Abstract: The invention relates to novel cyclodextrin inclusion compounds of 5,10-methylenetetrahydrofolic acid. The surprisingly good stability of these compounds makes possible their pharmaceutical use for the first time. The invention additionally relates to a process for the preparation of the said substances and their use for the preparation of medicaments.
Type:
Grant
Filed:
July 12, 1993
Date of Patent:
October 3, 1995
Assignee:
Eprova Aktiengesellschaft
Inventors:
Hans R. Muller, Martin Ulmann, Josef Conti
Abstract: Salts of 5,10-methylene-(6R)-, (6R,S)-, and (6S)-tetrahydrofolic acid with sulfuric acid or a sulfonic acid are stable in solid form and can be used as a constituent and/or as a starting material for the production of pharmaceutical compositions.
Type:
Grant
Filed:
October 15, 1992
Date of Patent:
April 5, 1994
Assignee:
Eprova Aktiengesellschaft
Inventors:
Hans R. Muller, Martin Ulmann, Josef Conti
Abstract: A method for the synthesis of serinol and serinol derivatives substituted at the nitrogen atoms by reacting a lower 1,3-dialkoxy-isopropyl halide with ammonia or an amine to form a 1,3-dialkoxy-isopropylamine and then removing the ether groups by heating with a hydrogen halide acid. The method allows the production of serinol and serinol derivatives using inexpensive starting materials in a simple manner and obtaining a high purity product which is free of interfering isomers. Novel compounds obtained by the method which are useful as pharmaceutical intermediates, X-ray contrasting agents and cytostatic or psychopharmacological drugs are also disclosed.
Type:
Grant
Filed:
November 15, 1982
Date of Patent:
March 5, 1985
Assignee:
Eprova Aktiengesellschaft
Inventors:
Ernst Felder, Sergio Bianchi, Heinrich Bollinger
Abstract: The yield of 4-methyl-5-hydroxymethyl-imidazole from the known reaction between formaldehyde and 4-methyl-imidazole can be increased greatly if the reaction is performed in a concentrated aqueous medium at pH 11-13.5, preferably 12-13.5, at a temperature of 20.degree.-60.degree. C., preferably 30.degree.-40.degree. C., with an amount of formaldehyde not exceeding 1.5 mole per mole of 4-methyl-imidazole.
Type:
Grant
Filed:
January 25, 1979
Date of Patent:
February 19, 1980
Assignee:
Eprova Aktiengesellschaft
Inventors:
Hans-Rudolf Mueller, Werner Kuendig, Alfred Hedinger