| 摘要 |
The present invention relates to a novel tricyclic derivative with efficient inhibitory activity against poly(ADP-ribose)polymerases (PARP) or pharmaceutically acceptable salts thereof, a preparation method thereof, and a pharmaceutical composition containing the same. The tricyclic derivative of the invention is useful for the prevention or treatment of diseases caused by excess PARP activity, especially neuropathic pain, neurodegenerative diseases, cardiovascular diseases, diabetic nephropathy, inflammatory diseases, osteoporosis, and cancer, by inhibiting the activity of poly(ADP-ribose)polymerases. |
| 主权项 |
1. A tricyclic compound represented by chemical formula 1 or pharmaceutically acceptable salts thereof: wherein Y1 and Y2 are independently H, methyl, ethyl, methoxy, ethoxy, hydroxy, COOR1, —NR2R3 or -A-B; Y3 is H, hydroxy, methoxy, ethoxy, propoxy, or methoxyethoxy, provided that at least one of Y1 and Y2 is methoxy, ethoxy, hydroxy, —COOR1, —NR2R3 or -A-B;
whereinA is —O—, —CH2—, —CH(CH3)—, —CH═N— or —CONH—;B is —(CH2)n1-Z, —(CH2)n2-NR2R3 or —(CH2)n3-OR1;Z is one base selected from the group consisting of the below structural formulae; wherein R1 is H, methyl, ethyl or isopropyl; R2 and R3 are independently H, methyl, ethyl, propyl, isopropyl, t-butyl or —(CH2)n4R7; R5 is H, compound, methyl, ethyl, propyl, phenyl or morpholino; R6 is H, methyl or ethyl; R7 is —NR8R9, —COOR1, —OR1, —CF3, —CN, F, Cl or Z; R8 and R9 are independently H or methyl; n1 to n4 are respectively integers between 0 and 5; and Y4 is H, methyl, ethyl or propyl. |
