Pfizer Corporation

Pfizer Products Inc.

Colman B Ragan

Robert J Rafka

Douglas J M Allen

Barry J Morton

Peter Bertinato

John P Dirlam

Alan Elwood Blize

Carl Bernard Ziegler

This invention relates to a novel crystalline diphosphate salt of (2R,3S,4R,5R,8R,10R,11R,12S,13S,14R)-13-[[2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(propylamino)methyl]-&#x3b1;-L-ribo-hexopryanosyl]oxy]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-11-[[3,4,6-trideoxy-3-(dimethylamino)-&#x3b2;-D-xylo-hexopyranosyl]oxy]-1-oxa-6-azacyclopentadecan-15-one that is useful as an antibacterial and antiprotozoal agent in mammals. This invention also relates to pharmaceutical compositions containing the free base of the diphosphate salt and the methods of treating bacterial and protozoal infections in mammals by administering the free base of the diphosphate to mammals requiring such treatment. The free base of the diphosphate salt of the present invention possesses potent activity against various bacterial and protozoal infections when given by parenteral application to mammals.

Diphosphate salt of a 4&#x2033;&#x2014;substituted-9-deoxo-9 A&#x2014;AZA&#x2014;homoerythromycin derivatives and its pharmaceutical composition

This invention relates to a novel crystalline diphosphate salt of (2R,3S,4R,5R,8R,10R,11R,12S,13S,14R)-13-[[2,6-dideoxy-3-C-methyl-3-o-methyl-4-C-[(propylamino)methyl]-&#x3b1;-L-ribo-hexopryanosyl]oxy]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-11-[[3,4,6-trideoxy-3-(dimethylamino)-&#x3b2;-D-xylo-hexopyranosyl]oxy]-1-oxa-6-azacyclopentadecan-15-one that is useful as an antibacterial and antiprotozoal agent in mammals. This invention also relates to pharmaceutical compositions containing the free base of the diphosphate salt and the methods of treating bacterial and protozoal infections in mammals by administering the free base of the diphosphate to mammals requiring such treatment. The free base of the diphosphate salt of the present invention possesses potent activity against various bacterial and protozoal infections when given by parenteral application to mammals.

Diphosphate salt of A 4&#x2033;-substituted-9-deoxo-9A-AZA-9A-homoerythromycin derivative and its pharmaceutical composition

Crystalline forms of macrolide antibiotic

This invention relates to a novel crystalline diphosphate salt of (2R,3S,4R,5R,8R,10R,11R,12S,13S,14R)-13-&lsqb;&lsqb;2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-&lsqb;(propylamino)methyl&rsqb;-&agr;-L-ribo-hexopryanosyl&rsqb;oxy&rsqb;-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-11-&lsqb;&lsqb;3,4,6-trideoxy-3-(dimethylamino)-&bgr;-D-xylo-hexopyranosyl&rsqb;oxy&rsqb;-1-oxa-6-azacyclopentadecan-15-one that is useful as an antibacterial and antiprotozoal agent in mammals. This invention also relates to pharmaceutical compositions containing the free base of the diphosphate salt and the methods of treating bacterial and protozoal infections in mammals by administering the free base of the diphosphate to mammals requiring such treatment. The free base of the diphosphate salt of the present invention possesses potent activity against various bacterial and protozoal infections when given by parenteral application to mammals.

Diphosphate salt of a 4&Prime;-substituted-9-deoxo-9A-AZA-9A- homoerythromycin derivative and its pharmaceutical composition

The invention relates to a method of preparing compounds of the formula 1

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Mystic, CT, United States of America

Colman B Ragan