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Title:
MACROLIDE ANTIINFECTIVE AGENTS
Document Type and Number:
WIPO Patent Application WO2000063224
Kind Code:
A3
Abstract:
Compounds of formula (1), (2) or (3), wherein Ra is H; substituted or unsubstituted alkyl (1-10C); substituted or unsubstituted alkenyl (2-10C); substituted or unsubstituted alkynyl (2-10C); substituted or unsubstituted aryl (4-14C); substituted or unsubstituted arylalkyl (5-20C); or ORa is replaced by H; 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 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; L is methylene or carbonyl; T is -O-, -N(R)-, -N(OR)-, -N(NHCOR)-, -N(N=CHR)-, or -N(NHR)- wherein R is H or Ra as defined above, with the proviso that when L is methylene, T is -O-; one of Z and Y is H and the other is OH, protected OH, or amino, mono- or dialkylamino, protected amino, or an amino heterocycle 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.

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Inventors:
CHU DANIEL T W (US)
ASHLEY GARY W (US)
Application Number:
PCT/US2000/009914
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)
ASHLEY GARY W (US)
International Classes:
A61K31/7048; A61P31/04; C07H17/00; C07H17/08; (IPC1-7): C07H17/08; A61K31/70
Domestic Patent References:
WO1997042206A11997-11-13
WO1999035157A11999-07-15
Foreign References:
US5141926A1992-08-25
FR2754821A11998-04-24
US5750510A1998-05-12
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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