Rhone-poulenc Rorer S.a.

Aventis Pharma S.a.

Sanofi

Centre National De La Recherche Scientifique

Université Paul Sabatier (toulouse Iii)

Eric Didier

Alain Commercon

Elie Fouque

Patrick Leon

Jean-Rene Authelin

Jean-Christophe Carry

Frank Halley

Laurent Schio

Bruno Filoche-Romme

Gilles Doerflinger

Fabienne Thompson

Didier Bourissou

Maurice Brollo

Victor Certal

Youssef El Ahmad

Gilles Oddon

Karl Andreas Karlsson

Michel Lavigne

Denis Pauze

Lionel Zaske

Harivardhan Reddy Lakkireddy

Isabelle Taillepied

Didier Bazile

Marc-Antoine Perrin

Didier Riguet

Franck Leveiller

Pascal Pecquet

Guy Amouret

Fethi Bensaid

Nicolas Tremaudeux

Abderrhamane Amgoune

Michel Veillard

Serge Sable

Stephanie Greco

The present invention relates to a novel crystalline ethyl acetate solvate form of cabazitaxel or 4&#x3b1;-acetoxy-2&#x3b1;-benzoyloxy-5&#x3b2;,20-epoxy-1&#x3b2;-hydroxy-7&#x3b2;,10&#x3b2;-dimethoxy-9-oxo-11-taxen-13&#x3b1;-yl(2R,3S)-3-tert-butoxycarbonylamino-2-hydroxy-3-phenylpropionate and process for preparing the same.

Crystalline form of cabazitaxel and process for preparing the same

The present invention relates to novel conjugates of active principles grafted to a polymer, to the nanoparticles comprising them, to their preparation and to their polymeric intermediates.

Polymeric conjugates of active principles, their process of preparation and their polymeric intermediates

The present invention relates to novel chemical compounds derived from pyrimidines, to the method for preparing same, to the novel intermediates obtained, to the use thereof as drugs, to the pharmaceutical compositions containing same, and to the therapeutic use thereof as AKT inhibitors.

Pyrimidine derivatives, preparation thereof, and pharmaceutical use thereof as akt(pkb) phosphorylation inhibitors

This invention discloses and claims an acetone solvate of dimethoxydocetaxel or 4-acetoxy-2&#x3b1;-benzoyloxy-5&#x3b2;,20-epoxy-1-hydroxy-7&#x3b2;,10&#x3b2;-dimethoxy-9-oxotax-11-en-13&#x3b1;-yl (2R,3S)-3-tert-butoxycarbonylamino-2-hydroxy-3-phenylpropionate and its preparation by crystallization from an aqueous/acetone solution.

Acetone solvate of dimethoxy docetaxel and its process of preparation

There is disclosed a process for the preparation of 4-acetoxy-2&#x3b1;-benzoyloxy-5&#x3b2;,20-epoxy-1,13&#x3b1;-dihydroxy-9-oxo-19-norcyclopropa[g] tax-11-ene from 4-acetoxy-2&#x3b1;-benzoyloxy-5&#x3b2;,20-epoxy-1,13&#x3b1;-dihydroxy-9-oxo-7&#x3b2;-(trifluoromethyl sulfonyloxy) tax-11-ene by reaction with a molecular sieve in sulfolane.

Process for the preparation of 4,10&#x3b2;-diacetoxy-2&#x3b1;-benzoyloxy-5&#x3b2;,20-epoxy-1,13&#x3b1;-dihydroxy-9-oxo-19-norcyclopropa[g]tax-11-ene

The present invention is directed to 4,10.beta.-diacetoxy-2.alpha.-benzoyloxy-5.beta.,20-epoxy-1-hydroxy-9-oxo- 19-norcyclopropa(g)tax-11-en-13.alpha.-yl (2r,3s)-3-tert-butoxycarbonylamino-2-hydroxy-3-phenylpropionate dihydrate and a process for its preparation.

4,10-.beta.-diacetoxy-

Taxane hydroxy monoacylation method

Method for preparing 4, 10-diacetoxy-2.alpha.-benzoyloxy-5.beta.,

The present invention relates to a novel process for preparing dialkoxy derivatives of the taxoid family by direct alkylation of the two positions 7 and 10 of deacetylbaccatin or derivatives thereof which are esterified in position 13.

Process for preparing derivatives of the taxoid family

This invention relates to a method of preparing taxane derivatives of formula (VIII) by esterification of protected baccatin III or 10-deacetylbaccatin III by means of an acid of formula (VII), elimination of protection groupings and acylation of the amine function of the side chain. In formulae (VIII) and (VII): Ar stands for aryl, R.sub.3 is a trihalomethyl radical or phenyl substituted by a trihalomethyl radical, R.sub.4 is a hydrogen atom or is the same as R.sub.1. G.sub.1 and G.sub.2 are hydroxy protecting groups. ##STR1##

Process for the preparation of taxane derivatives

This invention relates to a method of preparing taxane derivatives of formula (I) by esterification of protected baccatin III or 10-deacetylbaccatin III by means of an acid of formula (VII), elimination of protection groupings and acylation of the amine function of the side chain. The products of formula (I) have remarkable antitumor and antileukemia properties. In formulae (I) and (VII): Ar stands for aryl, R is hydrogen or acetyl, R.sub.1 is a benzoyl radical or an R.sub.2 --O--CO-- radical in which R.sub.2 is alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, phenyl or heterocyclyl, R.sub.3 is a trihalomethyl radical or phenyl substituted by a trihalomethyl radical, R.sub.4 is a hydrogen atom or is the same as R.sub.1. ##STR1##

Method for the preparation of .beta.-phenylisoserine derivatives

Process for preparing taxane derivatives

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Paris, France

Eric Didier