Modulators of protein tyrosine phosphatases (PTPASES)

A compound of Formula 1

• wherein
• A is together with the double bond in Formula 1 4,5,6,7-tetrahydro-thieno[2,3-b]pyridyl, 4,5,6,7-tetrahydro-thieno[2,3-c]pyridyl, 4,5,6,7-tetrahydro-thieno[3,2-c]pyridyl, 4,5,6,7-tetrahydro-thieno[3,2-b]pyridyl, or 4,5,6,7-tetrahydro-4,7-ethanon-thieno[2,3-b]pyridyl;
• R1 is hydrogen, COR5, OR6, CF3, nitro, SO3H, PO(OH)2, C(═NH)NH2 or selected from the following 5-membered heterocycles:
• R2 is COR5, OR6, CF3, nitro, cyano, SO3H, PO(OH)2, or C(═NH)NH2:
• R3, R16 and R17 are independently hydrogen, C1-C6alkyl, aryl, arylC1-C6alkyl, oxo, C1-C6alkyloxycarbonyl, aryloxycarbonyl, arylC1-C6alkyloxycarbonyl, arylC1-C6alkyloxy, arylC1-C6alkyloxyC1-C6alkyl, arylC1-C6alkylthio, arylC1-C6alkylthioC1-C6alkyl, arylC1-C6alkylaminoC1-C6alkyl, di(arylC1-C6alkyl)aminoC1-C6alkyl, arylC1-C6alkylcarbonyl, arylC1-C6alkylcarbonylC1-C6alkyl, arylcarboxyC1-C6alkyl, arylC1-C6alkylcarboxy, arylC1-C6alkylcarboxyC1-C6alkyl, arylC1-C6alkyl-carbonylamino, arylC1-C6alkylcarbonyl-aminoC1-C6alkyl, wherein the alkyl and aryl groups are optionally substituted;
• R4 is hydrogen, hydroxy, C1-C6alkyl, aryl, arylC1-C6alkyl, NR7R8, C1-C6alkyloxy;
• wherein the alkyl and aryl groups are optionally substituted;
• R5 is hydroxy C1-C6alkyloxy, C1-C6alkyl-oxyC1-C6alkyloxy, or arylC1-C6alkyloxy;
• wherein the alkyl and aryl groups are optionally substituted;
• R6 is hydrogen;
• R7 and R8 are independently selected from hydrogen, C1-C6alkyl, aryl, arylC1-C6alkyl, C1-C6alkylcarbonyl, arylcarbonyl, arylC1-C6alkylcarbonyl, C1-C6alkylcarboxy or arylC1-C6alkylcarboxy wherein the alkyl and aryl groups are optionally substituted;
• or R7 and R8 are together with the nitrogen to which they are attached forming a saturated, partially saturated or aromatic cyclic, bicyclic or tricyclic ring system containing from 3 to 14 carbon atoms and from 0 to 3 additional heteroatoms selected from nitrogen, oxygen or sulfur, the ring system can optionally be substituted with at least one C1-C6alkyl, aryl, arylC1-C6alkyl, hydroxy, oxo, C1-C6alkyloxy, arylC1-C6alkyloxy, C1-C6alkyloxyC1-C6alkyl, NR9R10 or C1-C6alkylaminoC1-C6alkyl, wherein R9 and R10 are independently selected from hydrogen, C1-C6alkyl, aryl, arylC1-C6alkyl, C1-C6alkylcarbonyl, arylcarbonyl, arylC1-C6alkylcarbonyl, C1-C6alkylcarboxy or arylC1-C6alkylcarboxy;
• wherein the alkyl and aryl groups are optionally substituted;
• or
• R7 and R8 are independently a saturated or partial saturated cyclic 5, 6 or 7 membered amine, imide or lactam;
• or a salt thereof with a pharmaceutically acceptable acid or base, or any optical or mixture of optical isomers, racemic mixtures, or any tautomeric forms.