公开(公告)号：US07138547B2

公开(公告)日：2006-11-21

申请号：US10297352

申请日：2001-06-06

申请人： Jose Luis Aceña ,  Javier Adrio ,  Carmen Cuevas ,  Pilar Gallego ,  Ignacio Manzanares ,  Simon Munt ,  Ignacio Rodriguez

发明人： Jose Luis Aceña ,  Javier Adrio ,  Carmen Cuevas ,  Pilar Gallego ,  Ignacio Manzanares ,  Simon Munt ,  Ignacio Rodriguez

IPC分类号： C07C233/00 ,  C07D493/00 ,  A61K31/42 ,  A61K31/35

CPC分类号： C07D263/24 ,  C07B2200/07 ,  C07C211/15 ,  C07C215/08 ,  C07C215/52 ,  C07C217/08 ,  C07C219/06 ,  C07C225/06 ,  C07C233/18 ,  C07C233/22 ,  C07C237/08 ,  C07C251/38 ,  C07C271/16 ,  C07C271/22 ,  C07C275/10 ,  C07C275/28 ,  C07C311/04 ,  C07C335/16 ,  C07D263/22 ,  C07F9/091

摘要： 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–C18 alkyl, substituted or unsubstituted C2–C18 alkenyl, substituted or unsubstituted C2–C18 alkynyl, 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 R1 is selected to suit the valency and each R1 is independently selected of H, OH, C(═O)R′, P(═O)R′R″, substituted or unsubstituted C1–C18 alkyl, substituted or unsubstituted C2–C18 alkenyl, substituted or unsubstituted C2–C18 alkynyl, 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–C18 alkyl, substituted or unsubstituted C2–C18 alkenyl, substituted or unsubstituted C2–C18 alkenyl, substituted or unsubstituted C2–C18 alkynyl, 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; R2 is H, C(═O)R′, P(═O)R′R″, S(═O)R′R″, S(═O)2R′, substituted or unsubstituted C1–C18 alkyl, substituted or unsubstituted C2–C18 Alkenyl, substituted or unsubstituted C2–C18 alkynyl, substituted or unsubstituted aryl; R3 is H, C(═O)R′, P(═O)R′R″, S(═O)R′R″, S(═O)2R′, substituted or unsubstituted C1–C18 alkyl, substituted or unsubstituted C2–C18 alkenyl, substituted or unsubstituted C2–C18 alkynyl, 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–C18 alkyl, substituted or unsubstituted C1–C18 alkoxy, substituted or unsubstituted C2–C18 alkenyl, substituted or unsubstituted C2–C18 alkynl, 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–C24 2-amino-3-hydroxyalkane or a C16–C24 2-amino-3-hydroxyalkene