Azole compound and medicinal use thereof

Details Azole compound and medicinal use thereof Azole compound and medicinal use thereof

C - Chemistry, Metallurgy

07

D

C07D 277/42 (2006.01) A61K 31/421 (2006.01) A61K 31/426 (2006.01) A61K 31/427 (2006.01) A61K 31/4439 (2006.01) A61K 31/454 (2006.01) A61K 31/496 (2006.01) A61K 31/5377 (2006.01) A61K 45/06 (2006.01) A61P 3/06 (2006.01) A61P 3/10 (2006.01) A61P 43/00 (2006.01) C07D 277/30 (2006.01) C07D 417/04 (2006.01) C07D 417/12 (2006.01)

Patent

CA 2469228

An azole compound represented by the general formula [I]: [I] [wherein W is sulfur or oxygen; R is -COOR7, -X1-A1-COOR7 (R7 is hydrogen or alkyl), or tetrazolyl; R1, R2, R3, and R4 each is hydrogen, etc; A is -(CH2)m-X- (X is - N(R8)-, -C(R9)(R10)-, -CO-, or -CO-N(R8)-); B is aryl or an aromatic heterocyclic group; R5 is hydrogen, etc.; R6 is -(Y)s1-(A2)s-Z (Y is -O-, - S(O)t-, -N(R13)-, -N(R14)-CO-, -N(R14)-SO2-, -SO2-N(R14)-, etc.); A2 is alkylene; and Z is cycloalkyl, aryl, an aromatic heterocyclic group, indanyl, or piperazinyl]; a prodrug of the compound; or a pharmaceutically acceptable salt of any of these. The compound [I] has protein tyrosine phosphatase 1B inhibitory activity and is useful as a therapeutic agent for diabetes, complications of diabetes, and hyperlipemia.

La présente invention concerne un composé azole représenté par la formule générale (I). Dans cette formule W est soufre ou oxygène, R est -COOR7, -X1 -A1-COOR7 ( R7 est hydrogène ou alkyle), ou tétrazolyle, R1, R2, R3 et R4 sont chacun hydrogène, etc., A est(CH2)m-X-(X est N(R8)-, -C(R9) (R10)-, -CO-, ou CO-N(R8)-), B est aryle ou un groupe hétérocyclique aromatique, R5 est hydrogène. Etc., R6 est (Y)s1-(A2)s-Z (Y est O-, -S(O)t-, est cycloalkyle, aryle, un groupe hétérocyclique aromatique, indanyle ou pipérazinyle. Cette invention concerne aussi un promédicament de ce composé ou un sel de n'importe quel de ces composés répondant aux normes pharmaceutiques. Ce composé (I) possède une activité inhibitrice de la protéine tyrosine phosphatase 1B et convient comme agent thérapeutique pour le diabète, les complications du diabète et l'hyperlipémie.

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