Novo Industri A/s

Novo Nordisk A/s

Henning Borge Petersen

Poul Borrevang

Erling Guddal

Jorgen Ilum Nielsen

Peter Faarup

Jesper F Lau

Knud Erik Andersen

Hans Petersen

Behrend Friedrich Lundt

Peter Kresten Nielsen

Subhash R Patel

Per O So Slashedrensen

Michael Cain

Michael H Chain

Vincent H Chang

The present invention relates to therapeutically active azaheterocyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating a central nervous system ailment related to the GABA uptake.

1-substituted, 3-carboxylic acid piperidine derivatives

The invention provides crystalline Tiagabine hydrochloride monohydrate, process for its preparation, compositions containing the same and its therapeutic use as anti-epileptic agent.

Crystalline Tiagabine monohydrate, its preparation and use

An improvement in the conversion of penam and cephem compounds to secondary ammonium salts of phosphite amides thereof by reacting as follows: ##STR1## wherein --R, is the non-reacting balance of the penam or cephem compound and ##STR2## ARE NON-REACTING SUBSTITUENTS. Catalytic amounts of H--N&lt; or the hydrogenhalide thereof may be present in the reaction medium.

Process for the preparation of phosphorus derivatives of secondary

Conversion of penicillin sulfoxides to the corresponding 3-desacetoxycelphalosporins are carried out in high yield by heating, e.g. 80.degree.-130.degree. C, a solvent solution of the penicillin in the presence of a complex formed by a phosphite or phosphine amide with the salt of a strong acid and a nitrogenous base, e.g. alpha-picoline hydrobromide. One preferred amide is 2-piperidino-1,3,2-dioxaphospolane.

Process for converting penicillin sulfoxides to the corresponding

Novel penicillin and cephalosporin intermediates for the synthesis of 6-APA or 7-aminocephem compounds involving formation of a 6 or 7 phosphite amido compound and the conversion of such compound to a desired 6-APA or 7-aminocephem compound.

Penicillin and cephalosporin intermediates

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Lyngby, Denmark

Henning Borge Petersen