Cerbios-pharma Sa

Sapec S.a. Fine Chemicals

Sapec S.a.

Fabrizio Marazza

Francis M Sirotnak

Jean Jacques

Jean-Claude Jaton

Ari Lewenstein

Pascal Jequier

Attilio Melera

Mathias Jud

Christof Schickli

Rene Viterbo

Nando Toderi

Ulrich Burger

Peter Buchs

Bernhard Jaun

Giovanni Mazzei

Paolo Crivelli

Raffaela Manzotti

Antonio Tognini

Raffaela Coppolecchia

Achille Arini

The inventive process for the reduction of pterins by means of an alkali metal boron hydride in water to the corresponding 5,6,7,8-tetrahydropterins is characterized in that the reduction is carried out in the presence of a catalytical amount of a water-soluble Pb(II)-salt.

Process for the reduction of pterins

Pharmaceutical compositions for the modulation of the immune reaction of warm blooded animals that are derivatives of the 2-oxindole-3-acetic acid or the 2-oxo-1,2,3,4-tetrahydroquinoline-4-carboxylic acid are described, and whereby the derivatives can optionally be in an equilibrium with each other. The derivatives included in the pharmaceutical compositions comprise those compounds which are already described in the literature and also new compounds. Furthermore, new derivatives of the the 2-oxindole-3-acetic acid and the 2-oxo-1,2,3,4-tetrahydroquinoline-4-carboxylic acid are described, particularly also the the pure antipodes of the mixture of enantiomeres of the 2-oxo-1,2,3,4-tetrahydroquinoline-4-carboxylic acid.

Pharmaceutical composition and method for modulating the immune reaction

A concentrated, stable solution, especially an injection solution, which comprises water and either sodium-leucovorin or potassium-leucovorin or sodium-N(5)-methyl-5,6,7,8-tetrahydrofolic acid or potassium-N(5)-methyl-5,6,7,8-tetrahydrofolic acid. Also described is a process for the preparation of the solution, as well as its uses.

Concentrated injection solution of alkali metal salts of reduced folates

What are described are new glucosides and their sugar-free decomposition products, as well as synthetically produced derivatives, which can be used as active components of pharmaceutical compositions. The novel glucosides have been isolated from aqueous extracts of vegetable pollen. These novel glucosides, sugar-free decomposition products and their derivatives have the effectiveness to modulate the immune system of warm blooded animals and they can be used as active components in pharmaceutical compositions for the treatment of tumors and virus-related diseases.

Glycosides isolated from pollen, their sugar-free decomposition products

The invention recites a process for preparing 9,10-secocholesta-5,7,10(19)-trienes of formula (I) ##STR1## where R.sup.1 is hydrogen or a hydroxy-protecting group and R.sup.2 and R.sup.3 are independently hydrogen or OR.sup.1. The compounds are prepared from epoxides of the following formulas ##STR2## by reaction with a low-valent metal reagent formed by reducing a metal halide, M(z)X.sub.z, preferably WCl.sub.6.

Process for the preparation of 9, 10-secocholesta-5,7,10 (19)-trienes

(6S)-THF is obtained by adding, in portions, an acid to an aqueous solution of a (6RS)-diastereoisomeric mixture of an alkali metal salt of 5,6,7,8-tetrahydrofolic acid. The addition is made at a temperature from 5.degree. C. to 80.degree. C. for the purpose of the selective crystallization for a period sufficient to stabilize the pH to a value of from 4.8 to 5.3. Then, the formed solid, i.e., (6S)-5,6,7,8-tetrahydrofolic acid, is separated.

Process for the preparation of (6S)-5,6,7,8-tetrahydrofolic acid

A process for the preparation of salts of (6R)-N(5),N(10)-methenyl-5,6,7,8-tetrahydrofolic acid of a particular formula (I). The process comprises:

Process for the preparation of diastereoisomeric pure tetrahydrofolates

There are described ammonium salts of N.sup.5 -methyl-5,6,7,8-tetrahydrofolic acid as well as processes for their preparation. These ammonium salts may be separated into the single (6R) and (6S)-diastereoisomers. The separated diastereoisomers may be transformed into the corresponding alkali metal or alkaline earth metal salts.

(6R)- and (6S)-diastereoisomers of an ammonium salts of N.sup.5

A process for the preparation of alkaline earth metal salts of (6R)-N(10)-formyl-5,6,7,8-tetrahydrofolic acid. An alkaline earth metal salt, either in the form of a solid, or in the form of an aqueous solution, is added, preferably under an inert gas atmosphere, to an ammonium salt or alkali metal salt of (6RS)-N(10)-formyl-5,6,7,8-tetrahydrofolic acid dissolved in water or an aqueous buffer solution. II is added an alkaline earth metal salt either in the form of a solid or in the form of an aqueous solution. The obtained mixture is allowed to crystallize, and the obtained solid is separated. The product is known to be cytostatic.

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Novaggio, Switzerland

Fabrizio Marazza