Use of compounds for the elevation of pyruvate dehydrogenase...

C - Chemistry – Metallurgy – 07 – C

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C07C 317/40 (2006.01) A61K 31/165 (2006.01) A61K 31/265 (2006.01) A61K 31/4015 (2006.01) C07D 207/27 (2006.01)

Patent

CA 2331685

The use of compounds of formula (I), and salts thereof; and pharmaceutically acceptable in vivo cleavable prodrugs of said compound of formula (I); and pharmaceutically acceptable salts of said compound or said prodrugs; in formula (I), Ring C is phenyl or a carbon linked heteroaryl ring substituted as defined within; R1 is an ortho substituent as defined within; n is I or 2; A-B is a linking group as defined within; R2 and R3 are as defined within; R4 is hydroxy, hydrogen, halo, amino or methyl; in the manufacture of a medicament for use in the elevation of PDH activity in warm-blooded animals such as humans is described. Pharmaceutical compositions, methods and processes for preparation of compounds of formula (I) are also described.

L'invention concerne l'utilisation de composés représentés par la formule (I), y compris les sels de ces composés, les promédicaments desdits composés pharmaceutiquement acceptables, clivables in vivo, représentés par la formule (I), et les sels pharmaceutiquement acceptables des mêmes composés ou promédicaments. Dans ladite formule, la chaîne C est une chaîne phényle ou hétéroaryle à liaison carbone, substituée comme indiqué dans l'invention; R<1> est un substituant ortho tel que défini dans l'invention; n vaut 1 ou 2; A-B est un groupe de liaison tel que défini dans l'invention; R<2> et R<3> sont tels que définis dans l'invention; R<4> est hydroxy, hydrogène, halo, amino ou méthyle. On utilise les produits considérés dans la fabrication d'un médicament qui permet d'élever l'activité de la pyruvate-déshydrogénase chez des animaux à sang chaud comme l'être humain. L'invention concerne en outre des compositions pharmaceutiques, des procédés et des processus pour la préparation des composés représentés par la formule (I).

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