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1. WO1997023473 - NOVEL TAXOIDS, PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME

Publication Number WO/1997/023473
Publication Date 03.07.1997
International Application No. PCT/FR1996/002031
International Filing Date 19.12.1996
Chapter 2 Demand Filed 23.06.1997
IPC
C07D 305/14 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
305Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms
14condensed with carbocyclic rings or ring systems
C07D 493/08 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
493Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
02in which the condensed system contains two hetero rings
08Bridged systems
CPC
A61K 31/335
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
335having oxygen as the only ring hetero atom, e.g. fungichromin
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
C07D 305/14
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
305Heterocyclic compounds containing four-membered rings having one oxygen atoms as the only ring hetero atoms
14condensed with carbocyclic rings or ring systems
C07D 493/08
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
493Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
02in which the condensed system contains two hetero rings
08Bridged systems
Y02P 20/55
YSECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
20Technologies relating to chemical industry
50Improvements relating to the production of bulk chemicals
55Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
Applicants
  • RHONE-POULENC RORER S.A. [FR]/[FR] (AllExceptUS)
  • BOUCHARD, Hervé [FR]/[FR] (UsOnly)
  • COMMERÇON, Alain [FR]/[FR] (UsOnly)
Inventors
  • BOUCHARD, Hervé
  • COMMERÇON, Alain
Agents
  • LE PENNEC, Magali
Priority Data
95/1537922.12.1995FR
Publication Language French (FR)
Filing Language French (FR)
Designated States
Title
(EN) NOVEL TAXOIDS, PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME
(FR) NOUVEAUX TAXOIDES, LEUR PREPARATION ET LES COMPOSITIONS PHARMACEUTIQUES QUI LES CONTIENNENT
Abstract
(EN)
Novel taxoids of general formula (I), the preparation thereof and pharmaceutical compositions containing same, are disclosed. In general formula (I), Z is a hydrogen atom or a radical of general formula (II), wherein R1 is an optionally substituted benzoyl, furoyl or thenoyl radical or a radical R2-O-CO- where R2 is an alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, optionally substituted phenyl or heterocyclyl radical; R3 is an alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, phenyl, naphthyl or aromatic heterocyclic radical; or R4 is a hydrogen atom, R6 and R7 together form a ketone function, and R and R5 together form a bond; or R4 is a hydrogen atom or a hydroxy radical or an alkoxy, alkenyloxy, optionally substituted alkynyloxy, alkanoyloxy, aroyloxy, alkenoyloxy, alkynoyloxy, cycloalkanoyloxy, alkoxyacetyl, alkylthioacetyl, alkyloxycarbonyloxy, cycloalkyloxy, cycloalkenyloxy, carbamoyloxy, alkylcarbamoyloxy or dialkylcarbamoyloxy radical; R5 is a hydrogen atom, or R4 and R5 together form a ketone function, R6 is a hydrogen atom, and R and R7 together form a bond. The novel products of general formula (I), wherein Z is a radical of general formula (II), have remarkable antitumoral and antileukemic properties.
(FR)
Nouveaux taxoïdes de formule générale (I), leur préparation et les compositions pharmaceutiques qui les contiennent. Dans la formule générale (I), Z représente un atome d'hydrogène ou un radical de formule générale (II), dans laquelle R1 représente un radical benzoyle éventuellement substitué, furoyle ou thénoyle ou un radical R2-O-CO- dans lequel R2 représente un radical alcoyle, alcényle, alcynyle, cycloalcoyle, cycloalcényle, bicycloalcoyle, phényle éventuellement substitué ou hétérocyclyle; R3 représente un radical alcoyle, alcényle, alcynyle, cycloalcoyle, cycloalcényle, phényle, naphtyle ou hétérocyclique aromatique; ou bien, R4 représente un atome d'hydrogène; R6 et R7 forment ensemble une fonction cétone; et R et R5 forment ensemble une liaison; ou bien, R4 représente un atome d'hydrogène ou un radical hydroxy ou un radical alcoxy, alcényloxy, alcynyloxy éventuellement substitué, alcanoyloxy, aroyloxy, alcénoyloxy, alcynoyloxy, cycloalcanoyloxy, alcoxyacétyle, alcoylthioacétyle, alcoyloxycarbonyloxy, cycloalcoyloxy, cycloalcényloxy, carbamoyloxy, alcoylcarbamoyloxy ou dialcoylcarbamoyloxy; R5 représente un atome d'hydrogène; ou R4 et R5 forment ensemble une fonction cétone; R6 représente un atome d'hydrogène; et R et R7 forment ensemble une liaison. Les nouveaux produits de formule générale (I) dans laquelle Z représente un radical de formule générale (II) présentent des propriétés antitumorales et antileucémiques remarquables.
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