Benzenesulfonamide-derivatives and their use as medicaments

Details Benzenesulfonamide-derivatives and their use as medicaments Benzenesulfonamide-derivatives and their use as medicaments

C - Chemistry, Metallurgy

07

D

C07D 295/22 (2006.01) A61K 31/18 (2006.01) C07C 311/46 (2006.01) C07C 311/51 (2006.01) C07C 311/58 (2006.01) C07C 311/60 (2006.01) C07C 317/34 (2006.01) C07C 323/49 (2006.01) C07C 323/62 (2006.01) C07D 207/48 (2006.01) C07D 209/08 (2006.01) C07D 211/46 (2006.01) C07D 211/56 (2006.01) C07D 211/96 (2006.01) C07D 213/42 (2006.01) C07D 213/76 (2006.01) C07D 239/48 (2006.01) C07D 241/22 (2006.01) C07D 243/08 (2006.01) C07D 261/16 (2006.01) C07D 277/04 (2006.01) C07D 285/06 (2006.01) C07D 295/13 (2006.01) C07D 29

Patent

CA 2323783

Compounds of formula (I), pharmaceutically acceptable salts or in vivo hydrolysable esters thereof, wherein: Ring X is phenyl or a six membered heteroaryl ring containing one or two ring nitrogens where said nitrogens are optionally oxidised to form the N-oxide; R1 and R2 are substituents as defined within; R3 and R4 are defined within and are alkyl or halo alkyl or together form a cycloalkyl or halocycloalkyl ring; R5 is a substituent as defined within; Y-Z is a linking group as defined within; are useful in the production of an elevation of PDH activity in a warm-blooded animal such as a human being. Pharmaceutical compositions, methods and processes for preparation of compounds of formula (I) are described.

L'invention concerne des composés de formule (I), des sels pharmaceutiquement acceptables ou leurs esters hydrolysables in vivo, dans laquelle le cycle X représente un phényle ou un cycle hétéroaryle à six chaînons contenant un ou deux azote(s) de cycle où lesdits azotes sont éventuellement oxydés pour former N-oxyde; R?1¿ et R?2¿ représentent des substituants tels que définis; R?3¿ et R?4¿ sont tels que définis et représentent un alkyle ou halo alkyle ou les deux formant un cycloalkyle ou un cycle halocycloalkyle; R?5¿ représente un substituant tel que défini; Y-Z représente un groupe de liaison tel que défini; ils sont utiles dans la production d'une augmentation de l'activité PDH dans un animal à sang chaud tel que l'être humain. Des compositions pharmaceutiques, des procédés et des processus de préparation des composés de formule (I) font aussi l'objet de cette invention.

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