Ketolide antibacterials

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United States of America Patent

PATENT NO 6590083
SERIAL NO

09691540

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ATTORNEY / AGENT: (SPONSORED)

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Abstract

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The present invention includes compounds of the formula ##STR1## wherein: X is hydrogen or halide; R.sup.2 is hydrogen, acyl, or a hydroxy protecting group; R.sup.6 is hydrogen, hydroxyl, or --OR.sup.a wherein R.sup.a is a substituted or unsubstituted moiety selected from the group consisting of C.sub.1 -C.sub.10 alkyl, C.sub.2 -C.sub.10 alkenyl, C.sub.2 -C.sub.10 alkynyl, aryl, heterocyclo, aryl(C.sub.1 -C.sub.10)alkyl, aryl(C.sub.2 -C.sub.10)alkenyl, aryl(C.sub.2 -C.sub.10)alkynyl, heterocyclo(C.sub.1 -C.sub.10)alkyl, heterocyclo(C.sub.2 -C.sub.10)alkenyl, and heterocyclo(C.sub.2 -C.sub.10)alkynyl; R.sup.13 is hydrogen or a substituted or unsubstituted moiety wherein the moiety is selected from the group consisting of methyl; C.sub.3 -C.sub.10 alkyl, C.sub.2 -C.sub.10 alkenyl, C.sub.2 -C.sub.10 alkynyl, aryl, heterocyclo, aryl(C.sub.1 -C.sub.10)alkyl, aryl(C.sub.2 -C.sub.10)alkenyl, aryl(C.sub.2 -C.sub.10)alkynyl, heterocyclo(C.sub.1 -C.sub.10)alkyl, heterocyclo(C.sub.2 -C.sub.10)alkenyl, and heterocyclo(C.sub.2 -C.sub.10)alkynyl; and, R is hydrogen or a substituted or unsubstituted moiety wherein the moiety is selected from the group consisting of C.sub.1 -C.sub.10 alkyl, C.sub.2 -C.sub.10 alkenyl, C.sub.2 -C.sub.10 alkynyl, aryl, heterocyclo, aryl(C.sub.1 -C.sub.10)alkyl, aryl(C.sub.2 -C.sub.10)alkenyl, aryl(C.sub.2 -C.sub.10)alkynyl, heterocyclo(C.sub.1 -C.sub.10)alkyl, heterocyclo(C.sub.2 -C.sub.10)alkenyl, and heterocyclo(C.sub.2 -C.sub.10)alkynyl; and the pharmaceutically acceptable salts, esters and pro-drug forms thereof. These compounds possess anti-infective activity and are useful for the treatment of bacterial and protozoal infections.

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Patent Owner(s)

Patent OwnerAddress
ORTHO-MCNEIL PHARMACEUTICAL INCU S ROUTE #202 RARITAN NJ 08869-0602

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Ashley, Gary Alameda, CA 55 477
Chu, Daniel T W Santa Clara, CA 9 106
Grant, Eugene B Edison, NJ 7 57
Henninger, Todd C Neshanic Station, NJ 10 87
Hlasta, Dennis Doylestown, PA 7 30
Khosla, Chaitin Palo Alto, CA 3 52

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