C - Chemistry – Metallurgy – 07 – H
Patent
C - Chemistry, Metallurgy
07
H
C07H 17/08 (2006.01) A61K 31/7048 (2006.01) A61P 31/04 (2006.01) A61P 33/02 (2006.01)
Patent
CA 2376748
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] -.alpha.-L- ribo-hexopryanosyl] oxy] -2-ethyl-3,4,10- trihydroxy- 3,5,8,10,12,14- hexamethyl-11- [[3,4,6- trideoxy-3- (dimethylamino) -b-D-xylo- hexopyranosyl] oxy]-1-oxa-6-azacyclopentade- can-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.
L'invention a trait à un nouveau sel diphosphate cristallin de (2<i>R</i>,3<i>S</i>,4<i>R</i>,5<i>R</i>,8<i>R</i>,10<i>R</i>,11<i>R</i>,12<i>S</i>,13<i>S</i>,14<i>R</i>)-13-[[2,6-didésoxy-3-<i>C</i>-méthyl-3-<i>O</i>-méthyl-4-<i>C</i>-[(propylamino)méthyl]-<i>a</i>-L-<i>ribo</i>-hexopryanosyl]oxy]-2-éthyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexaméthyl-11-[[3,4,6,tridésoxy-3-(diméthylamino)-<i>b</i>-D-<i>xylo</i>-hexopyranosyl]oxy]-1-oxa-6-azacyclopentadécan-15-one, qui est utile comme agent antibactérien et antiprotozoaire chez des mammifères. L'invention se rapporte également à des compositions pharmaceutiques contenant la base libre du sel diphosphate et à des méthodes de traitement d'infections bactériennes et protozoaires chez des mammifères, par l'administration de la base libre du diphosphate à des mammifères nécessitant un tel traitement. La base libre du sel diphosphate de l'invention possède une activité puissante contre diverses infections bactériennes et protozoaires lorsqu'elle est administrée par voie parentérale à des mammifères.
Allen Douglas John Meldrum
Rafka Robert John
Ragan Colman Brendan
Pfizer Products Inc.
Smart & Biggar
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