Process for preparing...

C - Chemistry – Metallurgy – 07 – F

Patent

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C07F 9/6558 (2006.01) A61K 31/675 (2006.01)

Patent

CA 2586114

The present invention is concerned with a process for the preparation of the compound {3-[2(R)-[(1R)-1-[3,5-bis(trifluoromethyl) phenyl]ethoxy]-3(S)-(4- fluorophenyl)-morpholin-4-yl]methyl]-5-oxo-4,5-dihydro-[1,2,4]-triazol-1- yl}phosphonic acid, and pharmaceutically acceptable salts thereof. This compound is useful as a substance P (neurokinin-1) receptor antagonist. In particular, the compound is useful e.g., in the treatment of emesis and inflammatory diseases.

Procédé de production du composé acide {3-[2(R)-[(1R)-1-[3,5-bis(trifluorométhyl)phényl]éthoxy]-3(S)-(4-fluorophényl)morpholin-4-yl]méthyl]-5-oxo-4,5-dihydro-[1,2,4]-triazol-1-yl}phosphonique et de sels acceptables sur le plan pharmaceutique dudit composé. Ce composé est utile en tant qu'antagoniste du récepteur de la substance P (neurokinine-1), en particulier, par ex., pour traiter les vomissements et les maladies inflammatoires.

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