Biochemie Gesellschaft M.b.h

Sandoz Ag

Ingolf Macher

Johannes Ludescher

Mahendra R Patel

Anup Kumar Ray

Mariappan Anbazhagan

Bernhard C Prager

Hiren V Patel

Christian Welz

Herwig Jennewein

Hiren Kumar V Patel

Johann Danklmaier

Gottfried Stubauer

Andreas Schmarda

Gerhard Widschwenter

The present invention relates to processes for preparing a polypeptide or pharmaceutically acceptable salt thereof comprising L-tyrosine, L-alanine, L-glutamate, and L-lysine. The polypeptide or pharmaceutically acceptable salt thereof is preferably glatiramer acetate.

Processes for preparing a polypeptide

The present invention relates to an improved process for preparing a polypeptide or pharmaceutically acceptable salt thereof comprising L-tyrosine, L-alanine, L-glutamate, and L-lysine. The polypeptide or pharmaceutically acceptable salt thereof is preferably glatiramer acetate. The process comprises: (a) polymerizing a mixture of N-carboxyanhydride of L-tyrosine, N-carboxyanhydride of L-alanine, N-carboxyanhydride of a protected L-glutamate and N-carboxyanhydride of a protected L-lysine, in a polar aprotic solvent in the presence of an initiator, to form a protected polypeptide; (b) admixing an acid with the protected polypeptide formed in Step (a) and a solvent, to form a product; and (c) admixing a substance selected from the group consisting of an alkali or alkaline earth metal hydroxide, a carbonate, a hydrogencarbonate, and mixtures thereof, with the product formed in Step (b), and a solvent or a mixture of a solvent and water, to form a deprotected polypeptide or a pharmaceutically acceptable salt thereof.

The present invention relates to pharmaceutical compositions comprising a pharmaceutically acceptable salt of caspofungin as active ingredient being useful for the prevention and/or treatment of fungal infections. The compositions additionally comprise specific bulking agents and small amounts or no amounts of an additional pH modifier and may be in a liquid or solid form, e.g. may be lyophilized compositions. The compositions show good stability and reduced amounts of sub-visible particulate matter formed in solutions which are reconstituted from the lyophilized product.

Caspofungin formulations

Production of cefotaxime and new sodium salts

Novel amidine salts of 7-Amino-3-hydroxymethyl-3-cephem-4-carboxylic acid (=HACA), particular guanidine and diaza-bicyclo-alkylene salts, are useful as intermediates in the synthesis of cephalosporins.

Intermediates in the synthesis of cephalosporins

The invention relates to a new process for the production of the disodium salt hemiheptahydrate of ceftriaxone by reacting 7-amino-3-{[(2,5-dihydro-6-hydroxy-2-methyl-5-oxo-1,2,4-triazin-3-yl)thio] methyl}-3-cephem-4-carboxylic acid with 2-(2-aminothiazol-4-yl)-2-syn-methoximinoacetic acid-(2-benzthiazolyl)thiolester in the presence of a base, characterized in that the reaction and the crystallization of the disodium salt hemiheptahydrate of ceftriaxone are carried out in aqueous acetone.

Process for the synthesis of the disodium salt hemiheptahydrate of

Pleuromutilin derivatives

Compounds of formula I ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and each represent hydrogen, alkyl, alkenyl, cycloalkyl, aryl or aralkyl are produced by a new environmentally acceptable process.

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Woergl, Austria

Ingolf Macher