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1. WO2012066195 - METHOD FOR PREPARING AMIDE-INITIATED POLYMERS HAVING A VARIED ARCHITECTURE

Publication Number WO/2012/066195
Publication Date 24.05.2012
International Application No. PCT/FR2011/000602
International Filing Date 14.11.2011
IPC
C08G 63/08 2006.01
CCHEMISTRY; METALLURGY
08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
GMACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING CARBON-TO-CARBON UNSATURATED BONDS
63Macromolecular compounds obtained by reactions forming a carboxylic ester link in the main chain of the macromolecule
02Polyesters derived from hydroxy carboxylic acids or from polycarboxylic acids and polyhydroxy compounds
06derived from hydroxy carboxylic acids
08Lactones or lactides
C08G 63/685 2006.01
CCHEMISTRY; METALLURGY
08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
GMACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING CARBON-TO-CARBON UNSATURATED BONDS
63Macromolecular compounds obtained by reactions forming a carboxylic ester link in the main chain of the macromolecule
68Polyesters containing atoms other than carbon, hydrogen, and oxygen
685containing nitrogen
C08G 63/82 2006.01
CCHEMISTRY; METALLURGY
08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
GMACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING CARBON-TO-CARBON UNSATURATED BONDS
63Macromolecular compounds obtained by reactions forming a carboxylic ester link in the main chain of the macromolecule
78Preparation processes
82characterised by the catalyst used
C08G 63/81 2006.01
CCHEMISTRY; METALLURGY
08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
GMACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING CARBON-TO-CARBON UNSATURATED BONDS
63Macromolecular compounds obtained by reactions forming a carboxylic ester link in the main chain of the macromolecule
78Preparation processes
81using solvents
A61K 9/14 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
14Particulate form, e.g. powders
A61K 9/16 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
14Particulate form, e.g. powders
16Agglomerates; Granulates; Microbeadlets
CPC
A61K 47/34
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
34Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
C08G 63/08
CCHEMISTRY; METALLURGY
08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
GMACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS
63Macromolecular compounds obtained by reactions forming a carboxylic ester link in the main chain of the macromolecule
02Polyesters derived from hydroxycarboxylic acids or from polycarboxylic acids and polyhydroxy compounds
06derived from hydroxycarboxylic acids
08Lactones or lactides
C08G 63/6852
CCHEMISTRY; METALLURGY
08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
GMACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS
63Macromolecular compounds obtained by reactions forming a carboxylic ester link in the main chain of the macromolecule
68Polyesters containing atoms other than carbon, hydrogen and oxygen
685containing nitrogen
6852derived from hydroxy carboxylic acids
C08G 63/81
CCHEMISTRY; METALLURGY
08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
GMACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS
63Macromolecular compounds obtained by reactions forming a carboxylic ester link in the main chain of the macromolecule
78Preparation processes
81using solvents
C08G 63/823
CCHEMISTRY; METALLURGY
08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
GMACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS
63Macromolecular compounds obtained by reactions forming a carboxylic ester link in the main chain of the macromolecule
78Preparation processes
82characterised by the catalyst used
823for the preparation of polylactones or polylactides
Applicants
  • IPSEN PHARMA S.A.S. [FR]/[FR] (AllExceptUS)
  • BOURISSOU Didier [FR]/[FR] (UsOnly)
  • MARTIN-VACA Blanca [ES]/[FR] (UsOnly)
  • ALBA Aurélie [FR]/[FR] (UsOnly)
  • CHERIF CHEIKH Roland [FR]/[ES] (UsOnly)
  • DE SOUSA DELGADO Anne-Paula [FR]/[ES] (UsOnly)
Inventors
  • BOURISSOU Didier
  • MARTIN-VACA Blanca
  • ALBA Aurélie
  • CHERIF CHEIKH Roland
  • DE SOUSA DELGADO Anne-Paula
Agents
  • RETZLER Charlotte
Priority Data
100442815.11.2010FR
Publication Language French (FR)
Filing Language French (FR)
Designated States
Title
(EN) METHOD FOR PREPARING AMIDE-INITIATED POLYMERS HAVING A VARIED ARCHITECTURE
(FR) PROCÉDÉ DE PRÉPARATION DE POLYMÈRES À ARCHITECTURE VARIÉE ET AMORÇAGE AMIDE
Abstract
(EN)
The invention relates to a method for preparing linear polymers having an amide end or having a star architecture comprising an amide core, by means of a ring opening using lactide and glycolide monomers or a lactide monomer ring in the presence of a catalyst, wherein the method includes the steps of: (i) reacting the excess monomer(s) with an initiator in a solvent, said initiator being selected from among an amine and an amino alcohol, given that the initiator has at least one primary or secondary amine function; (ii) adding a catalyst, said catalyst being a non-nucleophilic base and including at least one neutral sp2 nitrogen atom; and (iii) neutralizing the reaction mixture. Said novel method is particularly advantageous in that it can be easily monitored and enables better modulation of the polymers, and thus of the properties thereof, than the methods of the prior art. The invention also relates to novel polymers that are obtainable by means of said method.
(FR)
L'invention concerne un procédé de préparation de polymères linéaires à extrémité amide ou à architecture étoile à cœur amide par ouverture de cycle à base de monomères lactide et glycolide ou d'un monomère lactide en présence d'un catalyseur, comprenant les étapes consistant à : (i) faire réagir le ou les monomères en excès avec un amorceur dans un solvant, ledit amorceur étant choisi parmi une aminé et un aminoalcool, étant donné que l'amorceur présente au moins une fonction aminé primaire ou secondaire, (ii) ajouter un catalyseur, ledit catalyseur étant une base non nucléophile et comprenant au moins un atome d'azote neutre de type sp2, (iii) neutraliser le mélange réactionnel. Ce nouveau procédé est avantageux notamment parce qu'il est facilement contrôlable et présente une meilleure modulation des polymères et donc de leurs propriétés que les procédés de l'art antérieur. L'invention concerne également de nouveaux polymères pouvant être obtenus par ce procédé.
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