NEW DERIVATIVE OF ERYTHROMYCIN, THEIR PRODUCTION AND THEIR USE AS MEDICAMENT

Japanese Patent JP2000143689

A

To obtain the subject new compound having greatly high antibacterial activity against Gram-positive bacteria.

This new compound is a compound of formula I (X is H or a halogen; Z is H or an acid residue), e.g. 11,12-dideoxy-3-de[(2,6-dideoxy-3-C- methyl-3-O-methyl-α-L-ribohexopyranosyl)oxy]-6-O-methyl-3- oxo-12,11-[oxycarbonyl{[4-(4-(4-aminophenyl)-1H-imidazol-1-yl) butyl]imino}]erythromycin. The compound of formula I is obtained, for example, by making a compound of formula III act on a compound of formula II (OM is an acyl residue) followed by, if desired, making a 2'-position hydroxyl- functionalizing agent and/or an acid, if appropriate, act on the resultant compound to form a salt of the aimed compound. The compound of formula I have high activity against Gram-positive bacteria such as staphylococcus and streptococcus, in particular strains resistant to erythromycin as well.

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AGOURIDAS CONSTANTIN
DENIS ALEXIS
FROMENTIN CLAUDE

JP31801599A

May 26, 2000

November 09, 1999

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HOECHST MARION ROUSSEL INC

A61K31/7042; A61K31/7048; A61K31/7056; A61P31/04; C07D233/54; C07D233/64; C07H17/08; (IPC1-7): C07H17/08; A61K31/7056; A61P31/04

JPH04290893A	1992-10-15
JPH0853489A	1996-02-27
JPH06220082A	1994-08-09
JPH09176182A	1997-07-08

WO1998009978A1	1998-03-12
WO1998040392A1	1998-09-17

Motohiro Kurauchi (1 outside)

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