec. 1994 which is a continuation-in-part of U.S. patent application Ser. No. 08/171,083, filed Dec. 21, 1993 now abandoned.
US Referenced Citations (2)
Number |
Name |
Date |
Kind |
4791111 |
Heeres et al. |
Dec 1988 |
|
5039676 |
Saksena et al. |
Aug 1991 |
|
Foreign Referenced Citations (2)
Number |
Date |
Country |
0539938A1 |
May 1993 |
EPX |
WO 8904829 |
Jun 1989 |
WOX |
Non-Patent Literature Citations (1)
Entry |
Sinkula, in Annual Reports in Medicinal Chemistry vol. 10, Chapter 31, pp. 306-315 (1975). |
Continuation in Parts (1)
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Number |
Date |
Country |
Parent |
171083 |
Dec 1993 |
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