【発明の名称】抗腫瘍化合物

Japanese Patent JP2003535868

A

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, CO_2CH3, 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

Jose Luis Asenha
Javier Adrio
Carmen Cuevas
Pilar Gallego
Ignacio Manzanares
Simon Mund
Ignacio Rodríguez

JP2002501905A

December 02, 2003

June 06, 2001

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Pharma Mar Sociedad Anonima

C07D263/20; A61K31/131; A61K31/132; A61K31/133; A61K31/137; A61K31/164; A61K31/165; A61K31/17; A61K31/18; A61K31/215; A61K31/27; A61K31/421; A61K31/662; A61K31/695; A61P35/00; C07B53/00; C07C211/09; C07C211/15; C07C215/08; C07C215/18; C07C215/24; C07C215/52; C07C215/56; C07C217/08; C07C217/64; C07C219/06; C07C223/02; C07C225/06; C07C229/12; C07C229/26; C07C229/36; C07C233/18; C07C233/22; C07C237/08; C07C251/38; C07C271/12; C07C271/16; C07C271/18; C07C271/20; C07C271/22; C07C275/10; C07C275/28; C07C311/03; C07C311/04; C07C335/16; C07D263/22; C07D263/24; C07F7/18; C07F9/09; (IPC1-7): C07C223/02; A61K31/131; A61K31/132; A61K31/133; A61K31/137; A61K31/164; A61K31/165; A61K31/17; A61K31/18; A61K31/215; A61K31/27; A61K31/421; A61K31/662; A61K31/695; A61P35/00; C07C211/09; C07C211/15; C07C215/08; C07C215/18; C07C215/24; C07C215/56; C07C217/08; C07C217/64; C07C219/06; C07C225/06; C07C229/12; C07C229/26; C07C229/36; C07C233/18; C07C233/22; C07C237/08; C07C251/38; C07C271/12; C07C271/16; C07C271/18; C07C271/20; C07C275/10; C07C275/28; C07C311/03; C07C335/16; C07D263/20; C07D263/22; C07D263/24; C07F7/18; C07F9/09

WO1999052521A1

1999-10-21

Masatake Shiga (7 outside)

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