Patent ID: 6410594
Filing Date: 2002-06-25
Classification: A61P,C07C,C07D

Abstract:
A compound represented by the formula whereinX is CH2, O or S R1 is H, OH, NH2, or OR11; R9 is CO2H, SO3H, PO3H2, NO2, esters thereof, or salts thereof; each of R3 and R8 individually is H, (CH2)nCO2R10, (CH2)mOR10, CON(R10)m, (CH2)nN(R10)m, CH(R10)m, (CH2)n(R10)m, CH2CH(OR10)CH2OR10, CH(OR10)CH(OR10)CH2OR10, CH2OR10, CH(OR10)CH2NHR10, CH2CH(OR10)CH2NHR10, CH(OR10)CH(OR10)CH2NHR10, or NR10C(&boxH;NR10)N(R10)m; provided that at least one of R2, R3 and R8 is other than H; R4 is (CH2)nOH, (CH2)nNH2, (CH2)nC(&boxH;NH)NH2, (CH2)nNHC(&boxH;NR7)NH2, (CH2)nCN or (CH2)nN3; R5 is H, lower alkyl, branched chain alkyl, cyclic alkyl or CF3; R7 is H, OH, CN, NH2 or NO2; R10 is H, lower alkyl, lower alkylene, branched alkyl, cyclic alkyl, substituted cyclic alkyl, (CH2)n aromatic, (CH2)n-substituted aromatic, and when m is 2 both R10 groups can also be interconnected to form an N-heterocyclic ring; R11 is lower alkyl, branched alkyl, or (CH2)m aromatic; m is 1 or 2; n is 0-4; and further provided that when x is O or S, R3 and R8 is other than CH(OR10)CH(OR10)CH2OR10; and pharmaceutically acceptable salts thereof.