Antifungal compounds

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Carbohydrate doai

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536 65, 536 71, 536115, A61K 3170, C07H 1708

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active

052043304

ABSTRACT:
A compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein: R.sub.1 is a group --CH.sub.2 --X where X is hydrogen, halogen, --CN, --N.sub.3, --OC(O)R.sub.5, --S(O).sub.n R.sub.5, --SH, --OC(O)NHR.sub.5, --NHCONHR.sub.5 or --NR.sub.6 R.sub.7, where R.sub.5 is hydrogen optionally substituted C.sub.1-8 alkyl, or aryl, heteroaryl, aryl C.sub.1-4 alkyl or heteroaryl C.sub.1-4 alkyl in each of which the aromatic moiety is optionally substituted with the proviso that when X is --S(O).sub.n R.sub.5, R.sub.5 does not represent hydrogen, R.sub.6 and R.sub.7 are independently hydrogen or C.sub.116 alkyl, or one of R.sub.6 and R.sub.7 is hydrogen and the other is --formyl, C.sub.2-8 alkanoyl, dialkoxyphosphoryl, aroyl, heteroaroyl, aryl C.sub.1-4 alkanoyl, heteroaryl C.sub.1-4 alkanoyl, C.sub.1-8 alkylsulphonyl, arylsulphonyl, heteroarylsulphonyl, aryl C.sub.1-4 alkylsulphonyl or heteroaryl C.sub.1-4 alkylsulphonyl, where any aromatic moiety in R.sub.6 or R.sub.7 is optionally substituted, and n is 0, 1 or 2; R.sub.2 is hydroxy or optionally substituted C.sub.1-8 alkoxy; R.sub.3 is an amino group or a derivative thereof; and each R.sub.4 is hydrogen.

REFERENCES:
patent: 4035568 (1977-07-01), Schaffner et al.
patent: 4468511 (1984-08-01), Kirst et al.
patent: 4804749 (1989-02-01), Fujiwara et al.
K. C. Nicolaou et al., Journal of the American Chemical Society vol. 110, 1988, pp. 4660-4672.

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