Pharmaceutical composition containing at least a polymer combined with or conjugated to at least a phenylalkylcarboxylic acid salt, conjugate polymers and uses thereof
OwnerThierry Avramoglou, Rosita Bagheri +7inventors
InventorsThierry Avramoglou, Rosita Bagheri, Frederic Chaubet, Michel Crepin, Latifa Dahri, Melanie Dibenedetto, Claudia Gervelas, Remi Huynh, Jacqueline Jozefonvicz
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Abstract
The invention concerns a pharmaceutical composition containing at least a polymer associated or conjugated with at least a phenylalkylcarboxylic acid derivative, novel polymers conjugated with at least a phenylalkylcarboxylic acid derivative and their uses in particular in cancer treatment.
Claims16
A pharmaceutical composition, characterized in that it comprises, as active principle, at least one composition chosen from the group consisting of:
- a) a conjugate of a polymer comprising at least one free hydroxyl function and of at least one phenylalkylcarboxylic acid derivative of formula (I) below:
- R2—(CH2)n—COOR1 (I)
- in which:
- R1 represents a hydrogen atom, a halogen atom, an atom of a monovalent alkali metal such as sodium or potassium, or a group —CO(CH2)mR3,
- R2 and R3 represent an unsubstituted phenyl radical,
- n and m, which are identical, are integers of between 1 and 3 inclusive;
- said conjugate corresponding to formula (III) below:
- (Polymer)-(OOC—(CH2)n—R2)d (III)
- in which the polymer comprises at least one free hydroxyl function, n is an integer of between 1 and 3 inclusive, R2 represents an unsubstituted phenyl radical and d, which is the index of substitution (ds) of derivative of formula (I), is ≧0.05 and ≦1.5, and preferably >0.15;
- b) a combination of at least one polymer having a molecular mass of greater than or equal to 5000 Da and comprising at least one free hydroxyl function, and of at least one phenylalkylcarboxylic acid salt of formula (I′) below:
- R′2—(CH2)n′—COOR′1 (I′)
- in which:
- R′1 is an atom of a monovalent alkali metal such as sodium or potassium,
- R′2 represents an unsubstituted phenyl radical,
- n′ is an integer of between 1 and 3 inclusive;
- c) and mixtures thereof, and optionally one or more other additional active principles, and possibly in the presence or not of a pharmaceutically acceptable vehicle and/or of a physiologically acceptable carrier.
The pharmaceutical composition as claimed in any one of the preceding claims, characterized in that the phenylalkylcarboxylic acid salts of formula (I′) are chosen from sodium phenylacetate, potassium phenylacetate, sodium phenylpropionate, potassium phenylpropionate, sodium phenylbutyrate and potassium phenylbutyrate.
The pharmaceutical composition as claimed in any one of the preceding claims, characterized in that the ratio of concentration between the polymer(s), firstly, and the phenylalkylcarboxylic acid salt(s) of formula (I′), secondly, is between 10:1 and 1:1.
The composition as claimed in any one of the preceding claims, characterized in that it has the following biological activities:
- antiproliferative, cytostatic, necrotizing, proapoptotic, antiangiogenic, antimetastatic and mitogenic factor-inhibiting activities.
The composition as claimed in any one of the preceding claims, characterized in that it is intended to be administered systemically.
Dependencies are inferred from the claim text.