| 摘要 |
The disclosure relates to a family of guanidine derivates of general formula (I), wherein the variables are defined in the specification. The disclosure also relates to pharmaceutical compositions comprising these compounds and their use in preventing and/or treating VAP-1-related diseases, including diabetic nephropathy or diabetic macular edema. Example compounds include: 2-fluoro-3-{ 4-[(trans-4-methoxycyclohexyl)carbonyl]piperazin-1-yl} benzylcarbamimidoylcarbamate, 2-fluoro-3-[4-(tetrahydro-2H-pyran-4-ylacetyl)piperazin-1-yl]benzylcarbamimidoylcarbamate, 3-[4-(ethylsulfonyl)piperazin-1-y1]-2-fluorobenzylcarbamimidoylcarbamate, 3-{ 4-[(1-acetylpiperidin-4-yl)oxy]piperidin-1-yl} -2-fluorobenzylcarbamimidoylcarbamate, 2-fluoro-3-{ 3-[1-(methoxyacetyppiperidin-4-yl]azetidin-l-y1)benzylcarbamimidoylcarbamate, 2-fluoro-3-{ 3-[1-(3-methoxypropanoyl)piperidin-4-yl]azetidin-l-yl} benzylcarbamimidoylcarbamate, 2-fluoro-3-{ 3-[1-(methylsulfonyl)piperidin-4-yl]azetidin-1-yl} benzylcarbamimidoylcarbamate. |
