Pfizer Corporation

Wei-Guo Su

Takushi Kaneko

Yong-Jin Wu

Bingwei Vera Yang

Hiroko Masamune

Yan Chen

William Thomas McMillen

Katherine E Brighty

Paul R McGuirk

Hamish A McArthur

Robert G Linde, Ii

Kathleen T Smyth

Daniel J Durkin

Hongjuan Zhao

A macrolide antibiotic of the formulawherein the variables are defined as described herein.

Macrolide antibiotics

13-methyl erythromycin derivatives

Carbamate and carbazate ketolide antibiotics

Ketolide antibiotics

This invention relates to compounds of the formula

C-4 substituted macrolide antibiotics

The invention relates to the compounds of the formula 1

Erythromycin derivatives

The invention relates to crystalline 9-E-(O-methyl)oxime of 11,12-dideoxy-3-de(2,6-dideoxy-3-C-methyl-3-O-methyl-&agr;-L-ribohexopyranosyloxy)-6-O-methyl-12,11-(iminocarbonyl-(2-(3-(4-(3-pyridinyl)-1H-imidazol-1-yl)propyl)hydrazono))-3-oxoerythromycin wherein said crystalline compound is as the free base of said compound, the hemihydrate of said compound or the mesylate (methanesufonic acid) salt of said compound. The invention also relates to pharmaceutical compositions containing the foregoing crystalline compound and to methods of treating bacterial and protozoa infections by administering said crystalline compound.

Crystalline 9-E-(O-methyl)oxime of 11, 12-dideoxy-3-de(2,6-dideoxy-3-C-methyl-3-O-methyl-&agr;-L-ribohexopyranosyloxy)-6-O-methyl-12,11-(iminocarbonyl-(2-(3-(4-(3-pyridinyl)1H-imadazol-1-yl)propyl)hydrazono))-3-oxoerythromycin

This invention relates to compounds of the formula ##STR1## and to pharmaceutically acceptable salts thereof. The compounds of formula 1 are potent antibacterial and antiprotozoal agents that may be used to treat various bacterial and protozoal infections and disorders related to such infections. The invention also relates to pharmaceutical compositions containing the compounds of formula 1 and to methods of treating bacterial and protozoal infections by administering the compounds of formula 1.

C-4' substituted macrolide antibiotics

Growing community of inventors

East Lyme, CT, United States of America

Wei-Guo Su