Chinoin Gyogyszer Es Vegyeszeti Termekek Gyara Rt.

Sanofi

Euroapi Hungary Limited Liability Company

Péter Buzder-Lantos

Zsuzsanna Kardos

Irén Hortobágyi

István Lászlófi

Gábor Havasi

Imre Juhász

Ágnes Nagyné Borkó

Imre Rozsumberszki

Tamás Altsach

Imre Bata

László Takács

Veronika Bartane Bodor

Zsuzsanna Tomoskozi

Gyorgy Ferenczy

Attila Vasas

Gabor Szeleczky

Sandor Batori

Marcel Patek

Martin Smrcina

Aleksandra Weichsel

Csaba Váradi

Ervin Vajda

David Squire Thorpe

István Lászlofi

Zsuzsanna Szamosvölgyi

László Fónagy

Ibolya Fekete

György Ferenczy

Veronika BARTÁNÉ Bodor

Zsuzsanna TÖMÖSKÖZI

Gábor Szeleczki

Treprostinil is a synthetic prostacyclin derivative with thrombocyte aggregation inhibitory and vasodilatory activity. Treprostinil can be administered in subcutaneous, intravenous, inhalable, or oral forms. Disclosed is a method for the preparation of treprostinil of formula I and its amorphous form, anhydrate form, monohydrate form, and polyhydrate form salts with bases. In the disclosed method, the chiral center in the 3-hydroxyoctyl substituent is formed at the end of the synthesis, so that the method is robust and well scalable. Also disclosed are treprostinil intermediates and the preparation of the intermediates.

Process for the preparation of treprostinil

Treprostinil is a synthetic prostacyclin derivative with thrombocyte aggregation inhibitory and vasodilatory activity. Treprostinil can be administered in subcutaneous, intravenous, inhalable, or oral forms. Disclosed is a method for the preparation of treprostinil of formula I and its amorphous form, anhydrate form, monohydrate form, and polyhydrate form salts with bases. In the disclosed method, the chiral center in the 3-hydroxyoctyl substituent is formed at the end of the synthesis, so that the method is robust and well scalable. Also disclosed are treprostinil intermediates and the preparation of the intermediates. 

The subject of the invention is a process for the preparation of high purity prostaglandin acid of the general formula II wherein the bonds marked with dotted lines represent single or double bonds wherein the double bonds may be cis- or trans oriented, Y represents O or CH, and Rstands for a phenyl group which is optionally substituted with CF, wherein the crude prostaglandin acid of the general formula II is purified by normal phase silicagel chromatography. 

Pocess for the preparation of high purity prostaglandins

The subject of the invention is a process for the preparation of Latanoprostene bunod of formula (I) with a purity higher than 95% where chromatography is used applying normal phase gravity silica gel column chromatography where the used silica gel is irregular silica gel or spherical silica gel an as eluent and eluent mixture consisting of an apolar and a polar solvent is used and if desired, contamination of the purified compound of formula I arising from the solvents are removed by silica gel filtration chromatography.

Preparation of latanoprostene bunod of desired, pre-defined quality by gravity chromatography

The subject of the invention is a novel process for the preparation of Carboprost tromethamine salt where alkylation the enone of the general formula (II) is carried out in the presence of a chiral auxiliary in aprotic solvent with a Grignard reagent. The methyl ester epimers of formula (VII) are separated by gravity silica gel chromatography and the salt formation is carried out by using solid tromethamine base. 

Process for the preparation of carboprost and its tromethamine salt

Treprostinil is a synthetic prostacyclin derivative with thrombocyte aggregation inhibitory and vasodilatory activity. Treprostinil can be administered in subcutaneous, intravenous, inhalable, or oral forms. Disclosed is a method for the preparation of treprostinil of formula I and its amorphous form, anydrate form, monohydrate form, and polyhydrate form salts with bases. In the disclosed method, the chiral center in the 3-hydroxyoctyl substituent is formed at the end of the synthesis, so that the method is robust and well scalable. Also disclosed are treprostinil intermediates and the preparation of the intermediates.

The present invention relates to compounds of formula 1 that are useful for the preventive and/or therapeutic treatment of diseases caused by abnormal activation of CXCR3 chemokines. The invention relates furthermore to a process for the preparation of said compounds, to pharmaceutical compositions containing said compounds and to novel intermediates used in the preparation of said compounds.

Substituted B-amino acid derivatives as CXCR3 receptor antagonists

The present invention relates to compounds of formula 1 that are useful for the preventive or therapeutic treatment of diseases caused by abnormal activation of CXCR3 chemokines. The invention relates furthermore to a process for the preparation of said compounds, to pharmaceutical compositions containing said compounds and to novel intermediates used in the preparation of said compounds.

Cycloalkane carboxylic acid derivatives as CXCR3 receptor antagonists

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Budapest, Hungary

Péter Buzder-Lantos