| 摘要 |
New use of indirubin derivatives (I) as: (1) VEGF-R inhibiting medicaments for treating cancer, autoimmune diseases, chemotherapy-induced alopecia and mucositis, cardiovascular diseases, infectious diseases, fungal diseases, nephrological diseases, acute or chronic neurodegenerative diseases or viral infections; or (2) VEGF-R kinase-3 inhibiting medicaments for treating lymphangiogenesis. New use of indirubin derivatives of formula (I), or their optical isomers or salts, for the production of: (a) VEGF-R inhibiting medicaments for treating cancer, autoimmune diseases, chemotherapy-induced alopecia and mucositis, cardiovascular diseases, infectious diseases, fungal diseases, nephrological diseases, acute or chronic neurodegenerative diseases or viral infections; or (b) VEGF-R kinase-3 inhibiting medicaments for treating lymphangiogenesis; D = C=N-OR9, C(CH3)-OH or C=O; R1 - R8 = H, halo, OH, NO or NO2; 1-10C alkyl or 1-10C alkoxy (both optionally interrupted by one or more O); 1-18C alkyl (optionally substituted (os) by one or more of halo, OH and/or NH2); aryl or heteroaryl (both os by one or more of halo, T, OH, NH2 and/or OT); aralkyl, aryloxy, methylenearyloxy, cycloalkyl, cycloalkenyl or 3-7C methylenecycloalkyl (all os by one or more of halo, T, OH, NH2 and/or OT; and optionally containing heteroatom(s)); hydroxylamino, phosphate, phosphonate, sulfate, sulfonate or sulfonamide (all os by one or more of halo, T, OH, NH2 and/or OT); COR14, COOR14, CH2COOR14, CONR10R11, NR10R11, SO2NR10R11, -N=N-R13 or S(O)nR12; or O- or N-glycoside derived from a mono- or disaccharide; or adjacent groups R1 - R8 may together complete a ring containing 1-4C, os by one or more groups (other than H) as defined for R1 - R8 as individual substituents; T = 1-6C alkyl; R9 = H; 1-18C alkyl, cycloalkyl or cycloalkenyl (all optionally interrupted by one or more O and os by OH); aryl, heteroaryl or cycloalkyl (all optionally interrupted by one or more O and os by one or more of OH, halo and/or NH2); or -(CH2)m-COR15 or -(CH2)m-OR12; R10, R11 = H; 1-18C alkyl aryl, heteroaryl or acyl (all os by OH and/or NR16R17); or 1-18C alkyl, cycloalkyl or cycloalkenyl (all optionally interrupted by one or more O); NR10R11 = 3-8C cycloalkyl (sic), optionally containing one or more heteroatoms and os by one or more of 1-18C alkyl (os by one or more of halo, OH and/or NH2) or aryl, heteroaryl or cycloalkyl (all os by one or more of halo, OH, NH2, T and/or OT); R12 = H, NR10R11, 1-18C alkyl (os by one or more of halo, OH and/or NH2) or aryl, heteroaryl or cycloalkyl (all os by one or more of halo, OH, NH2, T and/or OT); R13 = aryl (os by one or more COOH, phosphoryl or sulfonate groups); R14 = H, 1-18C alkyl (os by one or more OH and/or NH2) or aryl, heteroaryl or cycloalkyl (all os by one or more of halo, T and/or OT); R15 = 1-10C alkyl, 1-10C alkoxy or NR10R11; R16, R17 = as R10, R11; or NR16R17 = ring as defined for NR10R11; n = 0-10; m = 0-10; Unless specified otherwise cycloalkyl or cycloalkenyl moieties have 3-8C.
|
