4439434 Cephalosporin derivative and pharmaceutical composition containing the derivative

New Patents

4438143

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1-ARYLOXY-3-ALKYLAMINO-2PROPANOLS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM Herbert Koppe, Werner Kummer, Helmut Stahle, Gojko Muacevic, Werner Traunecker, Ingelheim, Federal Republic Of Germany assigned to Boehringer Ingelheim KG CN

OH R1--CO--NH

ix

R2

This invention relates to compounds of the formula See Patent for Chemical Structure (I) wherein R1 represents a linear or branched alkyl of from 1 to 20 carbon atoms; R2 represents a hydrogen or halogen atom, a linear or branched alkyl or alkoxy of from 1 to 4 carbon atoms, or a divalent group -CH double bondCH-CH double bondCH- or -(CH2)n-, in which n is an integer of from 3 to 5, with the free valences bonded in the o-position relative to one another; and R3 represents a linear or branched alkyl of from 3 to 10 carbon atoms, with the provisos that R3 is not tert.butyl when R1 is ethyl or propyl and R2 is a hydrogen atom and that R3 is not isopropyl when R1 is propyl and R2 is a hydrogen atom, or a non-toxic, pharmacologically acceptable acid addition salt thereof. The compounds of Formula I are useful for treatment and prophylaxis of diseases of the coronaries, for the treatment of hypertension, and for treatment of cardiac arrhythmia, particularly tachycardia.

4439426 SEMISYNTHETIC MACROLIDIC ANTIBIOTICS, INTERMEDIATE C O M P O U N D S FOR THEIR PREPARATION AND RELATED PHARMACEUTICAL COMPOSITIONS CONTAINING THEM Luciano Toscano, Leonardo M Cappelletti, Milan, NY, Italy assigned to Pierrel S p A From the fermentation carried, out with mutants blocked in the synthesis respectively of erythromycin and of oleandomycin, namely

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. k'~J~"'OH CH3/ "OCH 3

Streptomyces erythreus ATCC 31772 and Streptomyces antibioticus ATCC 31771, using as the substrate a derivative of erythronolide A, namely (8S)-8-fluoroerythronolide A, a derivative of erythronolide B, namely (8S)-8fluoroerythronolide B, or a derivative of 3-0mycarosyl-erythronolide B, namely 3-0mycarosyl-(8S)-fluoroerythronolide B, the corresponding (8S)-8-fluoro derivatives of the erythromycins A, B, C and D, as well as 3-0oleandrosyl-5-desosaminyl-(8S)-8fluoroerythronolide A and 3-O-oleandrosyl-5O-desosaminyl-(8S)-8-fluoroerythronolide B, all belonging to the class of the macrolide antibiotics are obtained. The preparation of the aforesaid substrate comprises the convention of erythronolide A, erythronolide B or 3-0mycarosyl-erythronolide B into the corresponding hermiacetal, the reaction of the latter with a compound capable of generating electrophlic fluorine and the opening of the resulting acetal with aqueous acid.

4439434 CEPHALOSPORIN DERIVATIVE AND PHARMACEUTICAL COMPOSITION CONTAINING THE DERIVATIVE Shigeak Muto, Kouichi Niimura, Takao Ando, Masahiko Fujii, Takao Furusho, Chikao Yoshikumi, Tokyo, Japan assigned to Kureha Kagaku Kogyo Kabushiki Kaisha A compound having the general formula (I) is derived from a cephalosporin; See Patent for Chemical Structure (I) See Patent for Tabular Presentation CH2COOR', See Patent for Tabular Presentation wherein R' is a hydrogen atom, an alkyl group having 1 to 4 carbon atoms or an alkali metal. A pharmaceutical composition containing the compound is excellent in an antibacterial activity, the activity being recovered by the action of an activating enzyme