FUNDACION DE LA COMUNIDAD VALENCIANA "CENTRO DE INVESTIGACIONES PRINCIPE FELIPE"
发明人:
VICENT DOCON, MARIA JESUS,VICENT DOCÓN, María Jesús,BARZ, MATTHIAS,BARZ, Matthias,CANAL, FABIANA,CANAL, Fabiana,CONEJOS SANCHEZ, INMACULADA,CONEJOS SÁNCHEZ, Inmaculada,DURO CASTANO, AROA,DURO CASTAÑO,
申请号：
ESES2012/070740
公开号：
WO2013/060919A1
申请日:
2012.10.23
申请国别(地区):
WO
年份:
2013
代理人:
摘要：
The present invention relates to the control of the polymerization of N‑carboxyanhydrides (NCAs) of alpha‑amino acids via the use of non‑nucleophilic salts in order to obtain highly versatile polymeric architectures with low polydispersity indexes (homopolymers, diblock polymers, triblock polymers or multiblock systems), and also to processes for the preparation thereof and the use thereof in pharmaceutical compositions. Reference is specifically made to the production of functional polyglutamates with a defined structure, adjustable molecular weight and low polydispersity (D = Mw / Mn <1.3) by means of the ring‑opening polymerization of N‑carboxyanhydrides. Also, the acid groups of the polymeric chain of the polyglutamates may be activated with 4-(4,6-dimethoxy-1,3,5-triazin-2-yl)-4-methylmorpholine, which allows the incorporation of various functionalities by "post‑polymerization modification", thereby forming different reactive groups in the side chains of the polymer. The remaining reagents, such as azides, maleimides, thioles or (linear or cyclic) alkynes offer the opportunity for specific conjugation and can be used for drugs, directing units or markers. Furthermore, this functionalization strategy has also been used as a polyglutamate PEGylation mechanism, which reduces possible interactions arising from the carboxyl group load and therefore allows adjustment of the pharmacological properties of each case to the use thereof in drugs or molecular imaging agents with therapeutic and/or diagnostic applications.La presente invención se refiere al control de la polimerización de N- carboxianhídridos de α-aminoácidos (NCAs) a través del uso de sales no nucleofílicas con la finalidad de obtener arquitecturas poliméricas altamente versátiles, con bajos índices de polidispersidad, (homopolimeros, polímeros dibloque, tribloque o sistemas multibloque), así como a procesos para la preparación de los mismos y su utilización en composiciones farmacéuticas. Concretamente se
