Antitumoral compounds

Organic compounds -- part of the class 532-570 series – Organic compounds – Amino nitrogen containing

Reexamination Certificate

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C549S239000, C514S376000, C514S459000

Reexamination Certificate

active

07138547

ABSTRACT:
New spisulosine derivatives of use in treating tumors are of the formula (I) wherein: each X is the same or different, and represents H, OH, OR′, SH, SR′, SOR′, SO2R′, NO2, NH2, NHR′, N(R′)2, CN, halogen, C(═O)H, C(═O)CH3, CO2H, CO2CH3, substituted or unsubstituted C1–C18alkyl, substituted or unsubstituted C2–C18alkenyl, substituted or unsubstituted C2–C18alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaromatic, or two groups X may together form ═O; Y is NR1, OR1, PR1, SR1, or halogen, wherein the number of substituents R1is selected to suit the valency and each R1is independently selected of H, OH, C(═O)R′, P(═O)R′R″, substituted or unsubstituted C1–C18alkyl, substituted or unsubstituted C2–C18alkenyl, substituted or unsubstituted C2–C18alkynyl, substituted or unsubstituted aryl, and wherein the dotted line indicates an optional double bond; each Z is the same different, and represents H, OH, OR′, SH, SR′, SOR′, SO2R′, NO2, NH2, NHR′, N(R′)2, NHC(O)R′, CN, halogen, C(═O)H, C(═O)CH3, CO2H, CO2CH3, substituted or unsubstituted C1–C18alkyl, substituted or unsubstituted C2–C18alkenyl, substituted or unsubstituted C2–C18alkenyl, substituted or unsubstituted C2–C18alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaromatic, or two groups Z may together form ═O; z is 0 to 25; y is to 0 to 20; R2is H, C(═O)R′, P(═O)R′R″, S(═O)R′R″, S(═O)2R′, substituted or unsubstituted C1–C18alkyl, substituted or unsubstituted C2–C18Alkenyl, substituted or unsubstituted C2–C18alkynyl, substituted or unsubstituted aryl; R3is H, C(═O)R′, P(═O)R′R″, S(═O)R′R″, S(═O)2R′, substituted or unsubstituted C1–C18alkyl, substituted or unsubstituted C2–C18alkenyl, substituted or unsubstituted C2–C18alkynyl, substituted or unsubstituted aryl; each of the R′, R″ groups is independently selected from the group consisting of H, OH, NO2, NH2, SH, CN, halogen, ═O, C(═O)H, C(═O)CH3, CO2H, CO2CH3, substituted or unsubstituted C1–C18alkyl, substituted or unsubstituted C1–C18alkoxy, substituted or unsubstituted C2–C18alkenyl, substituted or unsubstituted C2–C18alkynl, substituted or unsubstituted aryl; there may be one or more unsaturations in the hydrocarbon backbone defined by the chain (II) and salts thereof; with the exception of a C16–C242-amino-3-hydroxyalkane or a C16–C242-amino-3-hydroxyalkene

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