| 摘要 |
An inhibitor of the b-isozyme of protein kinase C is used in the manufacture of a medicament for treating neoplasia, rheumatoid arthritis or keloid or for inhibiting VEGF stimulated capillary permeability associated with pulmonary edema. The preferred inhibitor is a bis-indolylmaleimide or a macrocyclic bis-indolylmaleimide. The bis-indolylmaleimide can have the formula I wherein W is O, S(O)q, CO, optionally substituted alkylene, alkenylene, aryl, aryl-(CH2)m-O-, fused bicyclic, fused bicyclic-(CH2)m-O-, heterocycle, heterocycle-(CH2)m-O-, NR3, NOR3, CONH or NHCO; X and Y are independently optionally substituted alkylene or together X, Y and W combine to form -(CH2)n-AA-; each R1 is H or up to four of halo, alkyl, hydroxy, alkoxy, haloalkyl, nitro, NR4R5 or NHCO-alkyl; R2 is H, CH3CO, NH2 or OH; n is 2 to 5; q is 0 to 2 and m is 0 to 3; AA is an amino residue and R3, R4 and R5 are as defined in the specification. |
