Japanese Patent JPS6350360

B2

Fusidinic acid derivs. of formula (I) and their pharmaceutically acceptable salts and easily hydrolysable esters are new: (C24 and C25 are joined by a single or double bond, Q1 and Q2 are H HO or O. A=O, S or SO. R1 = opt. branched 1-8C alkyl, 2-6C alkenyl or alkynyl, 3-7C cycloalkyl, aryl, aralkyl, heterocyclyl-alkyl or 5-6 membered heterocycle contg. O.S or N atoms; and all these gps. may be substd.). Prepn. is by reacting the 16 alpha-halo analogue, in which the 21-COOH is esterified, with R1AH then hydrolysing. (I) are useful for treating bacterial infections in humans and animals. They are more stable than fusidinic acid itself and are practically non-toxic. They may be administered in usual oral, parenteral or topical forms for an adult dose of 0.25-5, pref. 0.5-3g/day. A specifically claimed cpd., 16-desacetoxy-16 beta-isopropylthiofusidinic acid, was prepd. from 3-O-acetyl-16-desacetoxy-16 alpha-bromofusidinic acid p-nitrobenzyl ester, by reaction with isopropyl mercaptan, then hydrolysis with NaOH.

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BERUFU FUON DEENE
HOORU RODOBUROE RASUMUUSEN

JP7393176A

October 07, 1988

June 24, 1976

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LEO PHARM PROD AS

C07J9/00; A61K31/56; A61K31/575; A61P31/04; C07J13/00; C07J31/00; C07J41/00; C07J43/00

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