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Title:
MACROLIDE ANTIINFECTIVE AGENTS
Document Type and Number:
WIPO Patent Application WO2000063225
Kind Code:
A3
Abstract:
Compounds of formula (1), (2) or (3) or the 10,11-anhydro forms thereof, wherein Ra is H or OH; Rb is H or halogen; Rc is H or a protecting group; Rd is methyl; unsubstituted alkyl(3-10C); substituted alkyl(1-10C); substituted or unsubstituted alkenyl(2-10C) or substituted or unsubstituted alkynyl(2-10C); substituted or unsubstituted aryl(4-14C); substituted or unsubstituted arylalkyl(5-20C); substituted or unsubstituted arylalkenyl(5-20C); substituted or unsubstituted arylalkynyl(5-20C); substituted or unsubstituted amidoarylalkyl(5-20C); substituted or unsubstituted amidoarylalkenyl(5-20C); or substituted or unsubstituted amidoarylalkynyl(5-20C); Re is H or a protecting group or is mono- or disubstituted amino carbonyl; Rf is H; substituted or unsubstituted alkyl(1-10C), substituted or unsubstituted alkenyl(1-10C); substituted or unsubstituted alkynyl(1-10C); substituted or unsubstituted aryl(4-14C); substituted or unsubstituted arylalkyl(5-20C); or -ORf may be replaced by -H; one of Z and Y is H and the other is OH or protected OH, or is amino, mono- or dialkyl-amino, protected amino, or an aminoheterocycle or Z and Y together are =O, =NOH or a derivatized oxime; including any pharmaceutically acceptable salts thereof and any stereoisomeric forms and mixtures of stereoisomeric forms thereof, are antimicrobial agents.

Inventors:
CHU DANIEL T W (US)
Application Number:
PCT/US2000/009915
Publication Date:
January 18, 2001
Filing Date:
April 14, 2000
Export Citation:
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Assignee:
KOSAN BIOSCIENCES INC (US)
CHU DANIEL T W (US)
International Classes:
A61K31/7048; A61P31/04; C07H17/00; C07H17/08; (IPC1-7): C07H17/08; A61K31/70
Domestic Patent References:
WO1999035157A11999-07-15
Foreign References:
US5141926A1992-08-25
FR2754821A11998-04-24
Other References:
J.M. WEBER ET AL.: "An erythromycin derivative produced by targeted gene disruption in Saccharopolyspora erythraea", SCIENCE, vol. 252, 1991, pages 114 - 117, XP002141603
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