Salts of N-glycosyl derivatives of polyene macrolides, especially N-methylglucamine salts as well as the method of their preparation

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United States of America Patent

PATENT NO 4195172
SERIAL NO

05905178

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Abstract

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The new compounds, N-methylglucamine salts of N-glycosyl derivatives of polyene macrolides particularly N-methylglucamine salts of N-glycosyl derivatives of amphotericin B, polifungin and nystatin are described herein. These compounds exhibit high pharamacological activity in some topical and sistemic fungal infections. The product is prepared by reaction of an amino group containing polyene macrolide with an aldose or ketose mono- or oligosaccharide, in an organic solvent medium or in the mixture of solvents characterized in that the formed N-glycosyl derivatives is precipitated from the reaction medium by water or with an aqueous solution of inorganic salt, preferably ammonium sulphate, and after crystallization from a higher alkanol of C.sub.3-6 atoms, preferably n-butanol transformed into a salt, preferably an N-methylglucamine salt and then crystallized from higher alkanol, preferably n-butanol.

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Patent Owner(s)

  • POLITECHNIKA GDANSKA;INSTYTUT PRZEMYSLU FARMACEUTYCZNEGO

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Borowski, Edward Gdansk, PL 14 37
Bylec, Elzbieta Gdansk, PL 1 7
Dahlig, Halina Warsaw, PL 1 7
Falkowski, Leonard Gdansk, PL 2 10
Golik, Jerzy Sopot, PL 14 130
Jakobs, Ewa Sopot, PL 1 7
Kolodziejczyk, Pawel Gdansk, PL 2 10
Kowszyk-Gindifer, Zuzanna Warsaw, PL 1 7
Pawlak, Jan Sopot, PL 2 68
Plociennik, Zofia Warsaw, PL 1 7
Roslik-Kaminska, Danuta Warsaw, PL 1 7
Wagner, Wladyslawa Warsaw, PL 1 7
Zielinski, Jan Gdansk, PL 19 209

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