Pierre Fabre Medicament

Yves Rival

Didier Junquero

Elisabeth Dupont-Passelaigue

Isabelle Leroy

Michel Perez

Marie Lamothe

Karine Valeille

André Delhon

Jean-François Patoiseau

Elisabeth Dupont-passelaigue

The object of the present invention is benzothiazine derivatives having the capability of inhibiting 11&#x3b2;-HSD1 not only at an enzymatic level but also at a cell level. The compounds of the present invention are of general formula (I). Wherein notably Rrepresents a hydrogen or OR1 represents an ester or an ether. Rrepresents a naphthyl or a 1,2,3,4-tetrahydro-naphthalene or a biphenyl or phenyl pyridine or a substituted phenyl. Rrepresents a methyl or ethyl; Rand R'represent a hydrogen. 

Derivatives of benzothiazines, preparation thereof and application thereof as drugs

The present invention relates to derivatives of general formula I wherein: &#x2014;W represents nitrogen, &#x2014;Rrepresents: &#x2022;a hydrogen or a linear or branched C-Calkyl radical or, &#x2022;a C-Calkyl radical substituted with groups such as trifluoromethyl, nitrile, hydroxy, C-Calcoxy, C-Calkoxyalkoxy, indolyl, thiophenyl, oxothiophenyl, C-CN-alkylcarbamoyl groups or, &#x2022;a phenyl or pyridyl or naphthyl, or thiophenyl group optionally substituted with one or more groups such as halogen atoms, nitro, nitrile, trifluoromethyl, vinyl, methylsulfanyl, linear branched C-Calkyl, linear or branched C-Calkoxy groups, &#x2022;a C2-oxocycloalkyl radical&#x2014;Rrepresents a methyl or heptyl, -m, n are equal to 1, &#x2014;V represents CH, &#x2014;X&#x2014;Y represents &#x2014;N&#x2014; (C&#x2550;O)&#x2014;, &#x2014;CH&#x2014;O&#x2014;, &#x2014;Z represents a phenyl group substituted with one or more trifluoromethyl groups, halogen atoms or linear C-Calkyl groups. 

Derivatives of triazines and uracils, their preparation and their application in human therapeutics

The invention relates to 3,5-dioxo-(2H,4H)-1,2,4-triazine compounds of formula I in which the variables are defined herein, as well as additive salts with pharmaceutically acceptable bases and the various enantiomers of compounds having asymmetrical carbons, as well as their mixtures in all proportions, including racemic mixtures in particular.

1,2,4-triazine derivatives, preparation and use thereof in human therapy

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Lagarrigue, France

Yves Rival