Importance

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Abstract

The present invention provides novel macrolide compounds of the formulas 1 wherein: R is hydrogen, substituted C.sub.1-C.sub.10 alkyl, unsubstituted C.sub.1-C.sub.10 alkyl, substituted C.sub.2-C.sub.10 alkenyl, unsubstituted C.sub.2-C.sub.10 alkenyl, substituted C.sub.2-C.sub.10 alkynyl, unsubstituted C.sub.2-C.sub.10 alkynyl, substituted aryl, unsubstituted aryl, substituted alkylaryl, unsubstituted alkylaryl, substituted alkenylaryl, unsubstituted alkenylaryl, substituted alkynylaryl, or unsubstituted alkynylaryl; R.sup.0 is hydroxyl or methoxy; R.sup.1 is selected from the group consisting of hydrogen, hydroxyl, halide, NH.sub.2, OR.sup.9, 2 where R.sup.9 is substituted C.sub.1-C.sub.10 alkyl, unsubstituted C.sub.1-C.sub.10 alkyl, substituted C.sub.2-C.sub.10 alkenyl, unsubstituted C.sub.2-C.sub.10 alkenyl, substituted C.sub.2-C.sub.10 alkynyl, unsubstituted C.sub.2-C.sub.10 alkynyl, substituted aryl, unsubstituted aryl, substituted alkylaryl, unsubstituted alkylaryl, substituted alkenylaryl, unsubstituted alkenylaryl, substituted alkynylaryl, or unsubstituted alkynylaryl, and R.sup.10 and R.sup.11 are each independently hydrogen, substituted C.sub.1-C.sub.10 alkyl, unsubstituted C.sub.1-C.sub.10 alkyl, substituted C.sub.2-C.sub.10 alkenyl, unsubstituted C.sub.2-C.sub.10 alkenyl, substituted C.sub.2-C.sub.10 alkynyl, unsubstituted C.sub.2-C.sub.10 alkynyl, substituted aryl, unsubstituted aryl, substituted alkylaryl, unsubstituted alkylaryl, substituted alkenylaryl, unsubstituted alkenylaryl, substituted alkynylaryl, or unsubstituted alkynylaryl; R.sup.1 and R.sup.3 are each independently selected from the group consisting of hydrogen, substituted C.sub.1-C.sub.10 alkyl, unsubstituted C.sub.1-C.sub.10 alkyl, substituted C.sub.2-C.sub.10 alkenyl, unsubstituted C.sub.2-C.sub.10 alkenyl, substituted C.sub.2-C.sub.10 alkynyl, unsubstituted C.sub.2-C.sub.10 alkynyl, substituted aryl, unsubstituted aryl, substituted alkylaryl, unsubstituted alkylaryl, substituted alkenylaryl, unsubstituted alkenylaryl, substituted alkynylaryl, or unsubstituted alkynylaryl, or R.sup.2 and R.sup.3 together form a cycloalkyl or an aryl moiety; R.sup.4 is hydrogen or methyl; R.sup.5 is hydroxyl or oxo; R is hydrogen, hydroxyl, or OR.sup.12 where R.sup.12 is substituted C.sub.1-C.sub.10 alkyl, unsubstituted C.sub.1-C.sub.10 alkyl, substituted C.sub.2-C.sub.10 alkenyl, unsubstituted C.sub.2-C.sub.10 alkenyl, substituted C.sub.2-C.sub.10 alkynyl, or unsubstituted C.sub.2-C.sub.10 alkynyl; R.sup.7 is methyl, unsubstituted C.sub.3-C.sub.10 alkyl, substituted C.sub.1-C.sub.10 alkyl, substituted C.sub.2-C.sub.10 alkenyl, unsubstituted C.sub.2-C.sub.10 alkenyl, substituted C.sub.2-C.sub.10 alkynyl, unsubstituted C.sub.2-C.sub.10 alkynyl, substituted alkylaryl, unsubstituted alkylaryl, substituted alkenylaryl, unsubstituted alkenylaryl, substituted alkynylaryl, or unsubstituted alkynylaryl; R.sup.8 is unsubstituted C.sub.1-C.sub.10 alkyl, substituted C.sub.1-C.sub.10 alkyl, substituted C.sub.2-C.sub.10 alkenyl, unsubstituted C.sub.2-C.sub.10 alkenyl, substituted C.sub.2-C.sub.10 alkynyl, unsubstituted C.sub.2-C.sub.10 alkynyl, substituted alkylaryl, unsubstituted alkylaryl, substituted alkenylaryl, unsubstituted alkenylaryl, substituted alkynylaryl, or unsubstituted alkynylaryl; R.sup.13 is hydrogen, unsubstituted C.sub.1-C.sub.10 alkyl, substituted C.sub.1-C.sub.10 alkyl, substituted C.sub.2-C.sub.10 alkenyl, unsubstituted C.sub.2-C.sub.10 alkenyl, substituted C.sub.2-C.sub.10 alkynyl, unsubstituted C.sub.2-C.sub.10 alkynyl, substituted alkylaryl, unsubstituted alkylaryl, substituted alkenylaryl, unsubstituted alkenylaryl, substituted alkynylaryl, or unsubstituted alkynylaryl; R.sup.17 is hydrogen or methyl; x is a single or a double bond; and, Y is hydrogen, substituted C.sub.1-C.sub.10 alkyl, unsubstituted C.sub.1-C.sub.10 alkyl, substituted C.sub.2-C.sub.10 alkenyl, unsubstituted C.sub.2-C.sub.10 alkenyl, substituted C.sub.2-C.sub.10 alkynyl, unsubstituted C.sub.2-C.sub.10 alkynyl, substituted aryl, unsubstituted aryl, substituted alkylaryl, unsubstituted alkylaryl, substituted alkenylaryl, unsubstituted alkenylaryl, substituted alkynylaryl, unsubstituted alkynylaryl, unsubstituted cladinose, or substituted cladinose.

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First Claim