Derivatives of benzothiazines, preparation thereof and...

Details Derivatives of benzothiazines, preparation thereof and... Derivatives of benzothiazines, preparation thereof and...

C - Chemistry, Metallurgy

07

D

C07D 275/06 (2006.01) A61K 31/5415 (2006.01)

Patent

CA 2753630

The object of the present invention is benzothiazine derivatives having the capability of inhibiting 11.beta.-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 R1 represents a hydrogen or OR1 represents an ester or an ether. R2 represents a naphthyl or a 1, 2, 3, 4-tetrahydro-naphthalene or a biphenyl or phenyl pyridine or a substituted phenyl. R3 represents a methyl or ethyl; R4 and R'4 represent a hydrogen.

Cette invention concerne des dérivés des benzothiazines capables d'inhiber l'enzyme 11ß-HSD1 non seulement au niveau enzymatique mais aussi au niveau cellulaire. Les composés de l'invention sont de formule générale (I), R1 représentant hydrogène ou OR1 représentant un ester ou un éther, R2 représentant un groupe naphtyle ou un groupe 1,2,3,4-tétrahydronaphtalène ou un diphényle ou un groupe phénylpyridine ou un groupe phényle substitué, R3 représentant un groupe méthyle ou éthyle, R4 et R'4 représentant hydrogène.

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