Patent ID: 7265136

Claim:
A compound of formula AXB useful in inducing necrosis in vascular tissue of a tumor in a mammal, said compound containing (a) a first moiety, A, which is a cis-stilbene moiety of formula II wherein R1, R2 and R3 are each independently H, optionally substituted alkoxy, optionally substituted alkyl or halogen R4 is hydrogen or cyano R5, R6 and R7 are each independently H, hydroxy, optionally substituted alkyl, halogen, amino, alkylamino, dialkylamino, cyano, nitro, carboxyl, alkanoyl, alkoxycarbonyl, alkoxycarbonylamino, aminocarbonylamino, alkylaminocarbonylamino, di alkylaminocarbonylamino, alkylcarbonylamino, alkylsulphonyl, aminosulphonyl, alkylaminosulphonyl, dialkylaminosulphonyl, alkylsulphonylamino, aminosulphonylamino, alkylaminosulphonylaminio, dialkylaminosulphonylamino, mercapto, alkylsulphanyl, or alkylsulphinyl, with the proviso that at least two of R1, R2 and R3 must be optionally substituted alkoxy, and (b) a second moiety, B, which is an inhibitor of nitric oxide synthase said first and second moieties being coupled in the compound by X which is a linker bond or moiety bound to any available valency of B and any available valency of that phenyl ring of Formula II that is substituted by R5, R6 and R7 such that the compound has an increased activity in inducing necrosis in said vascular tissue as compared with a compound containing said first moiety without the second moiety, wherein X is selected from the group consisting of an optionally substituted methylene chain and —(CH2) m —Y—(CH2) n wherein Y is selected from —O—, —S—, —SO 2 , NH—, N alkyl, —CO—, —OC(O)—, —NHC(O), —N(alkyl)C(O)—, NNHC( ))NH—, NalkylC(O)NH-NalkylC(O)Nalkyl, NHSO 2 , NalkylSO 2 —, NHSO 2 NH, NalkylSO 2 NH, NalkylSO 2 Nalkyl and —OC(O)O, m is 0-3 and n is 0-3 or a hydrate or pharmaceutically acceptable salt of the compound.