ECSP961990A

ECSP961990A - NEW TAXOIDS, THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS THAT CONTAIN THEM

Info

Publication number: ECSP961990A
Authority: EC
Inventors: Herve Bouchard; Alain Commercon
Priority date: 1996-12-20
Filing date: 1996-12-20
Publication date: 1997-12-23

Abstract

La presente invención se refiere a nuevos taxoides de fórmula general (gráfico), a su preparación y las composiciones farmacéuticas que los contienen en la fórmula general (I) Z represente un átomo de hidrógeno o un radical de fórmula general (gráfico), en la que R1 representa un radical bencilo eventualmente substituido, furilo o tenilo o un radical R2 -O-CO- en la que R2 representa un radical alquilo, alquenilo, alquinilo, cicloalquilo, cicloalquenilo, bicicloalquilo, fenilo eventualmente substituido o heterociclilo. R3 representa un radical alquilo, alquenilo, alquenilo, alquinilo, cicloalquilo, cicloalquenilo, fenilo naftilo o heterociclico aromático o bien R4 representa un átomo de hidrógeno, R6 y R7 forman un conjunto un enlace, o bien R4 representa un átomo de hidrógheno o un radical hidroxi, o un radical alcoxi, alqueniloxi, alquiniloxi eventualmente substituido alcanoiloxi, ariloxi, alqueniloxi, alquiniloxi, cicloalcanoiloxi, alcoxiacetilo, alquiltioacetilo, alquiloxicarboniloxi, cicloalquiiloxi, cicloalqueniloxi, carbamoiloxi, alcoilcarbamoiloxi, dialcoicarbamoiloxi. R5 representa un átomo de hidrógeno, o R4 y R5 forman en conjunto una función cetona, R6 representa un átomo de hidrógeno y R y R7 forman en conjunto un enlace. Los nuevos productos de fórmula general (1) en la cual Z representa un radical de fórmula general (II), presentan propiedades antitumorales y antileucémicas notables.The present invention relates to new taxoids of the general formula (graph), their preparation and the pharmaceutical compositions containing them in the general formula (I) Z represents a hydrogen atom or a radical of the general formula (graph), in the that R1 represents an optionally substituted benzyl, furyl or tenyl radical or an R2 -O-CO- radical in which R2 represents an alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, optionally substituted phenyl or heterocyclyl radical. R3 represents an alkyl, alkenyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, phenyl naphthyl or aromatic heterocyclic radical, or R4 represents a hydrogen atom, R6 and R7 together form a bond, or R4 represents a hydrogen or radical atom. hydroxy, or an optionally substituted alkoxy, alkenyloxy, alkynyloxy radical alkanoyloxy, aryloxy, alkenyloxy, alkynyloxy, cycloalkanoyloxy, alkoxyacetyl, alkylthioacetyl, alkyloxycarbonyloxy, cycloalkyloxy, cycloalkenyloxy, carbamoyloxy, dialkylcarbamoyloxy, dialkylcarbamoyloxy. R5 represents a hydrogen atom, or R4 and R5 together form a ketone function, R6 represents a hydrogen atom and R and R7 together form a bond. The new products of general formula (1) in which Z represents a radical of general formula (II), have remarkable anti-tumor and anti-leukemic properties.